Search Result
Results for "
PARP inhibitor
" in MedChemExpress (MCE) Product Catalog:
6
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-117889
-
|
PARP
Apoptosis
|
Cancer
|
PARP14 inhibitor H10, compound H 10, is a selective inhibitor against PARP14 (IC50=490 nM), over other PARPs (≈24 fold over PARP1). PARP14 inhibitor H10 induces caspase-3/7-mediated cell apoptosis .
|
-
-
- HY-125218
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ITK7
|
PARP
|
Cancer
|
PARP11 inhibitor ITK7 (ITK7) is a potent and selective PARP11 inhibitor. PARP11 inhibitor ITK7 can potently inhibit PARP11 with an IC50 value of 14 nM. PARP11 inhibitor ITK7 can be used for the research of cellular localization .
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-
-
- HY-10885
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ABT-472
|
PARP
|
Cancer
|
A-620223 succinate (ABT-472) is an orally available poly(ADP-ribose) polymerase (PARP) inhibitor. A-620223 succinate (ABT-472) exhibits very good potency against the PARP-1 enzyme with a Ki value of 8 nM and an EC50 value of 3 nM in whole cell assay, making it useful in cancer research .
|
-
-
- HY-157165
-
|
Microtubule/Tubulin
PARP
|
Cancer
|
Tubulin/PARP-IN-1 (compound 14) is a dual PARP-tubulin inhibitor with activity against endometrial cancer. Tubulin/PARP-IN-1 inhibits PARP and tubulin with IC50s of 74 nM (PARP1), 109 nM (PARP2), and 1.4 μM (Microtubule/Tubulin), respectively. Tubulin/PARP-IN-1 can induce apoptosis and autophagy and cause cell cycle arrest in the G2/M phase .
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-
-
- HY-160409
-
|
Others
|
Cancer
|
TopBP1-IN-1 is a TopBP1 inhibitor. TopBP1-IN-1 has a synergistic effect with PARP inhibitors. TopBP1-IN-1 has antitumor activity .
|
-
-
- HY-120115
-
Olaparib-bodipy FL
|
PARP
|
Cancer
|
PARPi-FL is a small molecule and fluorescent inhibitor of PARP1. PARPi-FL is a highly selective probe and can be used as an imaging agent to detect glioblastomas in vivo .
|
-
-
- HY-W424851
-
6,7-Dimethoxy-2-(1-piperazinyl)-4-quinazolinamine hydrochloride
|
PARP
|
Infection
Inflammation/Immunology
|
DPQ hydrochloride (6, 7-dimethoxy-2 -(1-piperazinyl)-4-quinazolinamine hydrochloride) is a PARP1 inhibitor, with IC50 value of 40 nM. DPQ hydrochloride has anti-inflammatory and antiviral activity. DPQ hydrochloride is used to study acute lung injury .
|
-
-
- HY-161431
-
|
DNA/RNA Synthesis
|
Cancer
|
RTx-152 traps Polθ on DNA and is an allosteric Polθ-pol inhibitor (IC50: 6.2 nM). RTx-152 selectively kills HR-deficient cancer cells, and suppresses PARP inhibitor resistance in multiple genetic backgrounds, including homologous recombination (HR)-proficient cells. RTx-152 selectively kills BRCA2-null cells .
|
-
-
- HY-13540
-
GPI 21016
|
PARP
|
Cancer
|
E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent .
|
-
-
- HY-148566
-
|
PARP
|
Cancer
|
OUL232 is a potent inhibitor of mono-ARTs PARP7, PARP10, PARP11, PARP12, PARP14, and PARP15. OUL232 is the most potent PARP10 inhibitor described to date (IC50=7.8 nM), as well as the first PARP12 inhibitor ever reported .
|
-
-
- HY-157137
-
|
PARP
Caspase
Apoptosis
|
Cancer
|
PARP1-IN-17 is a PARP-1 inhibitor (IC50 = 19.24 nM for PARP-1 and = 32.58 nM for PARP-2) and induce apoptosis. PARP1-IN-17 shows excellent anti-proliferative activity .
|
-
-
- HY-153590
-
|
PARP
|
Cancer
|
PARP-1-IN-4 is a PARP-1 inhibitor. PARP-1-IN-4 has inhibitory activity against PARP-1 with IC50 value of 302 μM. PARP-1-IN-4 can be used for the research of lung adenocarcinoma .
|
-
-
- HY-147886
-
|
PARP
|
Cancer
|
PARP1-IN-11 (compound 49) is a potent PARP1 inhibitor with IC50 value of 0.082 µM. PARP1-IN-11 shows complete inhibition of PARP2 and substantially inhibits PARP3, TNKS1 and TNKS2 .
|
-
-
- HY-14478
-
|
PARP
|
Cancer
|
UPF 1069 is a PARP inhibitor, with IC50s of 8 and 0.3 μM for PARP-1 and PARP-2, respectively.
|
-
-
- HY-102035
-
|
PARP
|
Cancer
|
PARP-2-IN-1 is a potent and selective PARP-2 inhibitor with an IC50 of 11.5 nM.
|
-
-
- HY-143398
-
|
PARP
|
Cancer
|
PARP10/15-IN-1 (compound 8l) is a potent inhibitor of dual inhibitor of PARP10 and PARP15, with IC50s of 160 nM and 370 nM, respectively. PARP10/15-IN-1 can be used for cancer .
|
-
-
- HY-105253
-
|
PARP
|
Neurological Disease
|
PARP-2/1-IN-2 (Compound 4a), the enantiomer of Veliparib (HY-10129), is a potent PARP inhibitor with Kis of 2 and 5 nM against PARP-2 and PARP-1, respectively. PARP-2/1-IN-2 has an EC50 of 3 nM in a cell based assay of PARP activity .
|
-
-
- HY-155122
-
|
PARP
|
Cancer
|
PARP-1-IN-13 (Compound 19c) is a PARP-1 inhibitor (IC50: 26 nM). PARP-1-IN-13 inhibits DNA single-strand breakage repair and aggravates DNA double-strand breakage. PARP-1-IN-13 promotes the apoptosis of cancer cells through the mitochondrial apoptosis pathway .
|
-
-
- HY-148754
-
|
PARP
|
Cancer
|
PARP10-IN-3 is a selective mono‐ADP‐ribosyltransferase PARP10 inhibitor with an IC50 of 480 nM for human PARP10. PARP10-IN-3 reveals potent inhibition on PARP2 and PARP15 with IC50s of 1.7 μM for human PARP2 and human PARP15, respectively .
|
-
-
- HY-149800
-
|
PARP
Apoptosis
Caspase
|
Cancer
|
PARP-1-IN-3, a benzamide derivative, is a potent PARP-1 inhibitor with IC50 values of 0.25 nM and 2.34 nM for PARP-1 and PARP-2, respectively. PARP-1-IN-3 induces apoptosis and arrest cell cycle at G2/M phase. PARP-1-IN-3 can be used in research of cancer .
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-
-
- HY-10617
-
AG-014699 phosphate; PF-01367338 phosphate
|
PARP
|
Cancer
|
Rucaparib (AG014699) phosphate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib phosphate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib phosphate has the potential for castration-resistant prostate cancer (CRPC) research .
