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 Agonist
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STAT3 Antagonist
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STAT3 Activators
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STAT3 Modulators
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STAT3 Inducer
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STAT3 Degraders
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STAT3 Ligands
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STAT3 Related Products (319)
Related Products (319)
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Antibodies (5)
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NSC-368262
0 ImagesCat. No.: HY-120031CAS No.: 299421-08-2NSC-368262 is a STAT3 inhibitor. NSC-368262 selectively alkylates and covalently modifies STAT3 Cys468 at the DNA-binding interface of STAT3, blocks the DNA-binding activity of STAT3, and inhibits the phosphorylation of STAT3. NSC-368262 blocks the accumulation of activated STAT3 in the nucleus of cancer cells, induces PARP cleavage and apoptosis in cells, and inhibits tumor growth in mouse models. NSC-368262 can be used in research related to breast cancer and cervical cancer.
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XD2-149
0 ImagesCat. No.: HY-159570CAS No.: 2710221-08-0XD2-149 is a ZFP91 PROTAC degrader with DC50 values of 0.08 μM and 0.06 μM, respectively. ZFP91 is a bifunctional nuclear protein with both transcription factor and E3 ubiquitin ligase activities, and is classified as an oncogenic non-canonical NF-κB pathway regulator in tumor and immune regulation. XD2-149 induces proteasome-dependent degradation of the E3 ubiquitin-protein ligase ZFP91. XD2-149 inhibits the STAT3 signaling pathway in pancreatic cancer cells and induces NQO1-dependent cell death independent of ZFP91 degradation. XD2-149 can be used for the research of pancreatic cancer.
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SC-60
0 ImagesCat. No.: HY-W717425CAS No.: 1421677-31-7SC-60 is a derivative of Sorafenib (HY-10201). SC-60 exerts its anti-tumor effect by activating the phosphatase activity of SHP-1, thereby inhibiting the STAT3 signaling pathway. SC-60 exhibits strong proliferation inhibitory activity in various hepatocellular carcinoma (HCC) cell lines. SC-60 downregulates the expression of downstream anti-apoptotic proteins (such as Bcl-2, Cyclin D1, Survivin), ultimately inducing caspase-dependent apoptosis. SC-60 significantly inhibits tumor growth in xenograft tumor models. SC-60 can be used for the study of HCC.
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STAT3-IN-32
0 ImagesCat. No.: HY-164445CAS No.: 2591440-71-8STAT3-IN-32 is an orally active, selective STAT3 SH2 domain inhibitor with a Kd of 21.3 nM, showing selectivity over STAT1/5. STAT3-IN-32 binds to the STAT3 SH2 domain, blocks Tyr705 and Ser727 phosphorylation, abrogates nuclear transcription and mitochondrial oxidative phosphorylation functions. STAT3-IN-32 inhibits tumor growth in mouse pancreatic cancer xenograft models. STAT3-IN-32 can be used for the research of pancreatic cancer.
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STAT3-IN-43
0 ImagesCat. No.: HY-174386CAS No.: 2761657-21-8
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PDGFRA/CAIX/XII-IN-1
0 ImagesCat. No.: HY-181587Purity: 98.10%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.
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MMP-2/9-IN-2
0 ImagesCat. No.: HY-180117MMP-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.
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JAK2-IN-9
0 ImagesCat. No.: HY-155746CAS No.: 2568842-26-0JAK2-IN-9 is an orally active selective JAK2 inhibitor with a human IC50 of 5 nM. JAK2-IN-9 inhibits JAK2 kinase activity, blocks JAK2 phosphorylation, and suppresses the activation of the downstream JAK2-STAT signaling pathway. JAK2-IN-9 inhibits the phosphorylation of STAT3, STAT5 and AKT in cancer cells. JAK2-IN-9 induces cancer cell apoptosis (apoptosis) and cell cycle arrest. JAK2-IN-9 can be used for the research of myeloproliferative neoplasms.
