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Pathways Recommended: JAK/STAT Signaling
Results for "

STAT SH2

" in MedChemExpress (MCE) Product Catalog:

28

Inhibitors & Agonists

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Natural
Products

1

Antibodies

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13818
    Stattic
    Maximum Cited Publications
    280 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 .
    Stattic
  • HY-112288
    C188-9
    30+ Cited Publications

    TTI-101

    		 STAT Apoptosis DNA Methyltransferase Metabolic Disease Inflammation/Immunology Cancer
    C188-9 (TTI-101) is a STAT3 inhibitor with a Kd value of 4.7 nM. C188-9 targets the SH2 domain of STAT3, blocks the processes of STAT3 ligand binding, receptor recruitment, homodimerization and phosphorylation, and regulates STAT3-mediated genes associated with tumorigenesis and radioresistance. C188-9 regulates STAT1-mediated genes related to radioresistance and reduces the activation level of STAT1. C188-9 downregulates the expression of DNMT1, enhances DAC-induced demethylation and re-expression of RASSF1A, and simultaneously potentiates the anti-tumor effect of DAC on pancreatic cancer cells. C188-9 inhibits both anchorage-dependent and anchorage-independent growth of cancer cells, induces Apoptosis, blocks the growth of tumor xenografts, and suppresses muscle atrophy. C188-9 maintains muscle mass, increases body weight and improves grip strength in tumor-bearing mice. C188-9 can be used in research related to head and neck squamous cell carcinoma, pancreatic cancer, sepsis-related skeletal muscle wasting, non-small cell lung cancer, acute myeloid leukemia and cancer cachexia .
    C188-9
  • HY-148096
    STAT6-IN-1
    1 Publications Verification

    		 STAT Inflammation/Immunology Cancer
    STAT6-IN-1 (Compound 19a) is a STAT6 inhibitor with a high affinity for the SH2 domain of STAT6 (IC50=0.028 µM). STAT6-IN-1 can be used in studies of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease or cancer .
    STAT6-IN-1
  • HY-129603
    SI-109
    2 Publications Verification

    		 STAT Ligands for Target Protein for PROTAC Cancer
    SI-109 is a potent STAT3 SH2 domain inhibitor (Ki=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36 .
    SI-109
  • HY-153992
    STAT6-IN-3
    1 Publications Verification

    		 STAT Inflammation/Immunology
    STAT6-IN-3 is a phosphopeptide mimic targeting the SH2 domain of STAT6 and has a high affinity for STAT6 (IC50: 0.04 μM). STAT6-IN-3 can be used in the research of inflammation such as asthma .
    STAT6-IN-3
  • HY-124500
    AC-4-130
    5+ Cited Publications

    		 STAT Apoptosis Cancer
    AC-4-130 is a potent STAT5 SH2 domain inhibitor. AC-4-130 directly binds to STAT5 and disrupts STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription. AC-4-130 induces cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 has anti-cancer activity and can efficiently block pathological levels of STAT5 activity in acute myeloid leukemia (AML) .
    AC-4-130
  • HY-112647
    Stafib-1
    1 Publications Verification

    		 STAT Cancer
    Stafib-1 is the first selective inhibitor of the STAT5b SH2 domain, with a Ki of 44 nM and an IC50 of 154 nM .
    Stafib-1
  • HY-W035137
    5,15-Diphenylporphyrin

    5,15-DPP

    		 STAT Cancer
    5,15-Diphenylporphyrin (5,15-DPP) is an inhibitor of the oncogenic transcription factor STAT3. 5,15-Diphenylporphyrin specifically binds to the SH2 domain of STAT3, blocking the pTyr-SH2 interaction, thereby inhibiting the dimerization, nuclear translocation and DNA binding activity of STAT3, and ultimately inhibiting the expression of cancer cell-related genes. 5,15-Diphenylporphyrin can be used in research fields related to the development of anticancer drugs[1][2].
    5,15-Diphenylporphyrin
  • HY-115594
    Erasin

    		STAT Apoptosis Cancer
    Erasin is a potent Erlotinib (HY-50896)-resistance antagonizing STAT3 inhibitor with IC50s of 9.7 and 24 μM against STAT3 and STAT1, respectively. Erasin induces cancer cells apoptosis .
    Erasin
  • HY-112338
    C188

    CPD188

    		 STAT Apoptosis Cancer
    C188 (CPD188) is a STAT3 inhibitor with anticancer effects. C188 inhibits STAT3 SH2/pY-peptide binding (IC50 of 20 µM against pY-peptide binding) and IL-6-mediated STAT3 phosphorylation. C188 is selective for STAT3 over STAT1. C188 inhibits nuclear-to-cytoplasmic translocation of Stat3. C188 shows highly active induces apoptosis in breast cancer cell lines with constitutive Stat3 activation (EC50s of 0.73 µM, 3.96 µM, and 7.01 µM in MDA-MB-468, MDA-MB-231, and MDA-MB-435 cultures, respectively) .
    C188
  • HY-151577
    STAT3-SH2 domain inhibitor 1

