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AR Inhibitor

" in MedChemExpress (MCE) Product Catalog:

147

Inhibitors & Agonists

1

Screening Libraries

1

Peptides

1

Inhibitory Antibodies

17

Natural
Products

12

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10547
    OSU-03012
    4 Publications Verification

    AR-12; PDK1 Inhibitor AR-12

    PDK-1 Autophagy Cancer
    OSU-03012 (AR-12; PDK1 inhibitor AR-12) is a blood-brain permeable PDK-1 inhibitor with an IC50 of 5 μM .
    OSU-03012
  • HY-10512
    AR-A014418
    10+ Cited Publications

    AR 0133418; GSK 3β Inhibitor VIII; AR 014418

    GSK-3 Metabolic Disease Cancer
    AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM) .
    AR-A014418
  • HY-120208

    Aldose Reductase Metabolic Disease
    MK204 is an aldose reductase (AR) inhibitor that can be used in diabetes research .
    MK204
  • HY-RI01656

    MicroRNA
    hsa-miR-548ar-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
    hsa-miR-548ar-3p inhibitor
    hsa-miR-548ar-3p inhibitor
  • HY-RI01657

    MicroRNA
    hsa-miR-548ar-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
    hsa-miR-548ar-5p inhibitor
    hsa-miR-548ar-5p inhibitor
  • HY-10512S

    AR 0133418-d3; GSK 3β Inhibitor VIII-d3; AR 014418-d3

    Isotope-Labeled Compounds GSK-3 Metabolic Disease Cancer
    AR-A014418-d3 is the deuterium labeled AR-A014418. AR-A014418 is a potent, selective, and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM)[1].
    AR-A014418-d3
  • HY-105122

    WIN 49596

    Androgen Receptor Endocrinology Cancer
    Zanoterone is an orally active antagonist of the androgen receptor (AR) with a Ki of 2.2 μM. Zanoterone blocks the binding of androgens such as testosterone and dihydrotestosterone (DHT), inhibiting the androgen signaling pathway, thereby reducing androgen-dependent prostate hyperplasia and prostate cancer growth .
    Zanoterone
  • HY-12798C

    AR-13324 M1 metabolite

    Drug Metabolite Others
    AR-13503 (AR-13324 M1 metabolite) is a hydrolysis metabolite of AR-13324 mesylate. AR-13324 is a inhibitor of ROCK kinase.
    AR-13503
  • HY-19346

    ROCK Others
    AR-13324 analog mesylate is an analog of AR-13324. AR-13324 is an ROCK and norepinephrine transporter (NET) inhibitor .
    AR-13324 analog mesylate
  • HY-125639

    (rac)-AR-13324 M1 metabolite

    PKC ROCK Cardiovascular Disease
    (rac)-AR-13503 ((rac)-AR-13324 M1 metabolite) is the isoform of AR-13503 (HY-12798C). AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice .
    (rac)-AR-13503
  • HY-163510

    Androgen Receptor Cancer
    AR/AR-V7-IN-1 (Compound 20i) is an AR/ARV7 inhibitor (IC50 = 172.85 nM). AR/AR-V7-IN-1 potently inhibits cell growth with IC50 values of 4.87 and 2.07 μM in the LNCaP and 22RV1 cell lines, respectively. AR/AR-V7-IN-1 exhibits effective tumor growth inhibition in the 22RV1 xenograft study. AR/AR-V7-IN-1 can be used for the research of prostate cancer .
    AR/AR-V7-IN-1
  • HY-142923

    Androgen Receptor Cancer
    AR antagonist 2 (compound 58) is a potent androgen receptor (AR) inhibitor with an IC50 of 0.95 μM. AR antagonist 2 has the potential for cancer research .
    AR antagonist 2
  • HY-158180

    Adenosine Receptor Inflammation/Immunology
    A3AR agonist 4 is an A3 adenosine receptor (A3AR) agonist (Ki: 1.24 nM for hA3AR). A3AR agonist 4 inhibits cAMP production with an EC50 of 0.17 nM. A3AR agonist 4 can be used for research of inflammation and pain .
    A3AR agonist 4
  • HY-13265
    AR-42
    2 Publications Verification

