STAT1
Signal transducer and activator of transcription 1 (STAT1) is a critical transcription factor that mediates cellular responses to interferons and cytokines by undergoing tyrosine phosphorylation, dimerization, and nuclear translocation to regulate target gene expression[1][2]. Mechanistically, STAT1 modulates the JAK/STAT signaling pathway, influencing immune regulation, apoptosis, and inflammation, and it can inhibit the Ras-MAPK pathway and Rho GTPase expression, thereby controlling cell proliferation and adhesion[3]. STAT1 exists as functionally distinct α and β isoforms, which differ in transcriptional activity and protein stability; STAT1β specifically enhances tumor immune surveillance by promoting CD8+ T-cell infiltration and suppressing M2 macrophage polarization in ovarian cancer[4]. In disease models, aberrant STAT1 activation contributes to epithelial ovarian cancer progression, airway inflammation, and spinal cord injury, while targeted inhibition of STAT1 reduces apoptosis and inflammatory responses[5][6][7]. Compared with other STAT family members, STAT1 exhibits unique regulatory interactions, such as selective inhibition by PIAS1 and differential phosphorylation at Y701 and S727, which modulate both canonical and non-canonical pathways[1][3]. Small-molecule inhibitors and agonists, including fostamatinib, MK256, and 15dPGJ2, have been shown to modulate STAT1 activity in vitro and in vivo, offering tools for experimental intervention and potential therapeutic applications[8][9][2]. These findings position STAT1 as a key regulator of immune and stress responses, distinct from related isoforms, and a targetable node for experimental and clinical studies.
References:
- [1]. Tian X, et al. Physical interaction of STAT1 isoforms with TGF-β receptors leads to functional crosstalk between two signaling pathways in epithelial ovarian cancer. J Exp Clin Cancer Res. 2018 May 11;37(1):103. [Content Brief]
- [2]. Huang XP, et al. miR-135a inhibits airway inflammatory response in asthmatic mice via regulating JAK/STAT signaling pathway. Braz J Med Biol Res. 2021 Jan 15;54(3):e10023. [Content Brief]
- [3]. Lan N, et al. STAT1β modulates the tumor immune microenvironment to improve prognosis in ovarian cancer: a comprehensive study of transcriptional and protein expression differences. J Ovarian Res. 2025 Aug 23;18(1):192. [Content Brief]
- [4]. Liu B, et al. Inhibition of Stat1-mediated gene activation by PIAS1. Proc Natl Acad Sci U S A. 1998 Sep 1;95(18):10626-31. [Content Brief]
- [5]. Guo R, et al. Fostamatinib, a Spleen Tyrosine Kinase Inhibitor, Exerts Anti-Inflammatory Activity via Inhibiting STAT1/3 Signaling Pathways. J Inflamm Res. 2024 Nov 25;17:9757-9771. [Content Brief]
- [6]. Lee JC, et al. MK256 is a novel CDK8 inhibitor with potent antitumor activity in AML through downregulation of the STAT pathway. Oncotarget. 2022 Nov 2;13:1217-1236. [Content Brief]
- [7]. Wu YX, et al. STAT1 inhibitor alleviates spinal cord injury by decreasing apoptosis. Genet Mol Res. 2016 Mar 28;15(1). [Content Brief]
- [8]. Wang S, et al. Stat1 is an inhibitor of Ras-MAPK signaling and Rho small GTPase expression with implications in the transcriptional signature of Ras transformed cells. Cell Cycle. 2009 Jul 1;8(13):2070-9. [Content Brief]
- [9]. Chen CW, et al. Inhibition of IFN-gamma-mediated inducible nitric oxide synthase induction by the peroxisome proliferator-activated receptor gamma agonist, 15-deoxy-delta 12,14-prostaglandin J2, involves inhibition of the upstream Janus kinase/STAT1 signaling pathway. J Immunol. 2003 Jul 15;171(2):979-88. [Content Brief]
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STAT1 Related Products (61)
Related Products (61)
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Antibodies (6)
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Fa-Au
0 ImagesCat. No.: HY-183554Fa-Au is a TrxR inhibitor. Fa-Au downregulates GPX4, induces oxidative stress, mitochondria-associated ferroptosis (ferroptosis) and immunogenic cell death. Fa-Au induces ROS production in hepatoma cells. Fa-Au remodels the tumor immune microenvironment via M1 macrophage polarization, dendritic cell maturation, CD8+ T cell activation and reduction of regulatory T cells. Fa-Au induces an anti-tumor immune feedback loop through the IFNγ/STAT1/SLC7A11 axis. Fa-Au inhibits tumor growth. Fa-Au is applicable to hepatocellular carcinoma-related research.
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BAY-356
0 ImagesCat. No.: HY-P992321BAY-356, a potent TWEAK receptor agonist, is an aglycosylated anti-TWEAK receptor antibody. BAY-356 triggers TWEAKR hyperactivation, activates NFκB and STAT1 pathways, and undergoes TWEAKR-dependent internalization. BAY-356 can be used for the research of colorectal cancer, bladder cancer, non-small cell lung cancer and pancreatic cancer[1][2].
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ITA-5
0 ImagesCat. No.: HY-178915CAS No.: 2374162-36-2
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Apoptosis inducer 55
0 ImagesCat. No.: HY-180226Apoptosis inducer 55 (Compound 10) is an Apoptosis inducer. Apoptosis inducer 55 induces rapid apoptosis via the intrinsic pathway. Apoptosis inducer 55 potently inhibits several signaling cascades including AKT, ERK1/2, STAT1, STAT3, and S6K. Apoptosis inducer 55 has anti-cancer activity against melanoma.
