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].
References:
- [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 Related Products (309)
Related Products (309)
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Antibodies (5)
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Antitumor agent-195
0 ImagesCat. No.: HY-170947Antitumor agent-195 (compound 16c) is a dual targeting agent of STAT3 and NQO1. Antitumor agent-195 significantly inhibits phosphorylation of STAT3 at Tyr705 at a concentration of 1 μM and effectively induce Apoptosis in MDAMB-231 and MDA-MB-468 breast cancer cells. Antitumor agent-195 as a NQO1 substrate strongly increases ROS generation and causes severe DNA damage in a dose-dependent manner. Antitumor agent-195 shows encouraging anti-tumor efficacy in the MDA-MB-231 xenograft model.
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ALOX5 stabilizer-1
0 ImagesCat. No.: HY-175634ALOX5 stabilizer-1 is an arachidonate 5-lipoxygenase (ALOX5) stabilizer with a Kd of 7.26 μM. ALOX5 stabilizer-1 inhibits β-catenin protein levels and then suppresses STAT3 signal pathway. ALOX5 stabilizer-1 induces lung cancer cells apoptosis, inhibited cell migration and proliferation. ALOX5 stabilizer-1 can used for the study of non-small cell lung cancer (NSCLC).
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STAT-3/c-Src-IN-1
0 ImagesCat. No.: HY-175298STAT-3/c-Src-IN-1 (Compound 12d) is a dual STAT-3 (IC50=0.844 μM) and c-Src (IC50=0.268 μM) inhibitor. STAT-3/c-Src-IN-1 blocks tumor cell proliferation, migration, and angiogenesis signaling pathways. STAT-3/c-Src-IN-1 exhibits potent anti-proliferative activity against melanoma (SK-MEL-2) and CNS cancer (SNB-75) cell lines (GI50=-5.75 μM and -5.63 μM), inducing tumor cell apoptosis via G0/G1 and G2/M phase cell cycle arrest. STAT-3/c-Src-IN-1 is promising for research of melanoma and glioblastoma.
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7α-Morroniside
0 ImagesCat. No.: HY-N20636CAS No.: 61849-88-5
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Balsalazide disodium
0 ImagesCat. No.: HY-108244CAS No.: 213594-60-6Balsalazide disodium is a prodrug of amino salicylic acid that releases mesalamine (HY-15027) in the colon, offering various anti-inflammatory effects in areas of colitis, and it also exerts related anticancer effects by regulating the IL-6/STAT3 pathway.
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Cyclo(L-Ile-D-Leu)
0 ImagesCat. No.: HY-N18989CAS No.: 2193113-02-7
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15-Keto-prostaglandin E2-d4
0 ImagesCat. No.: HY-113205S1CAS No.: 2738376-85-515-Keto-prostaglandin E2-d4 is the d4 labeled 15-keto-Prostaglandin E2 (HY-113205). 15-keto-Prostaglandin E2 (15-keto-PGE2) is an endogenous PGE2 metabolite. 15-keto-Prostaglandin E2 inhibits STAT3 activation by binding to the Cys259 residue of STAT3. 15-keto-Prostaglandin E2 binds to and stabilizes EP2 and EP4 receptors. 15-keto-Prostaglandin E2 inhibits the growth and progression of breast cancer cells. 15-keto-Prostaglandin E2 activates PPAR-γ and promotes fungal growth. 15-keto-Prostaglandin E2 disrupts glomerular vascularization during zebrafish development and reduces the surface area of the glomerular filtration barrier.
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GYY4137 (GMP)
0 ImagesCat. No.: HY-107632GCAS No.: 106740-09-4GYY4137 (GMP) is the GMP-grade version of GYY4137 (HY-107632). Small molecules of GMP grade can be used as adjuvant reagents in cell therapy. GYY4137 (GMP) is a sustained-release H2S donor possessing vasodilatory, antihypertensive, and anti-inflammatory activities. GYY4137 (GMP) can inhibit cell growth, induce apoptosis, and cause cell cycle arrest by blocking the STAT3 pathway, demonstrating potent anticancer activity.
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MPT0B098
0 ImagesCat. No.: HY-124595CAS No.: 1254363-89-7MPT0B098 is a microtubule inhibitor with a Ki of 0.8 μM and an IC50 of 0.8 μM. MPT0B098 inhibits tubulin polymerization, blocks HuR nuclear-cytoplasmic translocation to decrease HIF-1α mRNA stability, suppresses HIF-1α, TGF-β/Smad, JAK2/STAT3 and FAK/actin cytoskeleton signaling pathways, upregulates SOCS3 to reinforce the inhibition of JAK2/STAT3 cascade, and induces apoptosis. MPT0B098 can be used for research on multiple malignancies including head and neck squamous cell carcinoma and human non-small cell lung cancer.