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-
-
- HY-10617A
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AG014699; PF-01367338
|
PARP
|
Cancer
|
Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research .
|
-
-
- HY-10617D
-
AG014699 acetate; PF-01367338 acetate
|
PARP
|
Cancer
|
Rucaparib (AG014699) acetate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib acetate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib acetate has the potential for castration-resistant prostate cancer (CRPC) research .
|
-
-
- HY-10617B
-
AG014699 hydrochloride; PF-01367338 hydrochloride
|
PARP
|
Cancer
|
Rucaparib (AG014699) hydrochloride is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib hydrochloride is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib hydrochloride has the potential for castration-resistant prostate cancer (CRPC) research .
|
-
-
- HY-119653
-
|
PARP
|
Cancer
|
AZ9482 is a triple PARP1/2/6 inhibitor, with IC50 values of 1 nM, 1 nM and 640 nM for PARP1, PARP2 and PARP6, respectively .
|
-
-
- HY-149398
-
|
Apoptosis
PARP
CDK
|
Cancer
|
PARP-1/2-IN-2-IN-1 (Compound 12e) is a PARP1/2/CDK12 inhibitor (IC50: 34, 30 and 285 nM respectively). PARP-1/2-IN-2 inhibits DNA damage repair, promotes cell cycle arrest and apoptosis. PARP-1/2-IN-2 inhibits the growth of TNBC cells and TNBC xenograft tumor .
|
-
-
- HY-102003
-
AG014699 monocamsylate; PF-01367338 monocamsylate
|
PARP
|
Cancer
|
Rucaparib (AG014699) monocamsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib monocamsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib monocamsylate has the potential for castration-resistant prostate cancer (CRPC) research .
|
-
-
- HY-102003A
-
AG014699 camsylate; PF-01367338 camsylate
|
PARP
|
Cancer
|
Rucaparib (AG014699) camsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib camsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib camsylate has the potential for castration-resistant prostate cancer (CRPC) research .
|
-
-
- HY-10617C
-
AG-014699 tartrate; PF-01367338 tartrate
|
PARP
|
Cancer
|
Rucaparib (AG014699) tartrate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib tartrate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib tartrate has the potential for castration-resistant prostate cancer (CRPC) research .
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-
-
- HY-155246
-
|
Apoptosis
PARP
|
Cancer
|
PARP1-IN-15 (Compound 6) is a PARP1 inhibitor. PARP1-IN-15 inhibits tankyrase (TNKS) and facilitates DNA double-strand breaks damage. PARP1-IN-15 induces tumor cell apoptosis. PARP1-IN-15 has anti-cancer activity in triple-negative breast cancer (TNBC) cells and TNBC patient-derived organoids. PARP1-IN-15 can be used for research of TNBC with or without BRCA1 mutations .
|
-
-
- HY-132297A
-
|
PARP
|
Cancer
|
PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer .
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-
-
- HY-132297
-
|
PARP
|
Cancer
|
PARP1-IN-5 is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 can be used for the research of cancer .
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-
-
- HY-151609
-
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PARP
|
Cancer
|
PARP7-IN-12 is a potent PARP7 Inhibitor with an IC50 value of 7.836 nM. PARP7-IN-12 can be used in research of cancer .
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-
-
- HY-163492
-
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PARP
|
Cancer
|
PARP7-IN-19 (compound 5a) is an inhibitor of PARP7 ( IC50 ≤10nM). PARP7-IN-19 can be used in the research area of tumors .
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-
-
- HY-148753
-
|
PARP
|
Cancer
|
PARP10-IN-2 is a potent mono‐ADP‐ribosyltransferase PARP10 inhibitor with an IC50 of 3.64 μM for human PARP10. PARP10-IN-2 reveals potent inhibition on PARP2 and PARP15 with IC50s of 27 μM and 11 μM for human PARP2 and human PARP15, respectively .
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-
-
- HY-145328
-
|
PARP
|
Others
|
PARP-1/2-IN-1 is a potent PARP-1/2 inhibitor with IC50 of 0.51 nM and 23.11 nM, respectively.
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-
-
- HY-163081
-
|
PARP
|
Cancer
|
PARP7-IN-17 is a potent inhibitor of PARP7 with IC50 of 4.5 nM that has oral bioavailability. PARP7-IN-17 displays antitumor effect .
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-
-
- HY-162114
-
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PARP
|
Cancer
|
PARP1-IN-18 (compound 25) is a potent PARP1 inhibitor with an IC50 value of 2.7 nM. PARP1-IN-18 has anticancer effects .
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-
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- HY-151625
-
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PARP
Apoptosis
|
Cancer
|
PARP-2-IN-3 (Compound 12) is a potent PARP-2 inhibitor with an IC50 of 0.07 μM. PARP-2-IN-3 induces apoptosis and necrosis in cancer cells. PARP-2-IN-3 shows appropriate predicted pharmacokinetic parameters and oral bioavailability .
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-
-
- HY-145749
-
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PARP
|
Cancer
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PARPYnD is a PARP enzyme photoaffinity probe (AfBP) based on the triple PARP1/2/6 inhibitor AZ9482 (HY-119653), which induces breast cancer Formation of multipolar spindles (MPS) in cells. PARPYnD inhibits PAPR wih IC50 of 38 nM (PARP1), 6 nM (PARP2), 230 nM (PARP6), respectively. PARPYnD enriches recombinant PARP6 incorporated into cell lysates and inhibits PARP6 in cell-free assays, but it does not label PARP6 in intact cells .
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-
-
- HY-13536
-
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PARP
|
Cancer
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AZD-2461 is a potent PARP inhibitor, with IC50s of 5 nM, 2 nM and 200 nM for PARP1, PARP2 and PARP3, respectively.
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-
-
- HY-157490
-
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PARP
HDAC
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Cancer
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PARP/HDAC-IN-1 (compound B102) is a potent dual inhibitor of PARP and HDAC. PARP/HDAC-IN-1 inhibits PARP1, PARP2 and HDAC1 with IC50s of 19.01, 2.13, 1690 nM, respectively .
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-
-
- HY-162172
-
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PARP
|
Cancer
|
Parp7-in-18 (Compund 8) is a selective PARP7 inhibitor with an IC50 of 0.11 nM. PARP7-IN-18 exhibits good anticancer activity and pharmacokinetic properties .
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-
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- HY-146502
-
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PARP
Apoptosis
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Cancer
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PARP10/15-IN-3 (Compound 8a) is a potent PARP10 and PARP15 dual inhibitor with IC50 values of 0.14 µM and 0.40 µM against PARP10 and PARP15, respectively. PARP10/15-IN-3 is able to enter cells and rescue cells from apoptosis .
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-
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- HY-151624
-
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PARP
Apoptosis
|
Cancer
|
PARP-2-IN-2 (compound 27) is a PARP‑2 inhibitor with an IC50 value of 0.057 µM. PARP-2-IN-2 induces cell cycle arrest and apoptosis of MCF-7 breast cancer cells. PARP-2-IN-2 can be used for the research of cancer .
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-
-
- HY-162349
-
|
HDAC
PARP
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Cancer
|
PARP7/HDACs-IN-1 (compound 9l) is a dual-target inhibitor targeting PARP7/HDAC with anti-tumor activity. PARP7/HDACs-IN-1 inhibits different subtypes of PARPs and HDACs with IC50s of 83.3 nM (PARP1), 3.1 nM (PARP7), 35 nM (HDAC1), 30.3 nM (HDAC2), 35.4 nM (HDAC3), and 6.4 nM respectively. (HDAC6) . br/ .
|
-
-
- HY-144338
-
|
Epigenetic Reader Domain
PARP
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
PARP1/BRD4-IN-1 is a potent and high selective PARP1/BRD4 inhibitor (IC50s of 49 and 202 nM in PARP1 and BRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells .
