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Pathways Recommended:	JAK/STAT Signaling

Results for "

STAT phosphorylation inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Oxidative Phosphorylation (1) STAT (39) Akt (1) Amyloid-β (1) Anaplastic lymphoma kinase (ALK) (1) Antibiotic (1) Apoptosis (27) Bcl-2 Family (1) Bcr-Abl (1) c-Kit (2) c-Met/HGFR (5) Caspase (2) CDK (2) Early 2 Factor (E2F) (1) Endogenous Metabolite (1) Ferroptosis (2) FLT3 (4) GHSR (1) HDAC (1) IGF-1R (1) IKK (1) Insulin Receptor (2) Interleukin Related (4) JAK (18) JNK (1) NF-κB (1) PARP (1) PDGFR (1) Phosphatase (1) PROTACs (2) Reactive Oxygen Species (1) ROS Kinase (1)
By Research Areas:	Cancer (59) Cardiovascular Disease (2) Endocrinology (2) Infection (2) Inflammation/Immunology (18) Metabolic Disease (1) Neurological Disease (1)
Click Chemistry:	Alkynes (1)

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Click Chemistry

Targets Recommended: STAT Oxidative Phosphorylation DYRK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-149007

STAT3-IN-11 1 Publications Verification	STAT Apoptosis	Cancer
STAT3-IN-11 (7a) is a selective *STAT3* inhibitor that inhibits the phosphorylation of STAT3 at site pTyr705. STAT3-IN-11 inhibits the phosphorylation of downstream genes (Survivin and Mcl-1) without affecting its upstream tyrosine kinases (Src and JAK2) levels and p-STAT1 expression. STAT3-IN-11 can induce cancer cell apoptosis, which is potential for the discovery of effective STAT3 inhibitors and antitumor agents against cancers .

HY-136658

1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea 1 Publications Verification	STAT Apoptosis	Cancer
STAT3-IN-7 is a Sorafenib analogue and potently inhibits the phosphorylation of *STAT3. STAT3-IN-7 induces cell apoptosis through SHP-1 dependent STAT3 inactivation. STAT3-IN-7 does not inhibit* kinase activity and has anticancer effects .

HY-120376

XZH-5

STAT Cancer

XZH-5 inhibits the phosphorylation of STAT3 and results in the induction of apoptosis and reduction of colony forming ability .

XZH-5	STAT	Cancer
XZH-5 inhibits the phosphorylation of STAT3 and results in the induction of apoptosis and reduction of colony forming ability .

HY-N10472

STAT3-IN-14	STAT	Cancer
STAT3-IN-14 (Compound 1) is a STAT3 inhibitor and has STAT3 phosphorylation inhibitory activity. STAT3-IN-14 (Compound 1) can directly bind to the hinge region of STAT3 .

HY-P10114

STAT3-IN-24, cell-permeable PpYLKTK-mts; STAT3 PI	STAT	Cancer
STAT3-IN-24, cell-permeable (PpYLKTK-mts) is a *STAT3* peptide inhibitor. STAT3-IN-24, cell-permeable inhibits recruitment of STAT3 to Jak2 and phosphorylation of Y705, thus preventing the dimerization and the nuclear translocation of STAT3 .

HY-112447

STAT3-IN-5	STAT	Cancer
STAT3-IN-5 is a potent *STAT3* inhibitor. STAT3-IN-5 inhibits STAT3-Y705 phosphorylation with an EC₅₀ value of 170 nM. STAT3-IN-5 inhibits cytokine induced JAK activation. STAT3-IN-5 induces apoptosis. STAT3-IN-5 can be used in research of cancer .

HY-146666

STAT3-IN-9	Apoptosis STAT	Cancer
STAT3-IN-9 is a potent *STAT3* inhibitor. STAT3-IN-9 inhibits the activation of STAT3 (Tyr705) without influencing the phosphorylation of STAT1 (Tyr701). STAT3-IN-9 induces apoptosis and cell cycle arrest at the G2/M phase .

HY-112391

SD-1029	JAK STAT	Cancer
SD-1029 is a *JAK2/STAT3* inhibitor . SD-1029 inhibits STAT3 nuclear translocation. SD-1029 is an inhibitor of STAT3 activation due to inhibition of JAK2 phosphorylation .

HY-151976

STAT3-IN-15 1 Publications Verification	STAT	Inflammation/Immunology
STAT3-IN-15 is a potent and orally active STAT3 inhibitor against idiopathic pulmonary fibrosis (IPF). STAT3-IN-15 inhibits STAT3 phosphorylation. STAT3-IN-15 also inhibits the migration and deformation of epithelial cells induced by TGF-β1 and inhibit epithelial-mesenchymal transition (EMT) .

