STAT5
STAT5 comprises STAT5A and STAT5B, transcription factors that regulate hematopoietic cell proliferation, differentiation, and apoptosis[1]. Mechanistically, STAT5 tyrosine phosphorylation in peripheral T cells is driven by cytokine receptor signaling rather than the T-cell receptor complex[2]. This cytokine-linked pathway supports immune regulation, lymphocyte development, and cell survival programs[3]. In disease contexts, STAT5B deficiency is associated with growth failure, immunodeficiency, and severe pulmonary disease[4]. Compared with STAT5A, STAT5B shows dominant activity in effector and regulatory T-cell responses, with paralog dose explaining much functional specificity[5]. In BCR/ABL leukemia models, STAT5B, but not STAT5A, serves as the major STAT5 isoform driving leukemogenesis[6]. For experimental applications, AC-4-130 directly binds STAT5 and disrupts activation, dimerization, nuclear translocation, and STAT5-dependent transcription in AML models[7]. Pimozide also decreases survival of chronic myelogenous leukemia cells resistant to kinase inhibitors[8].
References:
- [1]. Nosaka T, et al. STAT5 as a molecular regulator of proliferation, differentiation and apoptosis in hematopoietic cells. EMBO J. 1999 Sep 1;18(17):4754-65. [Content Brief]
- [2]. Moriggl R, et al. Stat5 activation is uniquely associated with cytokine signaling in peripheral T cells. Immunity. 1999 Aug;11(2):225-30. [Content Brief]
- [3]. Smith MR, et al. STAT5b: A master regulator of key biological pathways. Front Immunol. 2023 Jan 23;13:1025373. [Content Brief]
- [4]. Nadeau K, et al. STAT5b deficiency: an unsuspected cause of growth failure, immunodeficiency, and severe pulmonary disease. J Pediatr. 2011 May;158(5):701-8. [Content Brief]
- [5]. Villarino A, et al. Signal transducer and activator of transcription 5 (STAT5) paralog dose governs T cell effector and regulatory functions. Elife. 2016 Mar 21;5:e08384. [Content Brief]
- [6]. Kollmann S, et al. Twins with different personalities: STAT5B-but not STAT5A-has a key role in BCR/ABL-induced leukemia. Leukemia. 2019 Jul;33(7):1583-1597. [Content Brief]
- [7]. Wingelhofer B, et al. Pharmacologic inhibition of STAT5 in acute myeloid leukemia. Leukemia. 2018 May;32(5):1135-1146. [Content Brief]
- [8]. Nelson EA, et al. The STAT5 inhibitor pimozide decreases survival of chronic myelogenous leukemia cells resistant to kinase inhibitors. Blood. 2011 Mar 24;117(12):3421-9. [Content Brief]
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STAT5 Related Products (70)
Related Products (70)
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Antibodies (5)
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AS2863619 free base
0 ImagesAS2863619 free base is an orally active CDK8/19 inhibitor that also inhibits BMP2, MDA5 and RIG-I receptors. AS2863619 free base targets Stat5a-CDK8/19 to promote the differentiation of CD4+ T cells into regulatory T cells and induce FOXP3 expression, thereby restoring immune homeostasis and establishing transplant immune tolerance. AS2863619 free base also enhances the BMP2/SMAD signaling pathway to promote osteogenic differentiation and inhibit adipogenic differentiation. AS2863619 free base exerts osteoprotective effects by alleviating inflammation-induced impairment of osteogenic function and inducing neutrophil apoptosis (apoptosis). AS2863619 free base can be applied to research in related fields such as periodontitis-induced bone defects.
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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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GSK2618960
0 ImagesCat. No.: HY-P991424GSK2618960 is a human monoclonal antibody (mAb) targeting IL-7Ra/CD127. GSK2618960 inhibits IL-7-induced STAT5 phosphorylation. GSK2618960 enhances CD4 T cell proliferation response and increases CD83, CD86, and CD209 expression in PBMCs. GSK2618960 can be used for the research of autoimmune and allergic inflammatory diseases. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001).
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HODHBt
0 ImagesSynonyms: HOOBtHODHBt (HOOBt) inhibits STAT5-SUMO interaction by blocking SUMOylation of phosphorylated STAT5. HODHBt enhances the magnitude of IL-15 signaling and significantly increases the natural killer (NK) cell cytotoxicity phenotype and function and the generation of cytokine-induced memory-like (CIML) natural killer (NK) cells. HODHBt can be used for research of HIV-infection and cancer.
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QL-1200186
0 ImagesQL-1200186 is a selective, orally active, allosteric inhibitor targeting the tyrosine kinase TYK2 pseudokinase domain JH2 (IC50=0.06 nM, TYK2 JH2), with 164-fold selectivity over TYK1 JH2 (IC50=9.85 nM，TYK1 JH2). QL-1200186 first stabilizes the TYK2 JH2 conformation, inhibits the activity of the JH1 catalytic domain, and blocks the IFNα, IL-12/IL-23-mediated JAK-STAT signaling pathway. QL-1200186 can inhibit the production of Th1/Th17 cell-related cytokines (such as IFNγ, IL-23), reduce immune cell activation, and has no significant effect on JAK1/2/3 kinase activity. QL-1200186 can significantly improve skin inflammation in the Imiquimod (HY-B0180)-induced psoriasis mouse model and reduce the Psoriasis Area and Severity Index (PASI) score. QL-1200186 can be used in the study of autoimmune diseases such as psoriasis and systemic lupus erythematosus (SLE).