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-
-
- HY-158680
-
|
PARP
|
Cancer
|
PARP1-IN-21 (example 16) is a potent inhibitor of PARP1, with the IC50 of < 10 nM .
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-
-
- HY-158681
-
|
PARP
|
Cancer
|
PARP1-IN-22 (compound 15) is a potent inhibitor of PARP1, with the IC50 of < 10 nM .
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-
-
- HY-161607
-
|
PARP
|
Cancer
|
PARP7-IN-21 (compound 128) is a potent inhibitor of PARP7, with the IC50 of < 10 nM .
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- HY-161606
-
|
PARP
|
Cancer
|
PARP-1/2/7-IN-1 (compound 86) is a potent inhibitor of PARP-1/2/7, with IC50s of < 10 nM .
|
-
- HY-157212
-
|
Apoptosis
PARP
Proteasome
|
Cancer
|
PARP-1/Proteasome-IN-1 (compound 42i) is a dual PARP-1 and proteasome inhibitor with significant inhibitory effects on breast cancer. PARP-1/Proteasome-IN-1 can downregulate the expression of BRCA1 and RAD51 to inhibit homologous recombination repair function and induce apoptosis .
|
-
- HY-146501
-
|
PARP
Apoptosis
|
Cancer
|
PARP10/15-IN-2 (Compound 8h) is a potent PARP10 and PARP15 dual inhibitor with IC50 values of 0.15 µM and 0.37 µM against PARP10 and PARP15, respectively. PARP10/15-IN-2 is able to enter cells and rescue cells from apoptosis .
|
-
- HY-10129
-
ABT-888
|
PARP
Autophagy
|
Cancer
|
Veliparib (ABT-888) is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively .
|
-
- HY-149001
-
|
PARP
|
Cancer
|
PARP1-IN-9 (Compound 5c) is a PARP1 inhibitor with an IC50 of 30.51 nM. PARP1-IN-9 induces cell apoptosis and shows anticancer activity. PARP1-IN-9 has higher potency than Olaparib (HY-10162) .
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-
- HY-108632
-
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PARP
|
Cancer
|
BYK204165 is a potent and selective PARP1 inhibitor. BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with a pIC50 of 7.35 (pKi=7.05), and murine PARP-2 (mPARP-2) with a pIC50 of 5.38, respectively. BYK204165 displays 100-fold selectivity for PARP-1 .
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- HY-160417
-
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PARP
|
Cancer
|
PARP1-IN-19 is a PARP1 inhibitor with antitumor effects (CN107955001A; Embodiment 3) .
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- HY-157320
-
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Microtubule/Tubulin
Apoptosis
|
Cancer
|
Tubulin/PARP-IN-2 (compound 14) is a dual PARP-Tubulin inhibitor. Tubulin/PARP-IN-2 inhibits PARP1, PARP2, and tubulin activity with IC50 values of 74 nM, 109 nM, and 1.4 µM, respectively. Tubulin/PARP-IN-2 induces apoptosis as well as autophagy. Tubulin/PARP-IN-2 causes cell cycle arrest at the G2/M phase .
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-
- HY-146336
-
|
PARP
Apoptosis
|
Cancer
|
PARP1/2/TNKS1/2-IN-1 (Compound I-9) is a dual PARP-1, PARP-2, TNKS1 and TNKS2 inhibitor with IC50 values of 0.25 nM, 1.2 nM, 13.5 nM and 4.15 nM against PARP-1, PARP-2, TNKS1 and TNKS2, respectively. PARP1/2/TNKS1/2-IN-1 exhibits favorable synergistic antitumor efficacy and induces apoptosis .
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-
- HY-142657
-
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PARP
|
Cancer
|
PARP1-IN-7 is an inhibitor of poly(ADP-ribose) polymerase-1 (PARP1) as an anticancer agent.
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-
- HY-144642
-
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PARP
|
Cancer
|
PARP-1-IN-1 is a high selective and orally active PARP-1 inhibitor (IC50=0.96 nM). PARP-1-IN-1 has well tolerance and remarkable single dose activity in the MDA-MB-436 xenotransplantation model .
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-
- HY-143338
-
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PARP
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Cancer
|
ART-IN-1 (compound 7) is a selective PARP inhibitor with IC50s of 19, 22, 2.4, >100, 1.1 µM for PARP2, TNKS2, PARP10, PARP14, PARP15, respectively .
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- HY-155351
-
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PARP
|
Cancer
|
PARP7-IN-15 (Compound 18) is a PARP7 inhibitor with IC50 of 0.56 nM, that has antitumor activity .
|
-
- HY-148709
-
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PARP
|
Inflammation/Immunology
|
ARTD10/PARP10-IN-1 (compound 23) is a potent and non-selective PARP inhibitor, targeting to mono-ADP-ribosyltransferases ARTD7/PARP15, ARTD8/PARP14, ARTD10/PARP10 and poly(ADP-ribose) polymerase-1 (ARTD1/PARP1) with IC50s of 1.7 μM, 1.6 μM, 0.8 μM, and 4.4 μM, respectively .
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-
- HY-156298
-
|
PARP
Apoptosis
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Cancer
|
PARP1-IN-16 (compound 12a) is a potent PARP1 inhibitor, with an IC50 of 1.89 nM. PARP1-IN-16 can arrest the cell cycle in S phase and induce apoptosis in HCT-116 cells .
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-
- HY-153581
-
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Others
|
Others
|
ARTD3/PARP3-IN-1 is an unselective inhibitor of diphtheria toxin-like ADP-ribosyltransferase 3 (ARTD3)/PARP3 .
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-
- HY-16106
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BMN-673; LT-673
|
PARP
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Cancer
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Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity .
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-
- HY-108413
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BMN 673ts
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PARP
|
Cancer
|
Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1.
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-
- HY-146160
-
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PARP
HDAC
|
Cancer
|
PARP-1/HDAC-IN-1 is a PARP-1/HDAC6 dual targeting inhibitor with IC50s of 68.90 nM and 510 nM, respectively. PARP-1/HDAC-IN-1 displays remarkable anticancer, anti-migration and anti-angiogenesis activities .
|
-
- HY-156419
-
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PARP
|
Cancer
|
PARP7-IN-16 (compound 36) is a potent, selective and orally active inhibitor of PARP-1/2/7, with IC50s of 0.94, 0.87 and 0.21 nM, respectively. PARP7-IN-16 can be used for the research of breast cancer and prostate cancer .
|
-
- HY-147027
-
|
PARP
Caspase
Apoptosis
|
Cancer
|
PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis .
|
-
- HY-139879
-
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PARP
|
Cancer
|
PARP1-IN-6 is a dual tubulin/PARP-1 inhibitor with IC50 values of 0.94 and 0.48 μM, respectively.
|
-
- HY-150765
-
|
PARP
Apoptosis
|
Cancer
|
PARP1-IN-12 is a potent PARP1 inhibitor with an IC50 of 2.99 nM. PARP1-IN-12 exhibits antiproliferative activity, can induce cell apoptosis and cause cycle arrest at G2/M phase. PARP1-IN-12 also can induce DNA double strand breaks (DSBs) in BRCA-deficient cells .