HY-100614

AS1517499

20+ Cited Publications

STAT Inflammation/Immunology Cancer

AS1517499 is a potent and brain-permeable STAT6 phosphorylation inhibitor with an IC₅₀ of 21 nM.

AS1517499 20+ Cited Publications	STAT	Inflammation/Immunology Cancer
AS1517499 is a potent and brain-permeable *STAT6* phosphorylation inhibitor with an IC₅₀ of 21 nM.

HY-N7674

Angoline 2 Publications Verification	STAT	Cancer
Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC₅₀ of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation .

HY-N7674A

Angoline hydrochloride	STAT	Cancer
Angoline hydrochloride is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC₅₀ of 11.56 μM. Angoline hydrochloride inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation .

HY-13818

Stattic Maximum Cited Publications 148 Publications Verification	STAT Apoptosis	Inflammation/Immunology Cancer
Stattic is a potent *STAT3* inhibitor and inhibits STAT3 phosphorylation (at Y705 and S727) . Stattic inhibits the binding of a high affinity phosphopeptide for the SH2 domain of STAT3 . Stattic ameliorates the renal dysfunction in Alport syndrome (AS) mice .

HY-157847

phospho-STAT3-IN-2	STAT	Cancer
Phospho-STAT3-IN-2 (compound 4D) is a STAT3 inhibitor that effectively inhibits STAT3 phosphorylation. phospho-STAT3-IN-2 can significantly reduce tumor volume in mouse xenograft tumor models without drug toxicity to other organs and tissues .

HY-P2282

APTSTAT3-9R 1 Publications Verification	STAT	Cancer
APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking *STAT3* phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity .

HY-150603

STAT3-IN-13	STAT Apoptosis Bcl-2 Family	Cancer
STAT3-IN-13 (compound 6f) is a potent *STAT3* inhibitor. STAT3-IN-13 has anti-proliferative effects and binds to the STAT3 SH2 domain with a K_D of 0.46 μM. STAT3-IN-13 inhibits the phosphorylation of STAT3 Y705 and downstream target gene expression. STAT3-IN-13 induces apoptosis in vitro and suppresses the growth and metastasis of tumor in vivo. STAT3-IN-13 can be used for cancer research .

HY-100544

FLLL32 5 Publications Verification	STAT JAK Apoptosis	Cancer
FLLL32, a synthetic analog of curcumina, is a *JAK2/STAT3* dual inhibitor with anti-tumor activity. FLLL32 can inhibit the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells .

HY-160496

STAT3-IN-25	STAT	Cancer
STAT3-IN-25 (compound 4c) is an orally active, potent **STAT3 dual phosphorylation** inhibitor with an indole-containing tetra-aromatic heterocycle scaffold. STAT3-IN-25 has luciferase activities IC₅₀ of 5.3 nM and ATP inhibition IC₅₀ of 4.2 nM.STAT3-IN-25 significantly blocks p-Tyr705 and p-Ser727 and causes the abrogation of the corresponding nuclear transcription and mitochondrial oxidative phosphorylation functions of STAT3 in the low nanomolar range by targeting the STAT3 SH2 domain (K_D=21.3 nM). STAT3-IN-25 STAT3-IN-25 exhibits significant suppressive effects in a pancreatic cancer xenograft model .

HY-155982

STAT3-IN-20	STAT	Cancer
STAT3-IN-20 (Compound 40) is a selective *STAT3* inhibitor (IC₅₀: 0.65 μM). STAT3-IN-20 binds the SH2 domain to inhibit STAT3 phosphorylation, translocation, and downstream gene transcription. STAT3-IN-20 exhibits antiproliferative activities against STAT3-overactivated DU145 and MDA-MB-231 cancer cells (IC₅₀: 2.97 μM and 3.26 μM respectively). STAT3-IN-20 induces cell cycle arrest and apoptosis .

HY-N0897

Corylifol A

2 Publications Verification

Corylifol-A; Corylinin
STAT Others

Corylifol A inhibits IL-6-induced STAT3 activation and phosphorylation, with an IC₅₀ of 0.81 μM.

Corylifol A 2 Publications Verification Corylifol-A; Corylinin	STAT	Others
Corylifol A inhibits IL-6-induced *STAT3* activation and phosphorylation, with an IC₅₀ of 0.81 μM.

