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  3. JAK/STAT Signaling
    Stem Cell/Wnt
  4. STAT

STAT

STAT

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STAT is a family of cytoplasmic protein that regulates many aspects of growth, survival and differentiation in cells. The transcription factors of this family are activated by Janus kinase and dysregulation of this pathway is frequently observed in primary tumours and leads to increased angiogenesis, enhanced survival of tumours and immunosuppression. Gene knockout studies have provided evidence that STAT proteins are involved in the development and function of the immune system and play a role in maintaining immune tolerance and tumour surveillance. STAT proteins were originally described as latent cytoplasmic transcription factors that require phosphorylation for nuclear retention. The unphosphorylated STAT proteins shuttle between cytosol and the nucleus waiting for its activation signal. Once the activated transcription factor reaches the nucleus, it binds to consensus DNA-recognition motif called gamma-activated sites (GAS) in the promoter region of cytokine-inducible genes and activates transcription of these genes.

STAT Isoform Specific Products:

STAT Isoform Comparison
Cat. No. Nombre del producto Efecto Pureza Chemical Structure
  • HY-178716
    PTPN2/1-IN-4
    		Modulator
    PTPN2/1-IN-4 (Compound WS35) is an orally active, dual-functional inhibitor of PTPN1 and PTPN2 with IC50s of 12.8 and 5.8 nM for PTPN1 and PTPN2, respectively. PTPN2/1-IN-4 modulates the IFNγ-JAK-STAT signaling pathway and significantly augments CD8+ T-cell tumor infiltration. PTPN2/1-IN-4 has potent anticancer activity, robustly inhibiting tumor growth both as a monotherapy and in combination with an anti-PD-1 antibody in B16-OVA syngeneic mouse models.
    PTPN2/1-IN-4
  • HY-179732
    PROTAC ALK degrader-4
    		Inhibitor
    PROTAC ALK degrader-4 (Compound B8) is an ALK PROTAC degrader with a DC50 of 445.25 nM. PROTAC ALK degrader-4 exhibits excellent anti-proliferative activity against NCI-H2228 and NCI-H3122. PROTAC ALK degrader-4 leads to a significant downregulation of 390 proteins, including IGF-1R and its downstream proteins such as ERK1/2 and STAT3. PROTAC ALK degrader-4 can be used for research on lung adenocarcinoma. (Pink: ALK ligand (HY-15656); Blue: CRBN ligand (HY-179733); Black: linker).
    PROTAC ALK degrader-4
  • HY-D145729F
    FAM-Danvatirsen
    		Inhibitor
    FAM-Danvatirsen is a FAM-labeled Danvatirsen (HY-145729). Danvatirsen is an antisense oligonucleotide targeting STAT3 that can be used in the study of cancer.
    FAM-Danvatirsen
  • HY-169242
    JAK1-IN-16
    		Inhibitor
    JAK1-IN-16 (compound 4l) is an inhibitor of JAK1/STAT3 and effectively downregulates TLR4 protein expression..
    JAK1-IN-16
  • HY-N16376
    Thienodolin
    		Inhibitor
    Thienodolin (MJ 286A) is an alkaloid that has been found in S. albogriseolus. Thienodolin inhibits nitric oxide production in LPS (HY-D1056)-stimulated RAW 264.7 murine macrophage cells with an IC50 value of 17.2 μM. Thienodolin suppresses iNOS, blocks the degradation of IκBα, attenuates NF-κB p65 accumulation in the nucleus, and reduces the phosphorylation level of STAT1 at Tyr701. Thienodolin can be used for the study of inflammation.
    Thienodolin
  • HY-162405
    STAT6-IN-12
    		Inhibitor
    STAT6-IN-12 is a potent STAT6 inhibitor with an IC50 of 50 nM. STAT6-IN-12 also inhibits Smad2/3 with an IC50 of 68 nM. STAT6-IN-12 inhibits TGFβ-dependent Smad2/3 signaling pathway, IL-4-dependent STAT6 signaling pathway, and cellular inflammatory responses. STAT6-IN-12 can be used for the research of inflammation.
    STAT6-IN-12
  • HY-182430
    NVP-BVB808
    		Inhibitor
    NVP-BVB808 is a selective and ATP-competitive JAK2 inhibitor with an IC50 of 0.35 nM. NVP-BVB808 binds to JAK2’s ATP-binding site, stabilizes JAK2’s active conformation, increases JAK2 activation loop phosphorylation, and blocks downstream kinase function. NVP-BVB808 exhibits antiproliferative and pro-apoptosis effects, suppresses constitutive STAT5a phosphorylation. NVP-BVB808 can be used for the research of cancer, such as leukemia.
    NVP-BVB808
  • HY-168178
    Hsp110-STAT3 PPI-IN-2
    		Inhibitor
    Hsp110-STAT3 PPI-IN-2 (compound 10b) is a Hsp110-STAT3 interaction disruptor. Hsp110-STAT3 PPI-IN-2 can be used in pulmonary arterial hypertension (PAH) related research.
    Hsp110-STAT3 PPI-IN-2
  • HY-164349
    WZ-2-033
    		Inhibitor
    WZ-2-033 is a potent STAT3 inhibitor. WZ-2-033 inhibits MDA-MB-231, HCC70, and MDA-MB231-4175 cells proliferation, colony survival, migration, and invasion with IC50s of 0.7, 1.3, and 1.3 μM, respectively.