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-
- HY-148710
-
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PARP
|
Inflammation/Immunology
|
ARTD10/PARP10-IN-2 (compound 19) is a potent and non-selective PARP inhibitor, targeting to mono-ADP-ribosyltransferases ARTD10/PARP10 and poly(ADP-ribose) polymerase-1 ARTD1/PARP1 with IC50s of 2.0 μM, and 9.7 μM, respectively .
|
-
- HY-15050
-
-
- HY-13688
-
|
PARP
|
Cancer
|
PJ34 hydrochloride is an inhibitor of PARP1/2 with IC50 of 110 nM and 86 nM, respectively.
|
-
- HY-147030
-
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PARP
|
Cancer
|
PARP1-IN-8 (compound 11c) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 97 nM. PARP1-IN-8 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549 .
|
-
- HY-150613
-
|
Epigenetic Reader Domain
PARP
Apoptosis
|
Cancer
|
PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) .
|
-
- HY-150207
-
|
PARP
|
Inflammation/Immunology
|
RBN-3143 is a potent and NAD+-competitive catalytic PARP14 inhibitor with an IC50 value of 4 nM. RBN-3143 inhibits PARP14-mediated ADP-ribosylation and stabilizes PARP14 in cell lines. RBN-3143 can be used in research of lung inflammation .
|
-
- HY-105303
-
|
PARP
|
Cancer
|
CEP-9722, the proagent of CEP-8983, is a selective and orally active PARP-1 and PARP-2 inhibitor with IC50s of 20 nM and 6 nM, respectively. CEP-9722 has anticancer effects .
|
-
- HY-105692
-
|
PARP
|
Neurological Disease
|
DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo .
|
-
- HY-149003
-
|
PARP
Apoptosis
|
Cancer
|
PARP1-IN-10 (compound 12c) is a no-cytotoxicity and potent PARP1 inhibitor with an IC50 value of 50.62 nM in vitro. PARP1-IN-10 causes cell cycle arrest at G2/M phase and apoptosis, and enhances the cytotoxicity of temozolomide (TMZ) .
|
-
- HY-12418
-
E7449; 2X-121
|
PARP
|
Cancer
|
Stenoparib (E7449) is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ∼50 and ∼50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD + as substrate.
|
-
- HY-145804
-
|
PPAR
|
Neurological Disease
|
AZD-9574 is a potent and brain penetrant PARP1 inhibitor and shows >8000-fold selectivity for PARP1 compared to PARP2/3/5a/6. AZD-9574 acts by selectively inhibiting and trapping PARP1 at the sites of SSBs. AZD-9574 is an anti-cancer agent and can be used for HRD + breast cancer and advanced solid malignancies research .
|
-
- HY-116218
-
JPI-289
|
PARP
|
Cardiovascular Disease
Neurological Disease
|
Amelparib is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib inhibits PARP-1 activity (IC50 =18.5 nmol/L) and cellular PAR formation (IC50 =10.7 nmol/L) in the nanomolar range. Amelparib is a potential neuroprotective agent. Amelparib has the potential for the research of acute ischaemic stroke .
|
-
- HY-116218C
-
JPI-289 hydrochloride
|
PARP
|
Cardiovascular Disease
Neurological Disease
|
Amelparib (JPI-289) hydrochloride is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib hydrochloride inhibits PARP-1 activity (IC50 = 18.5 nM) and cellular PAR formation (IC50 = 10.7 nM). Amelparib hydrochloride is a potential neuroprotective agent. Amelparib hydrochloride has the potential for the research of acute ischaemic stroke .
|
-
- HY-161517
-
|
PARP
|
Cancer
|
PARP1-IN-20 (compound 19A10) is a potent inhibitor of PARP1, with the IC50 of 4.62 nM and has similar low PARP-Trapping effect compared with Veliparib(HY-10129, IC50 (MDA-MB-436) >100 μM) .
|
-
- HY-137457
-
IDX-1197
|
PARP
|
Cancer
|
Venadaparib (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC50s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib does not sensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSB) and can be used for solid tumors research .
|
-
- HY-161372
-
|
PARP
c-Met/HGFR
Apoptosis
|
Cancer
|
PARP1/c-Met-IN-1 (Compound 16) is a selective dual inhibitor for PARP1 and c-Met, with IC50s of 3.3 and 32.2 nM, respectively. PARP1/c-Met-IN-1 induces cell apoptosis and cell cycle arrest in G2/M phase in MDA-MB-231 cells. PARP1/c-Met-IN-1 exhibits antitumor activity in mice .
|
-
- HY-155766
-
|
PARP
Apoptosis
|
Cancer
|
PARP1-IN-14 (compound 19k) is a potent PARP1 inhibitor, with an IC50 of 0.6 ± 0.1 nM. PARP1-IN-14 exhibits antiproliferative effect against both MDA-MB-436 (BRCA1 −/−) and Capan-1 (BRCA2 −/−) cells with IC50 values below 0.3 nM .
|
-
- HY-18954
-
|
PARP
|
Cancer
|
NMS-P118 is a potent, orally available, and highly selective PARP-1 Inhibitor for cancer therapy.
|
-
- HY-U00223
-
|
PARP
|
Cancer
|
WD2000-012547 is a selective poly(ADP-ribose)-polymerase (PARP-1) inhibitor with a pKi of 8.221.
|
-
- HY-123512
-
NSC39047
|
PARP
|
Cancer
|
OUL35 (NSC39047) is a potent and selective inhibitor of ARTD10 (PARP-10), with an IC50 of 329 nM .
|
-
- HY-114324A
-
|
PROTACs
PARP
|
Cancer
|
rel-PROTAC PARP1 degrader is the relative configuration of ROTAC PARP1 degrader (HY-114324). ROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
|
-
- HY-14688
-
|
PARP
|
Cancer
|
CEP-8983 is a PARP-1 and PARP-2 inhibitor (IC50: 20 and 6 nM). CEP-8983 is an effective chemosensitizing agent, and can sensitize chemotherapy-resistant cell lines and subcutaneous xenografts to Temozolomide (HY-17364) and Camptothecin (HY-16560) .
|
-
- HY-132167
-
AZD5305
|
PARP
|
Cancer
|
Saruparib (AZD5305) is a potent, orally active and selective PARP inhibitor and trapper with IC50 values of 3 nM and 1400 nM for PARP1 and PARP2, respectively. Saruparib has anti-proliferative activity and inhibits growth in cells with deficiencies in DNA repair .
|
-
- HY-161083
-
|
PARP
Histone Methyltransferase
|
Cancer
|
PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC50 values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy .
|
-
- HY-158045
-
|
PROTACs
PARP
|
Inflammation/Immunology
Cancer
|
PROTAC PARP1 degrader-1 (Compound CN0) is a PROTAC degrader of PARP1. PROTAC PARP1 degrader-1 activates the cGAS/STING immunity pathway and eventually enhances T cell killing of tumor cells. PROTAC PARP1 degrader-1 inhibits DNA damage repair, resulting in highly efficient accumulation of cytosolic DNA fragments (Blue: CRBN ligand, Black: linker; Pink: PARP1 inhibitor) .
|
-
- HY-10162
-
Olaparib
Maximum Cited Publications
193 Publications Verification
AZD2281; KU0059436
|
PARP
Autophagy
Mitophagy
|
Cancer
|
Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator .
|
-
- HY-104044
-
BGB-290
|
PARP
|
Cancer
|
Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor, with IC50 values of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively. Pamiparib has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor .
|
-
- HY-114324
-
|
PROTACs
PARP
|
Cancer
|
PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
|
-
- HY-158138
-
|
PARP
Topoisomerase
Apoptosis
|
Cancer
|
TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice was 75.4% .