HY-12442

LY5	STAT Apoptosis	Cancer
LY5 is a *STAT3* inhibitor with an IC₅₀ value of 0.5 μM. LY5 induces apoptosis and inhibits STAT3 phosphorylation. LY5 shows antitumor activity in vivo, it can be used for the research of cancer .

HY-163176

WB518	STAT	Inflammation/Immunology
WB518 is a potent *STAT3* inhibitor. WB518 effectively inhibits STAT3 activation and Keratin 17 expression. WB518 effectively alleviates imiquimod (HY-B0180) and TPA (HY-18739)-induced animal psoriasis by inhibiting STAT3 phosphorylation and Keratin 17 .

HY-124858

SC99	STAT JAK Apoptosis	Cardiovascular Disease Cancer
SC99 is an orally active, selective *STAT3* inhibitor targeting JAK2-STAT3 pathway. SC99 docks into the ATP-binding pocket of JAK2. SC99 inhibits phosphorylation of JAK2 and STAT3 with no effects on the other kinases associated with STAT3 signaling. SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities .

HY-107595

SD-1008	JAK STAT Apoptosis	Cancer
SD-1008 is a potent JAK inhibitor. SD-1008 inhibits tyrosyl phosphorylation of STAT3, JAK2 and Src. SD-1008 also reduces STAT3-dependent luciferase activity. SD-1008 enhances apoptosis induced by Paclitaxel in ovarian cancer cells via directly blocking the JAK-STAT3 signaling pathway .

HY-19536

LLL12	STAT	Cancer
LLL12 is a small molecule inhibitor of *STAT3* that inhibits *STAT3* phosphorylation. LLL12 enhanced the inhibitory effect of Cisplatin (HY-17394) and Paclitaxel (HY-B0015) on ovarian cancer cell formation, migration, and growth .

HY-N1356

Reticuline	JAK STAT NF-κB Endogenous Metabolite	Cardiovascular Disease Inflammation/Immunology
Reticuline shows anti-inflammatory effects through *JAK2/STAT3* and NF-κB signaling pathways. Reticuline inhibits mRNA expressions of TNF-α, and IL-6 and reduces the phosphorylation levels of JAK2 and STAT3 . Reticuline exhibits cardiovascular effects .

HY-12960

SKLB4771 FLT3-IN-1	FLT3 c-Kit Apoptosis	Cancer
SKLB4771 is a potent and selective Flt3 inhibitor with an IC₅₀ value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue .

HY-148092

PM-43I	STAT	Inflammation/Immunology Cancer
PM-43I is a potent *STAT6* inhibitor and can reduce STAT6 phosphorylation level. PM-43I can be used in allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease and cancer research ^[1].

HY-10074

TPCA-1 25+ Cited Publications	IKK STAT Apoptosis	Inflammation/Immunology Cancer
TPCA-1 is a potent and selective inhibitor of IKK-2 with IC₅₀ of 17.9 nM. TPCA-1 is an effective inhibitor of *STAT3* phosphorylation, DNA binding, and transactivation.

HY-107429

Abrocitinib 4 Publications Verification PF-04965842	JAK	Inflammation/Immunology
Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC₅₀s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC₅₀, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease .

HY-112338

C188 CPD188	STAT	Cancer
C188 is a *STAT3* inhibitor that inhibits IL-6-stimulated STAT3 phosphorylation and nuclear translocation in HepG2 cells by targeting STAT3 SH2 domain peptide-binding pocket. C188, in particular, was highly active in inducing apoptosis of the breast cancer cell line MB-MDA-468 in vitro (EC₅₀= 0.7 μM).

HY-145935

NT219	Insulin Receptor STAT	Cancer
NT219 is a potent and dual inhibitor of insulin receptor substrates 1/2 (IRS1/2) and *STAT3. IRS1/2 and STAT3 are major signaling junctions regulated by various oncogenes. NT219 affects IRS1/2 degradation and inhibits* STAT3 phosphorylation. NT219 has the potential for the research of cancer diseases .

HY-139369

QD394	Reactive Oxygen Species	Cancer
QD394 is a reactive oxygen species (ROS) inducer that can induce lipid peroxidation, increase intracellular ROS accumulation, inhibit STAT3 phosphorylation, and induce ferroptosis .

HY-148093

PM-81I	STAT	Inflammation/Immunology Cancer
PM-81I is a potent *STAT6* inhibitor (targeting the SH2 structural domain) that effectively reduces *STAT6* phosphorylation levels. PM-81I can be used in studies of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease or cancer ^[1].

