STAT3
STAT3 is a widely expressed STAT family transcription factor that regulates cellular growth, differentiation, survival, immunity, hematopoiesis, and cell migration[1]. Mechanistically, cytokines and growth factors activate JAKs, phosphorylate STAT proteins, promote STAT dimerization, and drive nuclear transcriptional regulation[2]. In inflammatory disease models, STAT3 shows strong tyrosine phosphorylation in human ulcerative colitis, Crohn’s disease, and DSS-induced mouse colitis, where IL-6 deficiency reduces colitis and STAT3 activation[3]. In cancer models, persistent STAT3 activation supports proliferation, survival, invasion, metastasis, immune evasion, and drug resistance, making STAT3 signaling a practical axis for tumor biology research[1][4]. Compared with related isoforms, STAT1 knockout mice mainly show impaired interferon signaling, while STAT3 is emphasized in IL-6-linked inflammation, tumor progression, and Th17-related immune dysfunction[2][5]. For experimental applications, JAK/STAT inhibitors such as AG490 and AZD1480 reduce STAT1/STAT3 activation in renal ischemia-reperfusion and α-synuclein neuroinflammation models[6][7].
Références:
- [1]. Liu Y, et al. STAT3 and its targeting inhibitors in osteosarcoma. Cell Prolif. 2021 Feb;54(2):e12974. [Content Brief]
- [2]. Heim MH. The Jak-STAT pathway: cytokine signalling from the receptor to the nucleus. J Recept Signal Transduct Res. 1999 Jan-Jul;19(1-4):75-120. doi: 10.3109/10799899909036638. PMID: 10071751. et al. The Jak-STAT pathway: cytokine signalling from the receptor to the nucleus. J Recept Signal Transduct Res. 1999 Jan-Jul;19(1-4):75-120. [Content Brief]
- [3]. Suzuki A, et al. CIS3/SOCS3/SSI3 plays a negative regulatory role in STAT3 activation and intestinal inflammation. J Exp Med. 2001 Feb 19;193(4):471-81. [Content Brief]
- [4]. Wu CJ, et al. Activation of STAT3 and STAT5 Signaling in Epithelial Ovarian Cancer Progression: Mechanism and Therapeutic Opportunity. Cancers (Basel). 2019 Dec 19;12(1):24. [Content Brief]
- [5]. Tolomeo M, et al. The STAT Signaling Pathway in HIV-1 Infection: Roles and Dysregulation. Int J Mol Sci. 2025 Sep 18;26(18):9123. [Content Brief]
- [6]. Si Y, et al. Dexmedetomidine protects against renal ischemia and reperfusion injury by inhibiting the JAK/STAT signaling activation. J Transl Med. 2013 Jun 9;11:141. [Content Brief]
- [7]. Qin H, et al. Inhibition of the JAK/STAT Pathway Protects Against α-Synuclein-Induced Neuroinflammation and Dopaminergic Neurodegeneration. J Neurosci. 2016 May 4;36(18):5144-59. [Content Brief]
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STAT3 Inhibitors
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STAT3 Ligands
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STAT3 Produits associés (357)
Produits associés (357)
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Anticorps (5)
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Sorafenib
0 ImagesSynonyms: Bay 43-9006Sorafenib (Bay 43-9006) is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.
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Tofacitinib
0 ImagesSynonyms: Tasocitinib; CP-690550Tofacitinib (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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Deucravacitinib
0 ImagesSynonyms: BMS-986165Deucravacitinib (BMS-986165) is an orally active allosteric inhibitor of tyrosine kinase 2 (TYK2), with an IC50 of 0.2 nM and a Ki of 0.02 nM against the JH2 domain of TYK2, and it exhibits selectivity over other JAK subtypes and most of the kinome. Deucravacitinib blocks IL-23, IL-12, p-STAT1/3 and Type I IFN signaling, and inhibits Th17/Th1-mediated psoriasis inflammation. Deucravacitinib can be used in research related to moderate-to-severe plaque psoriasis, inflammatory bowel disease and systemic lupus erythematosus.
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Artesunate
0 ImagesArtesunate is an inhibitor of both STAT-3 and exported protein 1 (EXP1).
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ARV-825
0 ImagesARV-825 is a BET protein PROTAC degrader that recruits cereblon, and it targets BRD2, BRD3, and BRD4 for degradation via the ubiquitin-proteasome pathway. ARV-825 downregulates c-MYC, PLK1, MYCN, CDK4/6, JAK2, pSTAT3/5, PIM1, and Bcl-xL, upregulates p21 and p27, and modulates H3K27Ac-mediated transcription, the G2/M checkpoint, the Wnt/β-catenin pathway, and amino acid transport pathways. ARV-825 induces G1 phase cell cycle arrest, caspase 3/PARP-mediated apoptosis, DNA damage, and reactive oxygen species (ROS) production, reduces mitochondrial respiration, and simultaneously inhibits cell proliferation, clonogenic growth, and cell migration. ARV-825 is used in research on gastric cancer, leukemia, neuroblastoma, and cholangiocarcinoma.
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Tofacitinib citrate
0 ImagesSynonyms: Tasocitinib citrate; CP-690550 citrateTofacitinib citrate (Tasocitinib citrate) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib citrate blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib citrate 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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GYY4137
0 ImagesGY4137 is a sustained-release H2S donor possessing vasodilatory, antihypertensive, and anti-inflammatory activities. GY4137 can inhibit cell growth, induce apoptosis, and cause cell cycle arrest by blocking the STAT3 pathway, demonstrating potent anticancer activity.
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Homoharringtonine
0 ImagesSynonyms: Omacetaxine mepesuccinate; HHTHomoharringtonine (Omacetaxine mepesuccinate;HHT) is a cytotoxic alkaloid with antitumor properties which acts by inhibiting translation elongation.
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C188-9
0 ImagesSynonyms: TTI-101C188-9 (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.
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Colivelin
0 ImagesColivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury
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Astaxanthin
0 ImagesAstaxanthin, the red dietary carotenoid, is an orally effective and potent antioxidant. Astaxanthin inhibits NF-κB and down-regulates VEGF in blood glucose. Astaxanthin exerts anti-cancer cell proliferation, increases apoptosis, impairs migration and invasion by activating PPARγ and reducing the expression of STAT3. Astaxanthin also has neuroprotective and anti-inflammatory activity and can be used in studies of cancer, diabetic retinopathy, cardiovascular disease, and in the coloring of animal feed.
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Ritlecitinib
0 ImagesSynonyms: PF-06651600Ritlecitinib (PF-06651600) is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC50=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC50 >10 μ M). Ritlecitinib rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE).
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Scutellarin
0 ImagesScutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. Scutellarin is active against HIV-1IIIB, HIV-1(74V) and HIV-1KM018 with EC50s of 26 μM, 253 μM and 136 μM, respectively.