    HDAC-42; OSU-HDAC42

    HDAC Autophagy Apoptosis Cancer
    AR-42 (HDAC-42; OSU-HDAC42) is a potent, orally bioavailable pan-HDAC inhibitor (IC50=16 nM). AR-42 induces growth inhibition, cell-cycle arrest, apoptosis, and activation of caspases-3/7. AR-42 promotes hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21. AR-42 shows cytotoxicity against various human cancer cell lines .
    AR-42
  • HY-111151

    APAU

    Epoxide Hydrolase Infection Metabolic Disease
    AR9281 (APAU) is a potent, selective and orally active soluble epoxide hydrolase (s-EH) inhibitor. AR-9281 can inhibits human sEH (HsEH) and murine sEH (MsEH) with IC50 values of 13.8 nM and 1.7 nM, respectively. AR9281 can be used for the research of inflammation, hypertension and type 2 diabetes .
    AR-9281
  • HY-N1943

    Δ13-DehydrochapARrinone

    Androgen Receptor Inflammation/Immunology Cancer
    Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of both full-length androgen receptor (AR) (IC50=69 nM) and constitutively active truncated AR splice variants (AR1-651 IC50=309 nM).
    Ailanthone
  • HY-148771

    PROTAC AR-V7 degrader-2

    PROTACs Androgen Receptor Apoptosis Cancer
    MTX-23 is an AR-based PROTAC. MTX-23 inhibits CaP cellular proliferation by degrading AR-V7 and AR-FL. MTX-23 induces apoptosis .
    MTX-23
  • HY-155543

    Androgen Receptor Cancer
    Anticancer agent 135 (compound 26h) is a potent androgen receptor (AR) antagonist. Anticancer agent 135 can effectively block AR nuclear translocation and inhibit AR/AR-V7 heterodimerization, thereby inhibiting downstream gene transcription. Anticancer agent 135 displays potent robust efficacy in prostate cancer xenograft models .
    Anticancer agent 135
  • HY-16758

    AR-12286

    ROCK Neurological Disease
    Verosudil (AR-12286) is a potent, selective Rho-kinase (ROCK) inhibitor with Kis of 2 and 2 nM for ROCK1 and ROCK2, respectively. AR-12286 lowers intraocular pressure (IOP) primarily by increasing aqueous humour outflow through the trabecular meshwork .
    Verosudil
  • HY-158101

    CC-94676

    Androgen Receptor Cancer
    BMS-986365 is a selective heterobifunctional ligand-directed degrader (LDD) targeting the androgen receptor (AR). BMS-986365 demonstrated significant in vivo potency, degrading AR, inhibiting AR signaling, and inhibiting tumor growth in animal models of advanced prostate cancer.
    BMS-986365
  • HY-160547

    Androgen Receptor Metabolic Disease
    PROTAC AR Degrader-5 (compound A46) is a potent AR PROTAC Degrader with an IC50 value of 49 nM. PROTAC AR Degrader-5 inhibits sebaceous plaque and induces hair regeneration .
    PROTAC AR Degrader-5
  • HY-120018

    Androgen Receptor Cancer
    VPC-13566, a BF3-specific small molecule, is an androgen receptor (AR) inhibitor. VPC-13566 is effective in inhibiting AR transcriptional activity in vitro as well as the growth of AR-dependent PCa cell lines. VPC-13566 can be used as a chemical probe to help identify unknown AR partners.VPC-13566 can be used for the research of cancer.
    VPC-13566
  • HY-12798A

    AR-13324 dimesylate

    ROCK Others
    Netarsudil mesylate (AR-13324 mesylate) is a small-molecule inhibitor of Rho kinase and a norepinephrine transporter; reduces intraocular pressure (IOP) in normotensive monkey eyes.
    Netarsudil dimesylate
  • HY-15314
    Ranirestat
    1 Publications Verification

    AS-3201

    Aldose Reductase Neurological Disease Metabolic Disease
    Ranirestat (AS-3201) potent and orally active aldose reductase (AR) inhibitor with IC50s of 11 nM and 15 nM for rat lens AR and recombinant human AR, respectively, and a Ki of 0.38 nM for recombinant human AR. Ranirestat has the potential for diabetic sensorimotor polyneuropathy treatment. Ranirestat also has a neuroprotective effect on diabetic retinas .
    Ranirestat
  • HY-117669