|
-
- HY-100225
-
|
PARP
|
Cancer
|
ME0328 is a potent and selective ARTD3/PARP3 inhibitor with an IC50 of 0.89±0.28 μM.
|
-
- HY-Z0283S
-
Benzenecarboxamide-15N; Phenylamide-15N
|
Endogenous Metabolite
PARP
|
Others
|
Benzamide- 15N is a 15N-labeled Benzamide. Benzamide inhibits poly(ADP-ribose) polymerase (PARP)[1][2].
|
-
- HY-10614
-
|
PARP
|
Cancer
|
A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
|
-
- HY-D1107
-
|
PARP
|
Others
|
NCT-TFP is PARP probe used to identifying Poly(ADP-ribose) polymerases (PARP) inhibitors (extracted from patent US20190331688A1) .
|
-
- HY-132157
-
|
PARP
|
Others
|
8-Chloroquinazolin-4-ol (Compd 18) is a PARP-1 enzyme inhibitor, with an IC50 of 5.65 μM .
|
-
- HY-145734A
-
|
Microtubule/Tubulin
|
Cancer
|
AMXI-5001 hydrochloride is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 hydrochloride exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 hydrochloride induces complete regression of established tumors, including exceedingly large tumors .
|
-
- HY-145734
-
|
Microtubule/Tubulin
|
Cancer
|
AMXI-5001 is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 induces complete regression of established tumors, including exceedingly large tumors .
|
-
- HY-12975
-
AZ6102
1 Publications Verification
|
PARP
|
Cancer
|
AZ6102 is a potent dual TNKS1 and TNKS2 inhibitor, with IC50s of 3 nM and 1 nM, respectively, and alao has 100-fold selectivity against other PARP family enzymes, with IC50s of 2.0 μM, 0.5 μM, and >3 μM, for PARP1, PARP2, and PARP6, respectively.
|
-
- HY-34386
-
|
PARP
|
Inflammation/Immunology
Cancer
|
6(5H)-Phenanthridinone is a potent PARP-1 inhibitor and immunomodulator. 6(5H)-Phenanthridinone inhibits cell proliferation and can be used in cancer research .
|
-
- HY-16106S
-
BMN-673-13C,d4; LT-673-13C,d4
|
Isotope-Labeled Compounds
|
Others
|
Talazoparib- 13C,d4 is 13C and deuterated labeled Talazoparib (HY-16106). Talazoparib is an orally active PARP 1/2 inhibitor with Ki values of 1.2 nM and 0.87 nM for inhibiting PARP1 and PARP2 enzymatic activities, respectively. Has anti-tumor activity.
|
-
- HY-133124
-
|
PARP
PI3K
Apoptosis
|
Cancer
|
PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases .
|
-
- HY-10162S1
-
AZD2281-d8; KU0059436-d8
|
PARP
Autophagy
Mitophagy
|
Cancer
|
Olaparib-d8 is the deuterium labeled Olaparib (AZD2281). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
|
-
- HY-10130
-
ABT-888 dihydrochloride
|
PARP
Autophagy
|
Cancer
|
Veliparib (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Kis of 5.2 nM and 2.9 nM in cell-free assays, respectively.
|
-
- HY-12032
-
AG14361
3 Publications Verification
|
PARP
|
Cancer
|
AG14361 is a potent PARP-1 inhibitor, with a Ki of < 5 nM, and in permeabilized SW620 and intact SW620 cells, the IC50s are 29 nM and 14 nM, respectively.
|
-
- HY-128599
-
|
PARP
|
Cancer
|
NMS-P515 is a potent, orally active and stereospecific PARP-1 inhibitor, with a Kd of 16 nM and an IC50 of 27 nM (in Hela cells). Anti-tumor activity .
|
-
- HY-13990
-
TNKS656
|
PARP
Apoptosis
|
Cancer
|
NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC50 of 6 nM, and is > 300 fold selectivity against PARP1 and PARP2.
|
-
- HY-114869
-
|
PARP
|
Neurological Disease
|
DPQ is a potent PARP-1 inhibitor. DPQ can reduce the N-methyl-d-aspartate (NMDA)-induced PARP activation, restoring ATP to near control levels and significantly attenuating neuronal injury in the severe NMDA exposure model. DPQ can be used for researching neuroprotection .
|
-
- HY-155965
-
|
VEGFR
PARP
Apoptosis
|
Cancer
|
VEGFR/PARP-IN-1 (Compound 14b) is a VEGFR/PARP dual inhibitor (IC50s: 191 nM and 60.9 nM respectively). VEGFR/PARP-IN-1 inhibits DNA damage repair, induces cell apoptosis, and arrests cell in the G2/M phase. VEGFR/PARP-IN-1 has good antiproliferative efficacy against BRCA wild-type breast cancer cells (IC50: 4.1 and 3.5 μM for MDA-MB-231 and MCF-7 cells). VEGFR/PARP-IN-1 is an antitumor and anti-metastasis agent .
|
-
- HY-104044R
-
|
PARP
|
Cancer
|
Pamiparib (Standard) is the analytical standard of Pamiparib. This product is intended for research and analytical applications. Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor, with IC50 values of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively. Pamiparib has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor .
|
-
- HY-10162S3
-
AZD2281-d4-1; KU0059436-d4-1
|
Isotope-Labeled Compounds
PARP
Autophagy
Mitophagy
|
Cancer
|
Olaparib-d4-1 is the deuterium labeled Olaparib. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
|
-
- HY-137450
-
IMP4297; JS109
|
PARP
|
Cancer
|
Senaparib (IMP4297) is a highly potent, selective and orally active PARP1/2 inhibitor. Senaparib (IMP4297) exhibits strong antitumor activity in animal models .
|
-
- HY-161302
-
|
Apoptosis
DNA/RNA Synthesis
PARP
|
Cancer
|
Polθ/PARP-IN-1 (compound 25d) is a potent dual DNA polymerase theta (Polθ) and PARP inhibitor with IC50 values of 45.6, 5.4 nM, respectively. Polθ/PARP-IN-1 shows antiproliferative activity. Polθ/PARP-IN-1 induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage. Polθ/PARP-IN-1 shows anti-tumor activity .
|
-
- HY-10162R
-
|
PARP
Autophagy
Mitophagy
|
Cancer
|
Olaparib (Standard) is the analytical standard of Olaparib. This product is intended for research and analytical applications. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator .
|
-
- HY-12022
-
PARP-IN-1
|
PARP
|
Cancer
|
3-Aminobenzamide (PARP-IN-1) is a potent inhibitor of PARP with IC50 of appr 50 nM in CHO cells, and acts as a mediator of oxidant-induced myocyte dysfunction during reperfusion.
|
-
- HY-113432
-
2PY
|
Endogenous Metabolite
PARP
|
Metabolic Disease
|
Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .
|
-
- HY-132885
-
|
PARP
Histone Methyltransferase
|
Cancer
|
PARP/EZH2-IN-1 is a first-in-class dual PARP (IC50 6.87 nM) and EZH2 (IC50 36.51 nM) inhibitor for triple-negative breast cancer with wild-type BRCA.
|
-
- HY-W294889
-
|
PARP
|
Cancer
|
OUL245 is a 7-Hydroxy derivative, and a selectively PARP2 inhibitor (IC50=44 nM). OUL245 also inhibits other PARP and TNKS enzymes with IC50s of 2.9-8.8 μM .
|
-
- HY-156623
-
|
PARP
|
Cancer
|
Lerzeparib is an (ADP-ribose) polymerase (PARP) inhibitor, with antineoplastic activity .