    		STAT Apoptosis Cancer
    STAT3-SH2 domain inhibitor 1 is a potent Src Homology 2 (SH2) Domain of STAT3 (STAT3-SH2 domain) inhibitor with a Kd value of 1.57 μM. STAT3-SH2 domain inhibitor 1 inhibits STAT3 signaling transduction and transcriptional activation. STAT3-SH2 domain inhibitor 1 induces apoptosis in gastric cancer cells. STAT3-SH2 domain inhibitor 1 can be used in research of cancer .
    STAT3-SH2 domain inhibitor 1
  • HY-121725
    MM-206

    		STAT Cancer
    MM-206, a STAT3 activity inhibitor, potently inhibits the STAT3 SH2 domain-phosphopeptide interaction with IC50 of 1.2 μM. MM-206 demonstrates dose-dependent induction of apoptosis in acute myeloid leukemia (AML) cell lines .
    MM-206
  • 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].
    PM-81I
  • HY-150603
    STAT3-IN-13
    1 Publications Verification

    		 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 KD 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 .
    STAT3-IN-13
  • HY-N6651
    Isocryptotanshinone

    		STAT Phosphatase Apoptosis Autophagy p38 MAPK EGFR JAK Bcl-2 Family Survivin Akt mTOR PARP Caspase Atg8/LC3 CDK Cancer
    Isocryptotanshinone is a dual STAT3 and PTP1B (IC50 = 56.1 μM) inhibitor. Isocryptotanshinone inhibits STAT3 by binding to the STAT3 SH2 domain to block phosphorylation and nuclear translocation [1][2]. Isocryptotanshinone exerts its anti-proliferative effect via the induction of cell cycle arrest, apoptosis, and pro-death autophagy, through the regulation of STAT3, AKT/mTOR and MAPK signaling pathways. Isocryptotanshinone suppresses the xenograft gastric cancer (GC) tumor growth in BALB/c nude mice. Isocryptotanshinone can be used for cancer research, such as lung cancer, breast cancer and GC .
    Isocryptotanshinone
  • 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 .
    STAT3-IN-20
  • HY-13818R
    Stattic (Standard)

    		STAT Apoptosis Inflammation/Immunology Cancer
    Stattic (Standard) is the analytical standard of Stattic. This product is intended for research and analytical applications. 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 .
    Stattic (Standard)
  • HY-175771
    STAT3-IN-46

    		STAT c-Myc Bcl-2 Family Interleukin Related JAK Cancer
    STAT3-IN-46 is a selective and orally active inhibitor of signal transducer and activator of transcription 3 (STAT3) (KD = 323.3 nM). STAT3-IN-46 directly binds to the SH2 domain of the STAT3 and inhibits IL-6/JAK/STAT3 signaling pathway (IC50 = 0.87 μM) and downregulates c-Myc and Bcl-2 levels. STAT3-IN-46 can be used for the research of cancer, such as triple-negative breast cancer .
    STAT3-IN-46
  • HY-179468
    STAT3-IN-49

    		STAT Cancer
    STAT3-IN-49 (compound B16) is a potent and selective STAT3 inhibitor. STAT3-IN-49 binds to the SH2 domain of STAT3, thereby suppressing its phosphorylation and nuclear translocation. STAT3-IN-49 inhibits triple-negative breast cancer (TNBC) cell migration, invasion, and colony formation. STAT3-IN-49 inhibits tumor growth in an MDA-MB-231 xenograft mouse model. STAT3-IN-49 can be used for TNBC research .
    STAT3-IN-49
  • HY-164445
    STAT3-IN-32

    		STAT Cancer
    STAT3-IN-32 (compound 2p) is an orally active, potent STAT3 dual phosphorylation inhibitor with an indole-containing tetra-aromatic heterocycle scaffold. STAT3-IN-32 exhibits STAT3 luciferase inhibition activity using HEK293T cells with an IC50 of 5.3 nM and ATP production inhibition activity using BxPC-3 cells with an IC50 of 4.2 nM. STAT3-IN-32 significantly blocks p-Tyr705 and p-Ser727 and causes the abrogation of the corresponding nuclear transcription and mitochondrial oxidative phosphorylation functions of STAT3 by targeting the STAT3 SH2 domain (KD=21.3 nM). STAT3-IN-32 exhibits significant suppressive effects in a pancreatic cancer xenograft model .
    STAT3-IN-32
  • HY-146728
    STAT3-IN-10

    		STAT Apoptosis Cancer
    STAT3-IN-10 is a STAT3 inhibitor with an IC50 value of 5.18 µM. STAT3-IN-10 directly binds to STAT3 SH2 domain, induces cancer cells apoptosis .
    STAT3-IN-10
  • HY-168043
    STAT3-IN-35

    		STAT Cancer
    STAT3-IN-35 is a STAT3 inhibitor that binds to SH2 domain. STAT3-IN-35 inhibits the phosphorylation of STAT3 and possesses antiproliferative activities against triple-negative breast cancer (TNBC) cell lines. STAT3-IN-35 also has a toxicity and potent antitumor activity in a TNBC xenograft model .
    STAT3-IN-35
  • HY-169797
    STAT3-IN-38