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Orazipone
0 ImagesCat. No.: HY-106981CAS No.: 137109-78-5Synonyms: OR 1384Orazipone (OR 1384) is a small molecule immunomodulator with strong anti-inflammatory properties. Orazipone exerts its immunomodulatory effect by forming reversible thiol complexes, which bind to intracellular signaling proteins and the thiol groups of glutathione. Orazipone exhibits potent anti-eosinophilic activity by inducing apoptosis. Orazipone inhibits activation of inflammatory transcription factors NF-kB and STAT 1 and decreases inducible iNOS expression and NO production in response to inflammatory stimuli. Orazipone reduces NADPH oxidase activity and thereby decreases ROS production. Orazipone has a protective effect in intestinal radiation injury.
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PTPN2/1-IN-4
0 ImagesCat. No.: HY-178716CAS No.: 3093350-55-8PTPN2/1-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.
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Tofacitinib-13C3,15N
0 ImagesCat. No.: HY-40354S1Purity: 99.57%Synonyms: Tasocitinib-13C3,15N; CP-690550-13C3,15NTofacitinib-13C3,15N (Tasocitinib-13C3,15N; CP-690550-13C3,15N) is the 15N, 13C-labeled Tofacitinib (HY-40354). Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.
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TPST2-IN-1
0 ImagesCat. No.: HY-179288TPST2-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.
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PD-305
0 ImagesCat. No.: HY-183937APD-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.
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ADGRL1-IN-1
0 ImagesCat. No.: HY-184118CAS No.: 693829-95-7ADGRL1-IN-1 is a ADGRL1 inhibitor. ADGRL1-IN-1 activates the GSK3β-STAT1 signaling axis. ADGRL1-IN-1 induces anti-tumor immunity in a CT26 colorectal cancer mouse model. ADGRL1-IN-1 can be used in studies related to colorectal cancer.
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JAK1-IN-21
0 ImagesCat. No.: HY-184592JAK1-IN-21, biotin-conjugated isoxazole derivative, is a JAK1 inhibitor. JAK1-IN-21 directly engages and stabilizes JAK1, reduces the phosphorylation of JAK1, STAT1 and AKT, induces apoptotic marker cleavage (PARP, Caspase-3, Caspase-7) and exhibits broad-spectrum antiproliferative activity against cancer cells. JAK1-IN-21 can be used for the study of liver cancer, prostate cancer, and breast cancer.
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KSI-028
0 ImagesCat. No.: HY-183537KSI-028 is a STING inhibitor. KSI-028 disrupts STING-mediated signal transduction, reduces IFN-β and pro-inflammatory cytokine (IL-6, IL-1β and TNF-α) production. KSI-028 inhibits the phosphorylation of STING, TBK1, IRF3, and STAT1. KSI-028 attenuates renal and hepatic injury in a Cisplatin (HY-17394)-induced acute kidney injury mouse model.
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SNX631
0 ImagesCat. No.: HY-187035CAS No.: 868066-26-6SNX631 is an orally active and selective CDK8/CDK19 inhibitor. SNX631 reduces the phosphorylation of STAT1/STAT3 S727, and upregulates miR-21-5p, miR-21-3p and miR-221 in cancer cells. SNX631 transcription-independently inhibits meiotic resumption in mouse oocytes, blocks nuclear envelope breakdown, first polar body extrusion and mitochondrial expansion and aggregation, with no cytotoxicity. SNX631, in combination with Lapatinib (HY-50898) or Trastuzumab (HY-P9907), synergistically inhibits cancer cell growth, upregulates the tumor suppressor BTG2, prevents Lapatinib-induced upregulation of oncogenic miRNAs, overcomes drug resistance, reduces the infiltration of αSMA+ stromal fibroblasts and ARG1+ M2 macrophages, and exhibits favorable biosafety. SNX631 can be used in studies related to HER2-positive breast cancer and cancer.
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Polθ-IN-11
0 ImagesCat. No.: HY-183748CAS No.: 3082173-75-6Polθ-IN-11 is an orally active DNA polymerase θ (Polθ) ATPase inhibitor with an IC50 of 4.3 nM against human targets. Polθ-IN-11 activates the cGAS-STING pathway. Polθ-IN-11 upregulates the expression of PD-L1 in HR-deficient cancer cells. Polθ-IN-11 acts synergistically with PARP inhibition in HR-deficient cancer cells and in vivo xenograft models. Polθ-IN-11 can be used in studies related to HR-deficient cancers.
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Tofacitinib hydrochloride
0 ImagesCat. No.: HY-40354HCAS No.: 1803005-18-6Synonyms: Tasocitinib hydrochloride; CP-690550 hydrochlorideTofacitinib hydrochloride (Tasocitinib hydrochloride) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib hydrochloride blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib hydrochloride can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.
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Tofacitinib-13C
0 ImagesCat. No.: HY-40354S3Synonyms: Tasocitinib-13C; CP-690550-13CTofacitinib-13C (Tasocitinib-13C; CP-690550-13C) is the 13C-labeled Tofacitinib (HY-40354). Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.
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MK256
0 ImagesCat. No.: HY-183423CAS No.: 2271348-04-8MK256 is an orally active, selective CDK8 inhibitor and CDK19/cyclin C inhibitor with IC50 values of 2.5 nM and 3.3 nM, respectively. MK256 downregulates phosphorylated STAT1 (S727), STAT5 (S726), MCL-1 mRNA and CCL2 mRNA. MK256 exhibits anti-tumor activity in acute myeloid leukemia. MK256 can be used for the research of acute myeloid leukemia.
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Tofacitinib-d3
0 ImagesCat. No.: HY-40354S5Synonyms: Tasocitinib-d3; CP-690550-d3Tofacitinib-d3 (Tasocitinib-d3; CP-690550-d3) is the deuterated-labeled Tofacitinib (HY-40354). Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.