    Androgen Receptor Cancer
    VPC-14228 is a potent androgen receptor DNA binding domain (AR-DBD) inhibitor that interferes with the interaction of AR with androgen response elements and effectively blocks AR transcriptional activity. VPC-14228 can be used in prostate cancer research .
    VPC-14228
  • HY-116501

    Androgen Receptor Cancer
    VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC50 of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer .
    VPC-14449
  • HY-12122

    NO Synthase Neurological Disease
    AR-C102222 is a spirocyclic fluoropiperidine quinazoline selective iNOS inhibitor. AR-C102222 can be used for the research of neuropathic pain .
    AR-C102222
  • HY-156111

    PROTACs Androgen Receptor Cancer
    ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models .
    ARD-1676
  • HY-110126
    AR-C118925XX
    1 Publications Verification

    P2Y Receptor Inflammation/Immunology Cancer
    AR-C118925XX is a selective P2Y2 receptor antagonist. AR-C118925XX inhibits ATP-induced IL-6 production and phosphorylation of p38. AR-C118925XX also inhibits Bleomycin (HY-108345)-induced dermal fibrosis in mice. AR-C118925XX also inhibits ATP-induced tumor growth .
    AR-C118925XX
  • HY-145709

    Androgen Receptor Cancer
    Ar-V7-IN-1 is a potent inhibitor of Ar-V7. AR-V7 is a hormone-independent splice variant of the androgen receptor. Ar-V7-IN-1 has the potential for the research of various indications, in particular cancers such as prostate cancer (extracted from patent WO2018114781A1, compound 43) .
    Ar-V7-IN-1
  • HY-119993

    BMH-23

    DNA/RNA Synthesis Cancer
    AR03 (BMH-23) is an apurinic/apyrimidinic endonuclease 1 (Ape1) inhibitor with an IC50 of 2.1 µM. AR03 has low affinity for double-stranded DNA. AR03 potentiates the cytotoxicity of methyl methanesulfonate and temozolomide in SF767 cells .
    AR03
  • HY-151596

    Monoamine Oxidase 5-HT Receptor Neurological Disease
    MAO-A/5-HT2AR-IN-1 (compound I14) is a potent MAO-A and 5-HT2AR dual inhibitor, with IC50 values of 0.004 and 0.014 μM, respectively. MAO-A/5-HT2AR-IN-1 is a potential antidepressant agent .
    MAO-A/5-HT2AR-IN-1
  • HY-N4089

    Aldose Reductase Metabolic Disease
    Quercetin 3-gentiobioside is isolated from A. iwayomogi, AR and AGE formation inhibitor, demonstrates biological activities against Aldose reductase (AR) and the formation of advanced glycation endproducts (AGEs) .
    Quercetin 3-gentiobioside
  • HY-12798B

    AR-13324 hydrochloride

    ROCK Neurological Disease
    Netarsudil hydrochloride (AR-13324 hydrochloride) is a Rho-associated protein kinas (ROCK) and norepinephrine transporter (NET) inhibitor. Netarsudil hydrochloride has effective in intraocular pressure (IOP) reduction .
    Netarsudil hydrochloride
  • HY-147907

    Adenosine Receptor Neurological Disease Inflammation/Immunology Cancer
    Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with Ki values of >1000, 68.5, >1000, >1000 nM for A1AR, A2AAR, A2BAR, A3AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases .
    Adenosine receptor <em>inhibitor</em> 1
  • HY-163363

    Adrenergic Receptor Cancer
    β-AR antagonist 2 (compound 43) is an antagonist of β-AR (IC50: 0.17 μM). β-AR-IN-1 inhibits the growth of mouse A549 xenograft tumors and shows cardioprotective efficacy against DOX-induced HF in C57 mice .
    β-AR antagonist 2
  • HY-16079
    AZD3514
    2 Publications Verification

    Androgen Receptor Cancer
    AZD3514 is an orally activie and selective androgen receptor (AR) inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostate cancer cells in the absence of androgen with an pIC50 value of 5.75. AZD3514 can be used for the research of prostate cancer .
    AZD3514
  • HY-123875A

    EPI-506

    Androgen Receptor Cancer
    Ralaniten triacetate (EPI-506), the pro-agent of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7 .
    Ralaniten triacetate
  • HY-132292