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PROTAC ALK degrader-3
0 ImagesCat. No.: HY-168551PROTAC ALK degrader-3 is an orally active ALK PROTAC degrader with a DC50 of 119.33 nM in Karpas 299 cells. PROTAC ALK degrader-3 induces the degradation of ALK fusion proteins via the ubiquitin-proteasome system. PROTAC ALK degrader-3 induces NPM-ALK degradation and inhibits the expression of p-ALK and p-STAT3. PROTAC ALK degrader-3 inhibits cancer cell proliferation and suppresses the growth of xenografts in vivo. PROTAC ALK degrader-3 can be used for the research of ALK-positive cancers (e.g., anaplastic large cell lymphoma).
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PROTAC RET Degrader 2
0 ImagesCat. No.: HY-183783PROTAC RET Degrader 2 is a RET degrader with a target IC50 of 0.36 nM. PROTAC RET Degrader 2 is mainly composed of RET-IN-34 (HY-183729) and Thalidomide (HY-14658). PROTAC RET Degrader 2 mediates RET degradation via the ubiquitin-proteasome system. PROTAC RET Degrader 2 induces apoptosis, inhibits colony-forming ability, and exhibits antiproliferative activity in cancer cells. PROTAC RET Degrader 2 suppresses tumor growth in xenograft models. PROTAC RET Degrader 2 can be used in research related to medullary thyroid carcinoma, papillary thyroid carcinoma, and RET fusion-positive lung adenocarcinoma.
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STAT3/CAIX-IN-1
0 ImagesCat. No.: HY-174457CAS No.: 3053583-60-8STAT3/CAIX-IN-1 is a dual-target inhibitor of STAT3 (Kd: 60.03 μM) and CAIX (IC50: 80.45 nM). STAT3/CAIX-IN-1 induces ferroptosis by increases the levels of reactive oxygen species (ROS) and lipid peroxides. STAT3/CAIX-IN-1 inhibits cell migration, induces apoptosis, and causes cell cycle arrest in MDA-MB-231 cells. STAT3/CAIX-IN-1 can be used for the study of triple-negative breast cancer (TNBC).
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SHN7
0 ImagesCat. No.: HY-184706CAS No.: 3126116-06-8SHN7 is a selective HDAC1/HDAC6 inhibitor, NQO1 substrate and ROS inducer, with an IC50 of 30 nM against HDAC1 and an IC50 of 10 nM against HDAC6. SHN7 inhibits STAT3 with a Kd of 8.9 μM. SHN7 arrests the cell cycle at the G2/M phase and induces Apoptosis. SHN7 exhibits anti-tumor effects in triple-negative breast cancer (TNBC) xenograft models. SHN7 can be used for the research of triple-negative breast cancer.
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NTZ-24
0 ImagesCat. No.: HY-182510CAS No.: 69819-42-7NTZ-24 is a selective STAT3 pathway inhibitor. NTZ-24 suppresses STAT3 phosphorylation at Tyr705, blocks STAT3-DNA interaction, and downregulates the levels of STAT3 downstream target proteins. NTZ-24 induces cell-cycle arrest and promotes apoptosis in cancer cells. NTZ-24 exerts significant antiproliferative activity against HeLa cells (IC50 = 3.3 μM). NTZ-24 can be used for the research of cervical cancer.
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STAT3-IN-53
0 ImagesCat. No.: HY-181514CAS No.: 3113051-34-3STAT3-IN-53 (Compound L20) is a STAT3 inhibitor with a Kd value of 6.16 μM. STAT3-IN-53 binds directly to the SH2 domain of STAT3, inhibits phosphorylation at the Y705 site without affecting the total STAT3 protein level, and suppresses the IL-6/JAK/STAT3 pathway. STAT3-IN-53 downregulates the transcription and expression of cyclin-D1 and c-Myc. STAT3-IN-53 induces cell cycle arrest and promotes Apoptosis. STAT3-IN-53 exhibits anticancer activity against colorectal cancer.
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PROTAC STAT3 degrader-2
0 ImagesCat. No.: HY-153023CAS No.: 2429877-78-9PROTAC STAT3 degrader-2 is a selective and efficacious PROTAC degrader of STAT3 protein with a DC50 of 3.54 μM in Molm-16 Cell. PROTAC STAT3 degrader-2 has the potential for cancer research. PROTAC STAT3 degrader-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
