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 (327)
Related Products (327)
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Antibodies (5)
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Zoniporide hydrochloride
0 ImagesCat. No.: HY-105064BCAS No.: 241800-97-5Synonyms: CP-597396 hydrochlorideZoniporide hydrochloride (CP-597396 hydrochloride) is a selective Na+/H+ exchanger subtype 1 (NHE1) inhibitor with cardioprotective activity, with IC50 values of 67 nM and 73 nM against rat NHE1. Zoniporide hydrochloride reduces intracellular Na+ and Ca2+ overload, preserves mitochondrial integrity, activates pro-survival ERK1/2 and STAT3 signaling pathways, reduces necrosis and apoptosis, and decreases neutrophil aggregation. Zoniporide hydrochloride is applicable to research related to myocardial ischemia-reperfusion injury and heart graft ischemia-reperfusion injury.
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STAT3-IN-49
0 ImagesCat. No.: HY-179468STAT3-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.
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Avicin D
0 ImagesCat. No.: HY-N13338CAS No.: 197787-20-5Avicin D is a plant triterpenoid. Avicin D induces Autophagy by activation of AMPK. Avicin D inhibits mTOR and S6 kinase activity. Avicin D selectively induces Apoptosis and downregulates p-STAT-3, bcl-2, and Survivin. Avicin D has properties of being a selective Glucocorticoid receptor modulator. Avicin D inhibits NF-κB activation. Avicin D shows anti-tumor effects against cutaneous T-cell lymphomas.
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P-gp-IN-36
0 ImagesCat. No.: HY-181773P-gp-IN-36 is a potent P-glycoprotein (P-gp) inhibitor with an EC50 of approximately 1 μM. P-gp-IN-36 inhibits the efflux function of P-glycoprotein, overcoming P-gp-mediated multidrug resistance in cancer cells. P-gp-IN-36 inhibits STAT3 phosphorylation and reduces total STAT3 expression. P-gp-IN-36 sensitizes P-gp-expressing cancer cells to the cytostatic effects of conventional cytostatic drugs. P-gp-IN-36 can be used for the research of multidrug-resistant cancer.
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8α-Tigloyloxyhirsutinolide 13-O-acetate
0 ImagesCat. No.: HY-138071CAS No.: 83182-58-5Synonyms: 8αTGH8α-Tigloyloxyhirsutinolide 13-O-acetate (8αTGH) is a potent and orally active STAT3 inhibitor. 8α-Tigloyloxyhirsutinolide 13-O-acetate induces early oxidative stress and pyroptosis, and late DNA damage, cell cycle arrest, apoptosis in the TNBC cells. 8α-Tigloyloxyhirsutinolide 13-O-acetate suppresses tumor cell growth in vitro and tumor growth in vivo.
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(-)-Salcolin B
0 ImagesCat. No.: HY-N21550CAS No.: 1292294-32-6Synonyms: Tricin 4'-O-(threo-β-guaiacylglyceryl)ether(-)-Salcolin B (Tricin 4'-O-(threo-β-guaiacylglyceryl) ether) is an isomer of Salcolin B (HY-N16766) and anti-inflammatory agent. (-)-Salcolin B is isolable from Njavara. (-)-Salcolin B downregulates the activities of NF-κB and STAT3, reduces the expressions of iNOS and COX-2, activates the ERK signaling pathway, and inhibits LPS-induced NO and ROS production. (-)-Salcolin B induces Apoptosis. (-)-Salcolin B inhibits TPA (HY-18739)-induced ear edema. (-)-Salcolin B possesses antioxidant activity. (-)-Salcolin B can be used in research related to inflammatory diseases, colon adenocarcinoma, ovarian cancer and breast cancer.
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KB-0118
0 ImagesCat. No.: HY-176535CAS No.: 2648377-08-4Synonyms: BBC0115KB-0118 (BBC0115) is an orally active BET bromodomain inhibitor. KB-0118 selective binds to BRD2 and BRD4 over BRD3, with Kd values of 36.7 μM for BRD2 BD1 and 47.4 μM for BRD4 BD1. KB-0118 inhibits pro-inflammatory cytokines, including TNF, IL-1β, and IL-23a and selectively suppresses Th17 cell differentiation. KB-0118 modulates Th17-driven inflammation occurs through epigenetic suppression of BRD4, confirmed by downregulation of STAT3 and BRD4 target genes. KB-0118 has immunomodulatory effects in inflammatory bowel disease (IBD) model.