    PROTACs Androgen Receptor Cancer
    ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer .
    ARD-2128
  • HY-150025

    DNA Methyltransferase Apoptosis Cancer
    (4aS,8aR)-NPD-001 is a potent and allosteric inhibitor of DNMT3A. (4aS,8aR)-NPD-001 inhibits DNMT3A activity by disrupting protein-protein interactions. (4aS,8aR)-NPD-001 induces apoptosis of acute myeloid leukemia (AML) cell lines. (4aS,8aR)-NPD-001 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882 .
    (4aS,8aR)-NPD-001
  • HY-161409

    Androgen Receptor Apoptosis Cancer
    SC912 is an AR-V7 inhibitor (IC50 = 0.36 μM). SC912 possesses safety, potency and selectivity. SC912 binds directly to AR-FL and AR-V7 proteins, inhibites nuclear localization and chromatin binding capabilities. SC912 exerts anticancer activity through inhibition of proliferation, induction of cell cycle arrest and apoptosis .
    SC912
  • HY-147706

    Others Cancer
    Ar524 has higher inhibitory activity than the known transgenic inhibitor kifunensine. At the same time, ar524 inhibited low concentration (10 μ M) Spheroid formation of human malignant cells.
    AR524
  • HY-163379

    Complement System Inflammation/Immunology
    C5aR1 antagonist 2 (Compound 6a) is an orally active C5a receptor 1 (C5aR1) antagonist that shows efficacy in inhibiting the C5a-induced neutrophil count increase. C5aR1 antagonist 2 is potent in the DISCO and migration assays, with IC50 values of 21 and 3 nM, respectively. C5aR1 antagonist 2 can be used for the research of acute and chronic inflammatory diseases .
    C5aR1 antagonist 2
  • HY-101479S

    Isotope-Labeled Compounds Bacterial Antibiotic Infection
    Iclaprim-d6 (AR-100-d6) is the deuterium labeled Iclaprim. Iclaprim is a new selective bacterial Dihydrofolate inhibitor, which can inhibit the growth of S. aureus (MRSA) with an MIC90 of 0.06 μg/mL.
    Iclaprim-d6
  • HY-100348

    Androgen Receptor PPAR Apoptosis Cancer
    EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer .
    EPI-001
  • HY-147585

    Complement System Inflammation/Immunology
    C5aR-IN-1 is a potent inhibitor of C5aR. Increased level of C5a has been associated with disorders such as autoimmune disorders and inflammatory disorders. C5aR-IN-1 has the potential for the research of inflammation diseases (extracted from patent WO2022028586A1, compound 47) .
    C5aR-IN-1
  • HY-147586

    Complement System Inflammation/Immunology
    C5aR-IN-2 is a potent inhibitor of C5aR. Increased level of C5a has been associated with disorders such as autoimmune disorders and inflammatory disorders. C5aR-IN-2 has the potential for the research of inflammation diseases (extracted from patent WO2022028586A1, compound 49) .
    C5aR-IN-2
  • HY-147587

    Complement System Inflammation/Immunology
    C5aR-IN-3 is a potent inhibitor of C5aR. Increased level of C5a has been associated with disorders such as autoimmune disorders and inflammatory disorders. C5aR-IN-3 has the potential for the research of inflammation diseases (extracted from patent WO2022028586A1, compound 89) .
    C5aR-IN-3
  • HY-147100

    PROTACs Adrenergic Receptor Cancer
    α1A-AR Degrader 9c (compound 9c) is a potent, selective and reversible α1A-AR (Adrenergic receptor) PROTAC degrader, with a DC50 of 2.86 μM. α1A-AR Degrader 9c induces α1A-AR degradation can be attributed to proteasomal degradation. α1A-AR Degrader 9c inhibits the proliferation of PC-3 cells, with an IC50 of 6.12 μM. α1A-AR Degrader 9c shows antitumor activity, and can be used for prostate cancer research .
    α1A-AR Degrader 9c
  • HY-12122A

    NO Synthase Neurological Disease Inflammation/Immunology
    AR-C102222 hydrochloride is a potent, competitive, orally active and highly selective inducible nitric oxide synthase (iNOS) inhibitor, with an IC50 of 37 nM . AR-C102222 hydrochloride has antinociception and anti-inflammatory activities .
    AR-C102222 hydrochloride

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