|
-
- HY-161288
-
|
PARP
|
Cancer
|
UKTT15 (compound 6) is an allosteric inhibitor of PARP1 .
|
-
- HY-155458
-
|
PARP
|
Inflammation/Immunology
Cancer
|
HYDAMTIQ is a PARP-1/2 inhibitor (IC50: 29-38 nM) with anticancer, anti-inflammatory, and ischemic protective effects. HYDAMTIQ inhibits pulmonary PARP activity, is effective against allergen-induced cough and dyspnea, and inhibits bronchial hyperresponsiveness to methacholine. HYDAMTIQ has broad-spectrum tumor suppressor effects, including ovarian and breast cancers, prostate and pancreatic tumors, and glioblastoma multiforme. HYDAMTIQ has demonstrated in vivo efficacy in animal models of cerebral ischemia, asthma, cancer, and more .
|
-
- HY-100828
-
-
- HY-147245
-
STP1002
|
PARP
|
Cancer
|
Basroparib is a potent poly (ADP-ribose) polymerase (PARP) inhibitor, with antineoplastic activity .
|
-
- HY-137849
-
|
PARP
|
Cancer
|
RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model .
|
-
- HY-115552
-
|
PARP
|
Cancer
|
Simmiparib is a highly potent and orally active PARP1 and PARP2 inhibitor with IC50 values of 1.75 nM and 0.22 nM, respectively. Simmiparib has more potent PARP1/2 inhibition than its parent Olaparib (HY-10162). Simmiparib induces DNA double-strand breaks (DSB) accumulation and G2/M arrest in homologous recombination repair (HR)-deficient cells, thereby inducing apoptosis. Simmiparib exhibits remarkable anticancer activities in cells and nude mice bearing xenografts .
|
-
- HY-162104
-
|
Others
|
Cancer
|
BRCA2-RAD51-IN-1 (Compound 46) is a BRCA2-RAD51 inhibitor with an EC50 value of 28 μM. BRCA2-RAD51-IN-1 has antitumor activity .
|
-
- HY-10162S
-
AZD2281-d5; KU0059436-d5
|
PARP
Autophagy
Mitophagy
|
Cancer
|
Olaparib-d5 is a deuterium labeled Olaparib. Olaparib is a potent and oral PARP inhibitor[1].
|
-
- HY-122661
-
MPH
|
PARP
Apoptosis
|
Cancer
|
Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo .
|
-
- HY-10619D
-
MK 4827 (R-enantiomer)
|
PARP
|
Cancer
|
Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent PARP1 inhibitor with IC50 of 2.4 nM.
|
-
- HY-10619B
-
MK-4827 tosylate
|
PARP
Apoptosis
|
Cancer
|
Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-149348
-
|
Topoisomerase
PARP
Apoptosis
|
Cancer
|
DiPT-4 is a dual TOP1/PARP1 inhibitor that induces massive DNA double-strand breaks (DSBs), cell cycle arrest, and apoptosis in cancer cells. DiPT-4 has the potential to overcome cancer drug resistance .
|
-
- HY-12015
-
BSI-201; NSC-746045; IND-71677
|
PARP
Influenza Virus
|
Cancer
|
Iniparib (BSI-201) is an irreversible inhibitor of PARP1, used in the research of triple negative breast cancer.
|
-
- HY-15276
-
|
PARP
|
Cancer
|
4-Aminonaphthalimide is a potent PARP inhibitor and potentiates the cytotoxicity of γ-radiation in cancer cells .
|
-
- HY-10619
-
MK-4827
|
PARP
Apoptosis
|
Cancer
|
Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-10619A
-
MK-4827 hydrochloride
|
PARP
Apoptosis
|
Cancer
|
Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-10619E
-
MK-4827 tosylate hydrate
|
PARP
Apoptosis
|
Cancer
|
Niraparib (MK-4827) tosylate hydrate is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib tosylate hydrate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-108631
-
|
PARP
|
Inflammation/Immunology
|
EB-47 dihydrochloride, a potent and selective PARP-1/ARTD-1 inhibitor with an IC50 value of 45 nM, shows modest potency against ARTD5 with an IC50 value of 410 nM. EB-47 mimics the substrate NAD + and extends from the nicotinamide to the adenosine subsite .
|
-
- HY-15046
-
|
PARP
|
Cardiovascular Disease
Inflammation/Immunology
|
EB-47, a potent and selective PARP-1/ARTD-1 inhibitor with an IC50 value of 45 nM, shows modest potency against ARTD5 with an IC50 value of 410 nM. EB-47 mimics the substrate NAD + and extends from the nicotinamide to the adenosine subsite .
|
-
- HY-113432S
-
|
Endogenous Metabolite
PARP
|
Metabolic Disease
|
Nudifloramide-d3 (2PY-d3) is the deuterium labeled Nudifloramide. Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro[1].
|
-
- HY-155993
-
|
PARP
|
Cancer
|
YCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats .
|
-
- HY-G0023
-
Niraparib carboxylic acid metabolite M1; M1 metabolite of niraparib
|
Drug Metabolite
|
Others
|
Niraparib metabolite M1 is a metabolite of niraparib, and the latter one acts as a novel poly(ADP-Ribose) polymerase (PARP) inhibitor.
|
-
- HY-121719
-
|
PARP
|
Cardiovascular Disease
Cancer
|
TIQ-A is a potent TNKS (poly-ART, PARP) inhibitor, with an IC50 of 24 nM for TNKS2. TIQ-A is a potential anti-ischemic agent .
|
-
- HY-137457A
-
IDX-1197 hydrochloride
|
PARP
|
Cancer
|
Venadaparib (IDX-1197) hydrochloride is a potent and selective PARP inhibitor with anticancer activities. Venadaparib hydrochloride can be used for solid tumors research .
|
-
- HY-136489A
-
|
PARP
|
Cancer
|
KU-0058948 hydrochloride is a specific and potent PARP1 inhibitor with an IC50 of 3.4 nM. KU-0058948 hydrochloride shows anticancer effects .
|
-
- HY-108708
-
|
PARP
|
Cancer
|
GeA-69 is a selective, allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2 (MD2), with a Kd value of 2.1 µM. GeA-69 involves in DNA damage repair mechanisms and prevents recruitment of PARP14 MD2 to sites of laser-induced DNA damage .
|
-
- HY-136174
-
|
PARP
|
Cancer
|
RBN-2397 is a potent, accross species and orally active NAD + competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores IFN signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors .
|
-
- HY-W006566
-
5-Aminoisoquinolin-1-one
|
PARP
|
Cancer
|
5-AIQ (5-Aminoisoquinolin-1-one) is a water-soluble PARP-1 inhibitor. 5-AIQ is an important functional group in various drugs. 5-AIQ reduces the tissue injury associated with ischemia-reperfusion of the liver, it can be used for the research of the research conditions associated with ischemia-reperfusion of the liver .
|
-
- HY-150221
-
|
PARP
|
Cancer
|
DB008 is potent and selective PARP16 inhibitor with an IC50 value of 0.27 μM, containing an acrylamide electrophilic reagent. DB008 is membrane-permeable and marks PARP16 selectively . DB008 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-W748509
-
|
Caspase
Apoptosis
|
Cancer
|
Pipernonaline is a piperine derivative with antiprostate cancer activity. Pipernonaline inhibits the proliferation of androgen-dependent/independent LNCaP/PC-3 prostate cells. Pipernonaline activates caspase-3 and promotes procaspase-3/PARP cleavage. Pipernonaline also mediates reactive oxygen species (ROS) production, increased intracellular Ca(2+), and mitochondrial membrane depolarization .
