STAT6
STAT6 is a cytokine-responsive transcription factor that links receptor signaling to gene regulation in immune cells[1]. Mechanistically, IL-4 and IL-13 activate STAT6, and this axis drives TH2 polarization, IL-4-dependent lymphocyte responses, and IgE class switching[1][2][3]. In disease models, STAT6 regulates pathologic lung inflammation and supports experimental analysis of allergic asthma, airway hyperresponsiveness, and atopic inflammation[4][5][6]. Compared with related STAT isoforms, STAT6 shows a distinct functional focus on IL-4/IL-13 biology, whereas STAT4 primarily controls TH1 differentiation[7]. For experimental applications, STAT6 inhibition with AS1517499 reduced antigen-induced bronchial hypercontractility and blocked STAT6 signaling in mouse atopic dermatitis-asthma models[5][6].
参考文献:
- [1]. Hebenstreit D, et al. Signaling mechanisms, interaction partners, and target genes of STAT6. Cytokine Growth Factor Rev. 2006 Jun;17(3):173-88. [Content Brief]
- [2]. Takeda K, et al. Essential role of Stat6 in IL-4 signalling. Nature. 1996 Apr 18;380(6575):627-30. [Content Brief]
- [3]. Shimoda K, et al. Lack of IL-4-induced Th2 response and IgE class switching in mice with disrupted Stat6 gene. Nature. 1996 Apr 18;380(6575):630-3. [Content Brief]
- [4]. Walford HH, et al. STAT6 and lung inflammation. JAKSTAT. 2013 Oct 1;2(4):e25301. [Content Brief]
- [5]. Chiba Y, et al. A novel STAT6 inhibitor AS1517499 ameliorates antigen-induced bronchial hypercontractility in mice. Am J Respir Cell Mol Biol. 2009 Nov;41(5):516-24. [Content Brief]
- [6]. Li X, et al. The STAT6 inhibitor AS1517499 reduces the risk of asthma in mice with 2,4-dinitrochlorobenzene-induced atopic dermatitis by blocking the STAT6 signaling pathway. Allergy Asthma Clin Immunol. 2022 Feb 17;18(1):12. [Content Brief]
- [7]. Lund RJ, et al. Kinetics and STAT4- or STAT6-mediated regulation of genes involved in lymphocyte polarization to Th1 and Th2 cells. Eur J Immunol. 2003 Apr;33(4):1105-16. [Content Brief]
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STAT6 関連製品 (47)
関連製品 (47)
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抗体 (1)
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Ritlecitinib
0 Images別名: 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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AK-1690
0 ImagesAK-1690 is a selective PROTAC degrader targeting STAT6 (DC50=1 nM) with a Ki of 6 nM against human STAT6. AK-1690 degrades STAT6 via the interaction of STAT6 with cereblon and a ubiquitin-like process. AK-1690 effectively depletes STAT6 protein in mouse liver and lung tissues, and is applicable to research related to leukemia, Hodgkin's lymphoma, follicular lymphoma, etc..
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Gamma-glutamylcysteine
0 ImagesGamma-glutamylcysteine (γ-Glu-Cys) is an orally active, blood-brain barrier permeable dipeptide. Gamma-glutamylcysteine activates AMPK, SIRT1, IL-4/STAT6, AC/cAMP/PI3K, IGF-1R/IRS1/PI3K, and Nrf2 signaling pathways; it inhibits NF-κB, JAK1/STAT1/3, MAPKs, cadmium-induced p38 MAPK, JNK, and PI3K/Akt signaling pathways. Gamma-glutamylcysteine regulates macrophage polarization, modulates the trafficking of CD36 and GLUT4, induces glutathione synthesis, improves metabolic dysfunction, reduces lipid deposition, ameliorates glucose homeostasis, inhibits apoptosis (Apoptosis), stabilizes mitochondria, suppresses lipid peroxidation, iron accumulation and ferroptosis (Ferroptosis), reduces ds-HMGB1 levels, reverses mechanical hyperalgesia, and alleviates hepatic lipid droplet formation. Gamma-glutamylcysteine is applicable to research related to inflammatory bowel disease, type 2 diabetes, cadmium-induced neurotoxicity, Alzheimer's disease, cerebral ischemia/reperfusion injury, neuropathy, and alcoholic liver disease.