    		STAT Survivin Apoptosis Cancer
    STAT3-IN-38 (Compound 4m) is an inhibitor of STAT3 (KD of rhSTAT3: 45.33  µM). STAT3-IN-38 binds to the SH2 domain of STAT3 protein and suppresses the STAT3’s phosphorylation at site pTyr705 as well as its downstream genes (Survivin and Mcl-1). STAT3-IN-38 could block cell-cycle and induce Apoptosis in colorectal cancer cells .
    STAT3-IN-38
  • HY-12135
    Poloxipan

    		Polo-like Kinase (PLK) PIN1 STAT Cancer
    Poloxipan is a pan-specific polo-like kinase (PLK) inhibitor that can inhibit a non-catalytic region at the C-terminus called the Polo-box domain (PBD) found in kinases. The IC50 values for Poloxipan against the PBDs of PLK-1/2/3 are 3.2 μM, 1.7 μM, and 3.0 μM, respectively. Poloxipan also inhibits other phospho-tyrosine binding domains, such as the forkhead-associated (FHA) domain of CHK-2, the WW domain of peptidyl-prolyl cis/trans isomerase (PIN1), and the phospho-tyrosine binding domains of STAT1/3/5 and lymphocyte-specific protein tyrosine kinase's SH2 domain. Poloxipan can be used in cancer research .
    Poloxipan
  • HY-181514
    STAT3-IN-53

    		STAT CDK c-Myc Apoptosis Cancer
    STAT3-IN-53 (Compound L20) is a STAT3 inhibitor with a Kd value of 6.16 μM. STAT3-IN-53 binds directly to the SH2 domain of STAT3, inhibits phosphorylation at the Y705 site without affecting the total STAT3 protein level, and suppresses the IL-6/JAK/STAT3 pathway. STAT3-IN-53 downregulates the transcription and expression of cyclin-D1 and c-Myc. STAT3-IN-53 induces cell cycle arrest and promotes Apoptosis. STAT3-IN-53 exhibits anticancer activity against colorectal cancer .
    STAT3-IN-53
  • HY-182380
    ODZ10117

    		STAT NOD-like Receptor (NLR) Apoptosis Others Neurological Disease Inflammation/Immunology Cancer
    ODZ10117 is a STAT3 and NLRP3 inhibitor with a human STAT3 SH2 domain IC50 of 7.5 μM. ODZ10117 binds to the STAT3 SH2 domain, suppressing tyrosine phosphorylation, dimerization, nuclear translocation, and transcriptional activity. ODZ10117 binds to NLRP3, impairs NEK7 interaction, prevents inflammasome formation, and inhibits caspase-1 and IL-1β cleavage.ODZ10117 reduces MSU (HY-B2130A)-induced IL-1β release, lowers LPS (HY-D1056)-induced sepsis mortality, and exhibits anti-inflammatory effects. ODZ10117 induces apoptosis, suppresses breast cancer cell migration and invasion, reduces tumor growth and lung metastasis, and extends survival in breast cancer models. ODZ10117 can be used for the research of Monosodium urate (HY-B2130A)-induced peritonitis, LPS-induced sepsis, breast cancer, glioblastoma, and Alzheimer's disease .
    ODZ10117
  • HY-180245
    STAT3-IN-51

    		STAT Ferroptosis Apoptosis Glutathione Peroxidase Bcl-2 Family Reactive Oxygen Species (ROS) Cancer
    STAT3-IN-51 is a STAT3 inhibitor that directly binds to the STAT3 SH2 domain. STAT3-IN-51 induces apoptosis, ferroptosis, and immunogenic cell death (ICD) to potentiate anti-tumor immunity. STAT3-IN-51 inhibits STAT3 activation (phosphorylation, p-STAT3) and its downstream signaling. STAT3-IN-51 induces ROS generation, decreases Bcl-2 expression, disruptes mitochondrial function, suppresses GPX4 activity, and promotes lipid peroxidation. STAT3-IN-51 can be used for the study of colorectal carcinoma, breast adenocarcinoma, non-small cell lung cancer (NSCLC) and Cisplatin (HY-17394)-resistant pulmonary adenocarcinoma .
    STAT3-IN-51
  • HY-182288
    YN11

    		STAT Apoptosis Cancer
    YN11 is a STAT3 inhibitor (Kd=11.9 μM). YN11 directly binds to the SH2 domain of STAT3, inhibits the phosphorylation of STAT3, and reduces the expression of downstream target proteins. YN11 induces cell cycle arrest, promotes apoptosis, and inhibits cell invasion and migration in prostate cancer cells. YN11 suppresses tumor growth in a prostate cancer xenograft mouse model. YN11 does not cause significant body weight loss or obvious histopathological changes in major organs in xenograft mice. YN11 is applicable to relevant research on prostate cancer .
    YN11

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