|
-
- HY-10619R
-
|
PARP
Apoptosis
|
Cancer
|
Niraparib (Standard) is the analytical standard of Niraparib. This product is intended for research and analytical applications. Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-145584
-
JPI-547/OCN-201
|
PARP
|
Cardiovascular Disease
Neurological Disease
|
Nesuparib is a potent inhibitor of PARP. Nesuparib is useful for the research of neuropathic pain, neurodegenerative disease, and cardiovascular disease (extracted from patent WO2016200101A2) .
|
-
- HY-144874
-
|
PARP
|
Neurological Disease
Cancer
|
AZ3391 is a potent inhibitor of PARP. AZ3391 is a quinoxaline derivative. PARP family of enzymes play an important role in a number of cellular processes, such as replication, recombination, chromatin remodeling, and DNA damage repair. AZ3391 has the potential for the research of diseases and conditions occurring in tissues in the central nervous system, such as the brain and spinal cord (extracted from patent WO2021260092A1, compound 23) .
|
-
- HY-163527
-
|
FGFR
|
Cancer
|
FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC50=0.20±0.02 nM) and FGFR4(IC50=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity .
|
-
- HY-155038
-
|
PARP
CDK
|
Cancer
|
Antitumor agent-104 (Compound 9) is an antitumor agent by inhibiting DNA damage repair in tumors. Antitumor agent-104 inhibits PARP1 enzymatic activity and the PAR protein level. Antitumor agent-104 also inhibits the expression of CDK12 .
|
-
- HY-W015422
-
|
PARP
|
Metabolic Disease
|
1,5-Isoquinolinediol is a potent PARP inhibitor, with an IC50 of 0.18-0.37 µM. 1,5-Isoquinolinediol attenuates diabetes-induced NADPH oxidase-derived oxidative stress in retina .
|
-
- HY-15044
-
|
PARP
|
Neurological Disease
Cancer
|
NU1025 is a potent PARP inhibitor with an IC50 of 400 nM and a Ki of 48 nM. NU1025 potentiates the cytotoxicity of ionizing radiation and anticancer agents. NU1025 has anti-cancer and neuroprotective activity .
|
-
- HY-122935
-
|
HIV
Reverse Transcriptase
|
Infection
|
Nigranoic acid is a triterpenoid separated from Schisandra chinensis. Nigranoic acid inhibits HIV-1 reverse transcriptase. Nigranoic acid exhibits protective effects on brain through PARP/AIF signaling pathway in cerebral ischemia-reperfusion animal model .
|
-
- HY-163461
-
|
PARP
|
Cancer
|
4F-DDC is a novel PARP1 inhibitor with an IC50 value of 82 nM. 4F-DDC induces DNA damage and activates the cGAS–STING pathway. 4F-DDC inhibits the growth of HCC-1937-derived tumor xenografts .
|
-
- HY-139156
-
|
PARP
PROTACs
|
Cancer
|
SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1, with an IC50 of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations .
|
-
- HY-16106A
-
(8R,9S)-BMN-673; (8R,9S)-LT-673
|
PARP
|
Cancer
|
(8R,9S)-Talazoparib ((8R,9S)-BMN-673) is an enantiomer of Talazoparib. (8R,9S)-Talazoparib is an PARP1 inhibitor, with an IC50 of 144 nM .
|
-
- HY-162472
-
|
ATM/ATR
DNA-PK
|
Cancer
|
XRD-0394 is a potent and specific dual inhibitor of ATM and DNA-PKcs with oral activity. XRD-0394 significantly enhances tumor cell killing in vitro and in vivo under therapeutic ionizing radiation conditions. In addition, XRD-0394 can potentiate the effects of PARP and topoisomerase I inhibitors in vitro .
|
-
- HY-161430
-
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
RTx-161 is an allosteric Polθ polymerase inhibitor with an IC50 value of 4.1 nM. RTx-161 selectively kills HR-deficient cancer cells and suppresses PARP inhibitor (PARPi) resistance in multiple genetic backgrounds, including HR-proficient cells. Additionally, RTx-161 can induce apoptosis .
|
-
- HY-146096
-
|
P-glycoprotein
Apoptosis
|
Cancer
|
RMS3, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS3 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS3 has strong anticancer property .
|
-
- HY-121497
-
3-MBA
|
PARP
Bacterial
|
Cancer
|
3-Methoxybenzamide (3-MBA), an inhibitor of ADP-ribosyltransferase (ADPRTs) and PARP, inhibits cell division in Bacillus subtilis, leading to filamentation and eventually lysis of cells . 3-Methoxybenzamide (3-MBA) enhances in vitro plant growth, microtuberization, and transformation efficiency of blue potato (Solanum tuberosum L. subsp. andigenum) .
|
-
- HY-156520
-
|
Apoptosis
|
Inflammation/Immunology
|
Immunosuppressant-1 (Compound 31) inhibits anti-CD3/anti-CD28 co-stimulated T-cell proliferation. Immunosuppressant-1 has immunosuppressive activity, and induces apoptosis by activating caspase-3 and PARP in activated lymph node cells .
|
-
- HY-136979
-
|
PARP
|
Inflammation/Immunology
Cancer
|
RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of <3 nM. RBN012759 displays 300-fold selectivity over the monoPARPs and 1000-fold selectivity over the polyPARPs. RBN012759 decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants .
|
-
- HY-15045
-
|
PARP
|
Cancer
|
INO-1001 is a potent and selective poly (ADP-ribose) polymerase (PARP) inhibitor. INO-1001 is a potent enhancer of radiation sensitivity and enhances radiation-induced cell killing by interfering with DNA repair mechanisms, resulting in necrotic cell death . INO-1001 has anti-tumor effects .
|
-
- HY-13968
-
JW 55
2 Publications Verification
|
PARP
|
Cancer
|
JW 55 is a potent and selective β-catenin signaling pathway inhibitor, which functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). JW 55 decreases auto-PARsylation of TNKS1/2 in vitro with IC50s of 1.9 μM and 830 nM respectively.
|
-
- HY-126248
-
|
PARP
|
Cancer
|
Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model .
|
-
- HY-152696
-
|
Nucleoside Antimetabolite/Analog
|
Others
|
6-O-Methylinosine is a hypoxanthine analogue. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
|
-
- HY-130250
-
|
CDK
Apoptosis
|
Cancer
|
SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death .
|
-
- HY-107545
-
|
Dynamin
|
Cancer
|
Dynole 34-2 is a dynamin GTPase inhibitor (IC50s=6.9 and 14.2 µM for dynamin1 and dynamin2 GTPase activity, respectively) with antimitotic effect. Dynole 34-2 induces apoptosis, as revealed by cell blebbing, DNA fragmentation, and PARP cleavage . Dynole 34-2 also potently inhibits receptor mediated endocytosis (RME) .
|
-
- HY-Z0283
-
Benzenecarboxamide; Phenylamide
|
Endogenous Metabolite
PARP
|
Others
|
Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
|
-
- HY-13326
-
ASP3026
5 Publications Verification
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
ROS Kinase
Caspase
PARP
IGF-1R
STAT
Akt
JNK
|
Cancer
|
ASP3026 is a selective and orally active inhibitor of anaplastic lymphoma kinase (ALK). ASP3026 is a selective and oral active anaplastic lymphoma kinase (ALK) inhibitor with a IC50 value of 3.5 nM. ASP3026 can inhibit the phosphorylation of IGF-1R, STAT3, AKT and JNK proteins, and induce the cleavage of caspase 3 and PARP. It also inhibited ROS and ACK. ASP3026 can be used in anti-tumor research .