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G721-0282
0 ImagesG721-0282 is an orally active CHI3L1 inhibitor. G721-0282 can reduce the expression of inflammatory proteins and cytokines. G721-0282 inhibits the activation of the NF-κB signaling pathway. G721-0282 inhibits neuroinflammation and reduces anxious behavior. G721-0282 significantly inhibits the proliferation of osteosarcoma (OS) cells by suppressing the STAT3 signaling pathway. G721-0282 induces OS cell apoptosis by upregulating pro-apoptotic protein levels and downregulating anti-apoptotic protein levels. G721-0282 can be used for researches on neuroinflammatory conditions and cancer.
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WR-S-462
0 ImagesCat. No.: HY-170946WR-S-462 is a STAT3 inhibitor. WR-S-462 effectively suppresses STAT3 phosphorylation and biological functions in vitro. WR-S-462 inhibits MDA-MB-231 cells with an IC50 of 0.03 μM. WR-S-462 displays a strong binding affinity towards the STAT3 protein with a Kd of 58 nM. WR-S-462 inhibits the nuclear translocation of p-STAT3, selectively inhibits the expression of p-STAT3Tyr705 and downstream target genes regulated by STAT3 in MDA-MB-231 cells such as Cyclin D1, Bcl-2, and Bcl-xl. WR-S-462 inhibits TNBC (triple-negative breast cancer) growth and metastasis.
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EC-70124
0 ImagesCat. No.: HY-124067CAS No.: 1185908-92-2EC-70124 is an orally active multikinase inhibitor targeting IKKβ and JAK2. EC-70124 blocks IkB phosphorylation and STAT3 (Tyr705) activation, suppressing NF-κB nuclear translocation and STAT3 transcriptional activity. EC-70124 reduces tumor growth and cancer stem cell (CSC) populations in prostate cancer cells and xenograft models. EC-70124 is promising for research of prostate cancer.
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JAK1/STAT3-IN-1
0 ImagesCat. No.: HY-170977JAK1/STAT3-IN-1 (compound 4f) is an anti-AD (atopic dermatitis) agent by inhibiting JAK1/STAT3 signaling pathway. JAK1/STAT3-IN-1 inhibits NO generation with an IC50 of 2.17 μM. JAK1/STAT3-IN-1 improves the skin condition of AD-like mice, reduces inflammatory infiltration, inhibits the expressions of p-JAK1/JAK1 and p-STAT3/STAT3, and mitigates the excessive immune response on Calcipotriol (HY-10001) (MC903)-induced AD-like mice.
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Sorafenib-d3 tosylate
0 ImagesCat. No.: HY-10201S4CAS No.: 1333386-17-6Synonyms: Donafenib tosylate; Bay 43-9006-d3 tosylateSorafenib-d3 (Donafenib) tosylate is the deuterated-labeled Sorafenib tosylate (HY-10201A). Sorafenib (Bay 43-9006) tosylate 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 tosylate induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib tosylate inhibits tumor growth and metastasis in mouse and rat models. Sorafenib tosylate 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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CHI3L1-IN-4
0 ImagesCat. No.: HY-175781CAS No.: 1258696-85-3CHI3L1-IN-4 (Compound 8) is a Chitinase-3-Like Protein 1 (CHI3L1) inhibitor with a Kd of 6.8 μM. CHI3L1-IN-4 significantly reduces glioblastoma (GBM) spheroids viability and attenuates phospho-STAT3 levels by disrupting CHI3L1 pathway. CHI3L1-IN-4 can be used for GBM research.
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BRD4-IN-41
0 ImagesCat. No.: HY-115541CAS No.: 1877286-69-5BRD4-IN-41 is a BRD4 inhibitor with an IC50 of 34 nM. BRD4-IN-41 also inhibits JAK2, FLT3, RET, ROS1, NTRK3, PDGFRb, and FGFR1 kinases with IC50 values ranging from 0.9 nM to 43 nM. BRD4-IN-41 inhibits acetyl-lysine binding site of BRD4, downregulates c-MYC, reduces phosphorylated STAT3 levels, induces G1 cell cycle arrest and apoptosis, thereby inhibiting cancer cells growth. BRD4-IN-41 can be used for the research of cancer, such as multiple myeloma and acute myeloid leukemia.
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JAK1-IN-20
0 ImagesCat. No.: HY-181872CAS No.: 3106963-85-0JAK1-IN-20 (Compound 38) is a gut-restricted, orally active, selective JAK1 inhibitor with an IC50 of <0.5 nM. JAK1-IN-20 inhibits the enzymatic activity of JAK1, reduces the production of proinflammatory cytokines (TNF-α, IL-6), and suppresses the phosphorylation of STAT3. JAK1-IN-20 ameliorates ulcerative colitis. JAK1-IN-20 can be used for the research of inflammatory bowel disease.
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YN11
0 ImagesCat. No.: HY-182288CAS No.: 3118507-43-7YN11 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.