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Ibrutinib-MPEA
0 ImagesIbrutinib-MPEA is an orally active, blood-brain barrier permeable inhibitor of BTK and STAT5. As a derivative of Ibrutinib (HY-10997) conjugated with a PROTAC linker, Ibrutinib-MPEA allows the synthesis of a series of PROTAC molecules. Ibrutinib-MPEA significantly reduces the proliferation of neoplastic mast cells and primary mastocytoma cells by inducing apoptosis and inhibiting IgE-dependent histamine release. Ibrutinib-MPEA is applicable to the research of canine mast cell tumors, cerebral ischemia/reperfusion injury in diabetic mice, and neuroinflammation-related diseases.
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Ritlecitinib tosylate
0 ImagesSynonyms: PF-06651600 tosylateRitlecitinib (PF-06651600) tosylate 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 tosylate 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 tosylate 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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Patiromer
0 ImagesCat. No.: HY-112961CAS No.: 1208912-84-8Patiromer is an orally active, selective and non-absorbable intestinal potassium (K+) polymer binder that reversibly binds potassium ions in exchange for calcium (Ca2+). Patiromer can rapidly and continuously reduce serum potassium levels, maintain a normal blood potassium state, and reduce serum aldosterone levels. Patiromer also increases fecal potassium excretion. Patiromer is mainly used in the study of hyperkalemia associated with diseases such as chronic kidney disease, diabetes, and heart failure, and is particularly suitable for improving renin-angiotensin-aldosterone system inhibitor (RAASi) therapy.
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CT1113
0 ImagesCT1113 is a selective, orally active USP25/USP28 inhibitor. CT1113 inhibits cancer cell proliferation, induces apoptosis, and causes G2/S phase cell cycle arrest. CT1113 reduces the levels of total BCR-ABL1, phosphorylated BCR-ABL1, total STAT5, and phosphorylated STAT5, but does not alter the mRNA level of BCR-ABL1. CT1113 is applicable to research related to pancreatic cancer, colon cancer, and acute leukemia.
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UC-514321
0 ImagesUC-514321, a structural analog of NSC370284 with higher activity, directly targets STAT3/5 and represses TET1 expression, but not TET2 or TET3. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity.
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XOMA-213
0 ImagesCat. No.: HY-P991358Purity: 98.46%Synonyms: LFA-102; X213XOMA-213 (LFA-102; X213) is a human monoclonal antibody (mAb) targeting the prolactin receptor (PRLR), with a Kd value of 2 nM against the human target. XOMA-213 blocks PRL-induced cell proliferation and inhibits the activation of multiple PRLR ligands, including PRL and human growth hormone (hGH). XOMA-213 suppresses PRL-induced phosphorylation of Stat5, Akt and ERK1/2 in cells. XOMA-213 induces tumor regression, delays disease progression, and inhibits PRLR signaling as well as tumor growth. XOMA-213 can be used in research related to breast cancer.
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Pimozide-d4
0 ImagesSynonyms: R6238-d4Pimozide-d4 is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
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PF15 TFA
0 ImagesCat. No.: HY-143286APurity: 99.34%PF15 TFA is an orally active FLT3-ITD PROTAC degrader with a DC50 of 76.7 nM and an IC50 of 36 nM against FLT3-ITD. PF15 TFA induces FLT3-ITD protein degradation, thereby downregulating its phosphorylation level. PF15 TFA inhibits the proliferation of FLT3-ITD-positive cells and reduces the phosphorylation level of STAT5, a downstream molecule of FLT3-ITD. PF15 TFA exhibits efficacy in in vivo xenograft models of acute myeloid leukemia and prolongs survival. PF15 TFA can be used for the research of acute myeloid leukemia.
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Stafia-1-dipivaloyloxymethyl ester
0 ImagesCat. No.: HY-136568CAS No.: 2582755-72-2Stafia-1-dipivaloyloxymethyl ester (compound 27, 0-200 μM) decreases pSTAT5a expression significantly, and has no obvious inhibition on pSTAT5b.
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IMC-EB10
0 ImagesCat. No.: HY-P991641Purity: 98%Synonyms: LY3012218IMC-EB10 (LY3012218) is an anti-FLT3 monoclonal antibody. IMC-EB10 binds to FLT3 with high affinity (Kd = 158 pM) and blocks the binding of FLT3 ligand to FLT3 (IC50 ≈ 10 nM), thereby inhibiting MAPK, STAT5, and PI3K/Akt signaling in leukemia cells. IMC-EB10 can enhance the anti-leukemic effect of Methotrexate (HY-14519) and inhibit leukemias expressing wild-type or ITD-mutated FLT3 receptors. IMC-EB10 prolongs the survival of acute lymphoblastic leukemia (ALL) cells and primary leukemia samples and reduces engraftment in non-obese diabetic/severe combined immunodeficiency patients. IMC-EB10 is indicated for leukemia research.
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TAVO101
0 ImagesCat. No.: HY-P992474TAVO101 is a humanized anti-TSLP antibody with an EC50 of 0.19 nM against hTSLP. TAVO101 inhibits STAT5 activation and CCL17 release. TAVO101 carries Fc region mutations that enhance its binding to FcRn while reducing its binding to FcγRI, FcγRIIIA and C1q, thereby attenuating effector functions. TAVO101 reduces the levels of inflammatory markers, cell infiltration and histopathological damage in preclinical models of asthma, psoriasis and atopic dermatitis. TAVO101 can be used for research related to asthma, psoriasis and atopic dermatitis.
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Ritlecitinib malonate
0 ImagesCat. No.: HY-100754ACAS No.: 2140301-97-7Synonyms: PF-06651600 malonateRitlecitinib (PF-06651600) malonate 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 malonate 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 malonate 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).