|
-
- HY-W039271
-
2-Chloro-6-O-methyl-inosine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
2-Chloro-6-methoxypurine riboside is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
|
-
- HY-154017
-
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
2′-C-Methyl-6-O-methylinosine is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
|
-
- HY-149735
-
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
BET-IN-20 (compound 10) is an inhibitor of BRD4 BD1 (IC50=1.9 nM) with anticancer activity. BET-IN-20 can promote acute myeloid leukemia (AML) cell apoptosis and arrest the cell cycle in the G0/G1 phase. BET-IN-20 also inhibits c-Myc and CDK6 and enhances PARP cleavage .
|
-
- HY-123851
-
M2912
|
PARP
|
Cancer
|
MSC2504877 (M2912) is a potent and orally active tankyrase inhibitor with IC50s of 0.0007, 0.0008, 0.54 µM for TNKS, TNKS2, PARP1, respectively. MSC2504877 increases the expression of AXIN2 and TNKS protein levels and decreases β-catenin levels. MSC2504877 shows anti-tumor activity .
|
-
- HY-122611
-
|
Androgen Receptor
Apoptosis
|
Cancer
|
CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
|
-
- HY-122611A
-
|
Androgen Receptor
Apoptosis
|
Cancer
|
CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 hydrochloride induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the prostate cancer mouse model
|
-
- HY-155570
-
|
PI3K
Apoptosis
Caspase
PARP
|
Cancer
|
Anticancer agent 137 (8q) is a potent PI3k inhibitor. Anticancer agent 137 has broad-spectrum anticancer activity. Anticancer agent 137 induces G2/M cell cycle arrest and apoptosis. Anticancer agent 137 increases cleaved PARP, caspase 3, and 7. Anticancer agent 137 can be used in research of cancer .
|
-
- HY-154393
-
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
2-Chloro-2'-deoxy-6-O-methylinosine is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
|
-
- HY-152678
-
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
6-Methoxypurine-9-β-D-5’(R)-C-methylriboside is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
|
-
- HY-W141392
-
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
2'-Fluoro-5'-O-DMT-2'-deoxyinosine-3'-CE-phosphoramidite is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
|
-
- HY-W392836
-
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
2'-O-Methyl-5'-O-dmt-inosine-3'-CE-phosphoramidite is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
|
-
- HY-146097
-
|
P-glycoprotein
Apoptosis
|
Cancer
|
RMS5, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS5 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS5 slightly diminishes the expression of the anti-apoptotic Bcl-2 family proteins Bcl-XL and Mcl-1. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS5 has strong anticancer property .
|
-
- HY-144691
-
|
PROTACs
CDK
|
Cancer
|
PP-C8 is a potent and selective PROTAC CDK12-Cyclin K degrader. PP-C8 induces CDK12-Cyclin K degradation with DC50s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC) .
|
-
- HY-147291
-
|
c-Myc
PARP
Apoptosis
|
Cancer
|
VPC-70063 is a potent Myc-Max inhibitor with an IC50 value of 8.9 μM for Myc-Max transcriptional activity inhibition. VPC-70063 reduces UBE2C promotor activity and AR-V7 levels, and induces PARP cleavage. VPC-70063 induces apoptosis and blocks Myc-Max interactions with DNA. VPC-70063 can be used for researching anticancer .
|
-
- HY-114778
-
SHR3162; Fuzuloparib
|
PARP
|
Cancer
|
Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell‐free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)‐deficient cells, and sensitizes both HR‐deficient and HR‐proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research .
|
-
- HY-111329
-
ILS-JGB-1741
|
Sirtuin
Apoptosis
|
Cancer
|
JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC50 of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC50>100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediated apoptosis with modulation of Bax/Bcl2 ratio, cytochrome c release and PARP cleavage. JGB1741 has the potential for breast cancer research .
|
-
- HY-N1970
-
|
Keap1-Nrf2
Arenavirus
Caspase
PARP
|
Neurological Disease
|
5,7-Dihydroxychromone, the extract of Cudrania tricuspidata, activates Nrf2/ARE signal and exerts neuroprotective effects against 6-hydroxydopamine (6-OHDA)-induced oxidative stress and apoptosis. 5,7-Dihydroxychromone inhibits the expression of activated caspase-3 and caspase-9 and cleaved PARP in 6-OHDA-induced SH-SY5Y cells .
|
-
- HY-146817
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Tubulin polymerization-IN-11 is a potent tubulin polymerization inhibitor with an IC50 value of 3.4 µM. Tubulin polymerization-IN-11 shows antiproliferative activity. Tubulin polymerization-IN-11 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-11 decreases the expression of cyclin B1, p-cdc2, and Bcl-2 protein levels and increases the expression of cleaved PARP .
|
-
- HY-156094
-
|
HDAC
Histone Demethylase
Apoptosis
|
Cancer
|
JMJD3/HDAC-IN-1 (compound A5b) is a dual inhibitor targeting Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylase (HADC1, IC50=16 nM). JMJD3/HDAC-IN-1 promotes hypermethylation of histone H3K27 and hyperacetylation of H3K9, and also cleaves caspase-7 and PARP to induce apoptosis. JMJD3/HDAC-IN-1 effectively inhibits cancer cell cloning, migration, and invasion .
|
-
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-Z0283S
-
|
Benzamide- 15N is a 15N-labeled Benzamide. Benzamide inhibits poly(ADP-ribose) polymerase (PARP)[1][2].
|
-
-
- HY-16106S
-
|
Talazoparib- 13C,d4 is 13C and deuterated labeled Talazoparib (HY-16106). Talazoparib is an orally active PARP 1/2 inhibitor with Ki values of 1.2 nM and 0.87 nM for inhibiting PARP1 and PARP2 enzymatic activities, respectively. Has anti-tumor activity.
|
-
-
- HY-10162S1
-
|
Olaparib-d8 is the deuterium labeled Olaparib (AZD2281). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
|
-
-
- HY-10162S3
-
|
Olaparib-d4-1 is the deuterium labeled Olaparib. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
|
-
-
- HY-10162S
-
|
Olaparib-d5 is a deuterium labeled Olaparib. Olaparib is a potent and oral PARP inhibitor[1].
|
-
-
- HY-113432S
-
|
Nudifloramide-d3 (2PY-d3) is the deuterium labeled Nudifloramide. Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro[1].
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-150221
-
|
|
Alkynes
|
DB008 is potent and selective PARP16 inhibitor with an IC50 value of 0.27 μM, containing an acrylamide electrophilic reagent. DB008 is membrane-permeable and marks PARP16 selectively . DB008 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-145749
-
|
|
Alkynes
|
PARPYnD is a PARP enzyme photoaffinity probe (AfBP) based on the triple PARP1/2/6 inhibitor AZ9482 (HY-119653), which induces breast cancer Formation of multipolar spindles (MPS) in cells. PARPYnD inhibits PAPR wih IC50 of 38 nM (PARP1), 6 nM (PARP2), 230 nM (PARP6), respectively. PARPYnD enriches recombinant PARP6 incorporated into cell lysates and inhibits PARP6 in cell-free assays, but it does not label PARP6 in intact cells .
|
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