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Stapokibart
0 Images別名: CM310Stapokibart (CM310) is a humanized monoclonal antibody targeting IL-4Rα (KD values of 0.25 nM, 1.50 nM, and 2.75 nM for human, cynomolgus monkey, and rat IL-4Rα, respectively). Stapokibart effectively blocks the interaction of cytokines IL-4 and IL-13 with their co-receptor subunit IL-4Rα. Stapokibart reduces IL-4 and IL-13 mRNA, inhibits CD23 upregulation, and inhibits IL-4 and IL-13-induced STAT6 activation. Stapokibart improves inflammation (airway inflammation, rhinitis, dermatitis).
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BP79
0 Images製品番号: HY-206870CAS 番号: 3104965-33-2BP79 is a potent TSLP receptor inhibitor. BP79 disrupts TSLP-mediated ternary complex formation, blocks TSLPR-IL7Rα co-localization, binds and stabilizes TSLPR, and inhibits phosphorylated STAT3/6. BP79 suppresses immune cell infiltration, secretion of IL-13, IL-4. BP79 can be used for the research of inflammation diseases, such as atopic dermatitis, allergic asthma, and allergic rhinitis.
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YYSW001
0 Images製品番号: HY-182359CAS 番号: 2763672-36-0YYSW001 is a selective and orally acrive JAK1 inhibitor with an IC50 of 6 nM and a Kd of 32.32 μM. YYSW001 blocks JAK1-dependent phosphorylation of STAT6, as well as IL-6-induced phosphorylation of STAT3. YYSW001 suppresses pro-inflammatory cytokine levels, reduces paw swelling, lowers clinical arthritis scores, alleviates joint damage and decreases bone loss. YYSW001 is applicable for the research of rheumatoid arthritis.
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YM-341619
0 Images別名: AS1617612YM-341619 (AS1617612) is a potent and orally active STAT6 inhibitor with an IC50 of 0.70 nM. YM-341619 inhibits Th2 differentiation in mouse spleen T cells induced by IL-4 (IC50=0.28 nM) without affecting Th1 cell differentiation. YM-341619 is a promising compound for the the research of allergic diseases, such as allergic asthma.
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Medrysone
0 ImagesMedrysone (HMS; 6α-Methyl-11β-hydroxyprogesterone) is a STAT6 modulator and M2 macrophage polarization inducer. Medrysone enhances IL-4-triggered STAT6 activation, upregulates the expression of M2 markers, and promotes the secretion of VEGF and CCL2. Medrysone also enhances the pro-migratory activity of M2-like macrophages toward endothelial cells. By regulating macrophage polarization and related repair pathways, Medrysone significantly promotes corneal wound repair in a rat mechanical injury model. Medrysone can be used for research related to corneal injury.
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Rademikibart
0 Images別名: CBP-201Rademikibart (CBP-201) is a human monoclonal antibody targeting IL-4Rα and IL-4Rα inhibitor with a KD of 20.7 pM when binding to human IL-4Rα epitopes. Rademikibart does not bind to IL-4Rα from other species. Rademikibart inhibits IL-4 and IL-13-mediated STAT6 signaling, TF-1 cell proliferation and thymus activation regulated chemokine (TRAC) production. Rademikibart can be used for the research of atopic dermatitis and asthma.
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SD-436
0 ImagesSD-436 is a highly selective and efficacious STAT3 PROTAC degrader (DC50: 0.5 μM), with IC50 of 19 nM (STAT3), 270 nM (STAT1), 360 nM (STAT4), >10 μM (STAT5) and >10 μM (STAT6). SD-436 promotes ubiquitination and degradation of STAT3, and induces tumor regression. SD-436 can be used for tumor research, such as leukemia and lymphoma.
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UNC1062
0 ImagesUNC1062 is a highly selective tyrosine kinase (MERTK) inhibitor with an IC50 of 1.1 nM (Morrison Ki = 0.33 nM). UNC1062 exhibits good selectivity for the TAM family (TYRO3 IC50 = 60 nM, AXL IC50 = 85 nM). UNC1062 exhibits significant anti-proliferative effects and induces apoptosis in various cancer models (such as melanoma, gastric cancer, and acute myeloid leukemia). UNC1062 inhibits multiple pathways, including MAPK/ERK, PI3K/AKT and JAK/STAT and affects the motility of head and neck squamous cell carcinoma (HNSCC) cells through the RhoA signaling pathway. UNC1062 inhibits macrophage efferocytosis, and it suitable for research on atherosclerosis.