HY-107429R

Abrocitinib (Standard)	JAK	Inflammation/Immunology
Abrocitinib (Standard) is the analytical standard of Abrocitinib. This product is intended for research and analytical applications. Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC₅₀s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC₅₀, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease .

HY-P10283

S1H	GHSR STAT	Endocrinology
S1H, a mimetic of hGH, is a human growth hormone receptor (hGHR) antagonist. S1H inhibits the interaction of hGH with hGHR. S1H inhibits phosphorylation of STAT5 in cells co-treated with hGH .

HY-161015

JAK1-IN-13	JAK	Inflammation/Immunology
JAK1-IN-13 (compound 36b) is an orally active, potent and highly selective inhibitor of JAK1 with an IC₅₀ of 0.044 nM. JAK1-IN-13 significantly decreases *STAT3* phosphorylation .

HY-155746

JAK2-IN-9	JAK	Infection Inflammation/Immunology
JAK2-IN-9 (Compound A8) is a selective JAK2 inhibitor (IC₅₀: 5 nM). JAK2-IN-9 inhibits the phosphorylation of JAK2, STAT3, and STAT5. JAK2-IN-9 has metabolic stabilities. JAK2-IN-9 induces apoptosis. JAK2-IN-9 can be used for research of myeloproliferative neoplasms (MPNs) .

HY-N0236

Corylin 4 Publications Verification	Antibiotic STAT	Infection Metabolic Disease Cancer
Corylin is an orally active flavonoid anti-inflammatory and osteogenic agent that inhibits IL-6-induced STAT3 promoter activity and STAT3 phosphorylation. Corylin also has anticancer, antiatherosclerotic, and ameliorating activity in hyperlipidemia and insulin resistance, inducing adipocyte browning and lipolysis through SIRT1 or β3-AR-dependent pathways .

HY-153701

JAK-IN-26	JAK	Cancer
JAK-IN-26 (compound 2) is an orally active JAK inhibitor with good pharmacokinetic characteristics. JAK-IN-26 inhibits IFN-α2B-induced phosphorylation of *STAT3* in Jurkat cells (IC₅₀=17.2 nM) .

HY-101019

Ossirene 1 Publications Verification AS101	Interleukin Related Caspase	Inflammation/Immunology Cancer
Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor . Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies .

HY-N1987

Cucurbitacin IIb 1 Publications Verification	Apoptosis	Inflammation/Immunology
Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α .

HY-112724

Ivarmacitinib SHR0302	JAK Apoptosis	Inflammation/Immunology Cancer
Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits *JAK1-STAT3* phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects .

HY-153190A

W1131 TFA	Ferroptosis STAT	Cancer
W1131 TFA is a potent STAT3 inhibitor that induces ferroptosis. W1131 inhibits cancer progression in subcutaneous xenograft, organoid, and PDX models of gastric cancer. W1131 effectively alleviates cancer cell chemoresistance to 5-FU (HY-90006). W1131 regulates the cell cycle, DNA damage response, and oxidative phosphorylation, including the IL6-JAK-STAT3 pathway and the ferroptosis pathway .

HY-112724A

Ivarmacitinib sulfate SHR0302 sulfate	JAK Apoptosis	Inflammation/Immunology Cancer
Ivarmacitinib (SHR0302) sulfate is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits *JAK1-STAT3* phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects .

HY-136657

SC-43 2 Publications Verification	Phosphatase STAT Apoptosis	Cancer
SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of *STAT3* and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects .

HY-102084

LMT-28 5+ Cited Publications	Interleukin Related	Inflammation/Immunology
LMT-28 is an orally active and the first synthetic IL-6 inhibitor that functions through direct binding to gp130. LMT-28 shows low toxicity and selectively inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130 .

HY-15614

SC144 5 Publications Verification	Interleukin Related Apoptosis	Cancer
SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells .

HY-15614A

SC144 hydrochloride 5 Publications Verification	Interleukin Related Apoptosis	Cancer
SC144 hydrochloride is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 hydrochloride binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 hydrochloride shows potent inhibition of gp130 ligand-triggered signaling. SC144 hydrochloride induces apoptosis in human ovarian cancer cells .

HY-100037

NT157 1 Publications Verification Tyrphostin NT157	Insulin Receptor STAT	Endocrinology Cancer
NT157 (Tyrphostin NT157) is a selective IRS-1/2 inhibitor that induces Ser-phosphorylation and consequently the degradation of IRS-1/2. NT157 (Tyrphostin NT157) is a first-in-class anti-cancer agent that also targets *Stat3* signaling pathway .

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STAT phosphorylation inhibitor

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