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DETD-35
0 ImagesCat. No.: HY-164473CAS No.: 1836209-98-3DETD-35 is an inhibitor of the MEK-ERK, Akt, and STAT3 signaling pathways, which promotes cancer cell apoptosis (Apoptosis) and reduces cancer cell resistance to Vemurafenib (HY-12057). The IC50 values of DETD-35 against wild-type and mutant melanoma cell lines B16-F10, MeWo, SK-MEL-2, A2058c, and A375c are 2.7, 6.0, 3.9, 3.1, and 2.5 μM, respectively. DETD-35 holds promise for research in the field of anti-melanoma therapy.
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Isocucurbitacin B
0 ImagesIsocucurbitacin B is a natural terpenoid compound found in Pedicellus Melo. Isocucurbitacin B can inhibit the PI3K/AKT, MAPK, and STAT3 signaling pathways and downregulate CAV1 expression. Isocucurbitacin B can inhbit cancer cell proliferation, migration and invision. Isocucurbitacin B can induce apoptosis and cause G2/M phase arrest. Isocucurbitacin B can decrease intracellular cholesterol and PH levels and increase intracellular calcium levels. Isocucurbitacin B can be used for the research of cancer, such as glioma[1][2].
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STAT3-IN-39
0 ImagesCat. No.: HY-171038CAS No.: 3037596-35-0STAT3-IN-39 (compound 10K) is an orally active STAT3 inhibitor that exhibits excellent inhibitory activity against STAT3 phosphorylation, with an IC50 of 0.47 μM in NIH-3T3 cells. STAT3-IN-39 inhibits the TGF-β1-induced fibrotic response and blocks the epithelial-mesenchymal transition in A549. STAT3-IN-39 can be utilized in research related to idiopathic pulmonary fibrosis.
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Pulchinenoside E2
0 ImagesPulchinenoside E2 is a triterpenoid saponin. Pulchinenoside E2 inhibits the phosphorylation of STAT3 and JAK2, blocks the nuclear translocation and transcriptional activity of STAT3, and suppresses STAT3-dependent mitochondrial oxidative phosphorylation. Pulchinenoside E2 inhibits invasion, migration and autophagy of triple-negative breast cancer cells. Pulchinenoside E2 can be used in research related to triple-negative breast cancer.
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Tyk2-IN-25
0 ImagesCat. No.: HY-184833CAS No.: 2417137-50-7
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STA-1474 sodium
0 ImagesCat. No.: HY-13752BCAS No.: 1402907-09-8STA-1474 sodium is an orally active and highly selective HSP90 inhibitor, as well as a phosphate prodrug of the HSP90 inhibitor STA-9090 (HY-15205). STA-1474 sodium disrupts the chaperone function of HSP90 and promotes the degradation of client proteins. STA-1474 sodium inhibits the phosphorylation of Met, Akt and STAT3, thereby blocking related signaling pathways. STA-1474 sodium induces apoptosis and inhibits proliferation of osteosarcoma cells, and triggers the up-regulation of HSP70 and HSP90. STA-1474 sodium induces tumor regression and caspase-3 activation in mouse osteosarcoma xenograft models. STA-1474 sodium can be used in the research of osteosarcoma.
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FLLL12
0 ImagesCat. No.: HY-183402CAS No.: 917813-60-6Synonyms: GO-Y026FLLL12 (GO-Y026) is a curcumin analog anticancer agent. FLLL12 inhibits the phosphorylation of AKT, Bcl-2, Bid, EGFR, mTOR, FOXO1a, FOXO3a, STAT3, HER2/neu, as well as pancreatic AKT/STAT3; upregulates the expression of Bim and DR5; and activates PTPs. FLLL12 regulates downstream pathways, induces mitochondria-mediated and DR5-dependent extrinsic apoptosis, inhibits cancer cell viability, proliferation, anchorage-independent growth and migration, and exerts a synergistic effect with Doxorubicin (HY-15142A). FLLL12 can be used in research related to head and neck squamous cell carcinoma, breast cancer, prostate cancer, pancreatic cancer, lung cancer, colon cancer and colorectal cancer.
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GPA512
0 ImagesCat. No.: HY-123827CAS No.: 1808115-35-6GPA512 is an orally active STAT3 inhibitor and a prodrug of Galiellalactone (HY-125170). GPA512 inhibits the binding of STAT3 to DNA, downregulates STAT3-activated genes, and suppresses tumor growth in prostate cancer xenograft models. GPA512 is rapidly converted to Galiellalactone in plasma. GPA512 can be used in research related to castration-resistant prostate cancer.
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Madindoline A
0 ImagesCat. No.: HY-N14323CAS No.: 184877-64-3Madindoline A is an orally active gp130 antagonist with a KD of 288 μM. Madindoline A inhibits IL-6- and IL-11-induced osteoclastogenesis, suppresses IL-6-stimulated serum amyloid A protein production, inhibits bone resorption and bone loss, and also inhibits IL-6- and IL-11-dependent cell line growth, as well as IL-6-dependent Stat3 tyrosine phosphorylation. Madindoline A is applicable for the research of hormone-dependent postmenopausal osteoporosis.