    WZ-2-033
  • HY-174386
    STAT3-IN-43
    		Inhibitor
    STAT3-IN-43 (Compound K2) is a covalent inhibitor targeting the allosteric site at the junction of the STAT3 coiled-coil domain and DNA-binding domain, with an IC50 of 40.7 μM. STAT3-IN-43 can be used in cancer research.
    STAT3-IN-43
  • HY-172201
    NF-κB-IN-19
    		Inhibitor
    NF-κB-IN-19 (Compound 8) is an NF-κB inhibitor. NF-κB-IN-19 effectively induces DNA damage, promotes the generation of ROS, and induces autophagy and apoptosis through the NF-κB signaling pathway in tumor cells. In addition, NF-κB-IN-19 can inhibit the levels of VEGF and HIF-1α, and exert antiproliferative activity in tumor cells through the PI3K/AKT and STAT-3 pathways. NF-κB-IN-19 can effectively overcome cisplatin resistance and has anti-tumor activity.
    NF-κB-IN-19
  • HY-179288
    TPST2-IN-1
    TPST2-IN-1 is a potent and selective TPST2 inhibitor with an IC50 of 946 nM and a Ka of 19.4 μM. TPST2-IN-1 increases the phosphorylation of Stat1 and upregulates the IFNγ-responsive gene CXCL10 by inhibiting TPST2 activity.TPST2-IN-1 exhibits anti-tumor activity and enhances T cell-mediated antitumor immunity characterized by increased infiltration of effector CD8+ T cells. TPST2-IN-1 can be used for the research of cancer, such as colon cancer.
    TPST2-IN-1
  • HY-181587
    PDGFRA/CAIX/XII-IN-1
    		Inhibitor
    PDGFRA/CAIX/XII-IN-1 is an inhibitor of PDGFRA, CA IX and CA XII, with an IC50 of 20 nM against PDGFRA, a Ki of 93.3 nM against CA IX, and a Ki of 80.0 nM against CA XII. PDGFRA/CAIX/XII-IN-1 binds to the ATP-binding pocket of PDGFRA and blocks the downstream STAT3, AKT and ERK1/2 signaling pathways. PDGFRA/CAIX/XII-IN-1 induces G0/G1 cell cycle arrest and endogenous apoptosis (Apoptosis), including cleavage of PARP-1, caspase-9 and caspase-3, activation of caspase 3/7, and down-regulation of Mcl-1. PDGFRA/CAIX/XII-IN-1 exhibits antiproliferative activity in eosinophilic leukemia cells. PDGFRA/CAIX/XII-IN-1 can be used for the research of leukemia.
    PDGFRA/CAIX/XII-IN-1
  • HY-183937A
    PD-305
    		Activator
    PD-305 is a selective PTPN2 PROTAC degrader, with DC50 values of 0.25 nM and 5.11 nM against PTPN2 and PTPN1, respectively. PD-305 enhances IFN-γ-induced STAT1 phosphorylation, inhibits the proliferation of IFN-γ-stimulated colorectal cancer cells, promotes CD8+ T cell activation, enhances the tumor-killing activity of T cells, and suppresses tumor growth in mouse models. PD-305 can be used for the research of colorectal cancer.
    PD-305
  • HY-183306
    mTOR/STAT3-IN-1
    		Inhibitor
    mTOR/STAT3-IN-1 is a dual mTOR/STAT3 inhibitor. mTOR/STAT3-IN-1 exhibits potent mTOR inhibitory activity and moderate STAT3 inhibitory activity, while exerting cell type-dependent antiproliferative and senolytic activities in human cell lines. mTOR/STAT3-IN-1 can be used in the research of glioblastoma and aging-related diseases.
    mTOR/STAT3-IN-1
  • HY-W704363
    Pimozide-d5
    Pimozide-d5 (R6238-d5) is the deuterium labeled Pimozide (HY-12987). Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
    Pimozide-d<sub>5</sub>
  • HY-180117
    MMP-2/9-IN-2
    		Inhibitor
    MMP-2/9-IN-2 (Compound 6k) is a MMP-2 and MMP-9 inhibitor, with IC50 values of 29.27 and 24.87 μM respectively. MMP-2/9-IN-2 exhibits good selective toxicity against multiple human hepatoma cell lines. MMP-2/9-IN-2 induces cell cycle arrest and apoptosis, significantly inhibits cell migration and invasion. MMP-2/9-IN-2 inhibits the phosphorylation of the STAT3 signaling pathway. MMP-2/9-IN-2 shows strong anti-tumor activity in a nude mouse xenograft model of HepG2 liver cancer cells.
    MMP-2/9-IN-2
  • HY-181901
    PROTAC STAT6 degrader-4
    		Degrader
    PROTAC STAT6 degrader-4 (Compound 3u247) is a STAT6 PROTAC degrader with a DC50 of 0.04 nM. PROTAC STAT6 degrader-4 promotes the ubiquitination and degradation of STAT6, and is applicable to the research of immune diseases.
    PROTAC STAT6 degrader-4
  • HY-162607
    STAT3-IN-28
    		Inhibitor
    STAT3-IN-28 (compound 18) is a STAT3 inhibitor. STAT3-IN-28 can inhibit the activation of microglia and has anti-neuroinflammatory effects. STAT3-IN-28 can cross the blood-brain barrier.
    STAT3-IN-28
  • HY-169361
    STAT3 ligand 5
    STAT3 ligand 5 is a ligand for STAT3, that can be used as target protein ligand for synthesis of PROTAC degrader SD-436 (HY-169360).
    STAT3 ligand 5
Cat. No. Nombre del producto / Synonyms Application Reactivity
STAT Isoform Comparison

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