JAK3
Janus kinase 3 (JAK3) is a non-receptor tyrosine kinase of the JAK family that mediates cytokine receptor signaling and transduces extracellular immune signals through the JAK/STAT signaling pathway[1]. JAK3 functions downstream of cytokine receptors and participates in receptor-associated signaling events that regulate immune cell development, activation, and homeostasis through STAT phosphorylation and transcriptional regulation[1][2]. Mechanistically, cytokine-induced receptor dimerization activates JAK proteins, leading to receptor phosphorylation, STAT recruitment, STAT activation, and subsequent regulation of target gene expression involved in immunity and inflammatory responses[2][3]. In disease contexts, dysregulated JAK/STAT signaling is associated with immune-mediated disorders and inflammatory diseases, making JAK family members important therapeutic targets for pathway modulation[2][3]. Compared with the broadly expressed isoforms JAK1, JAK2, and TYK2, JAK3 exhibits a more restricted expression pattern and is primarily produced in hematopoietic and lymphoid cells, providing a key biological distinction among JAK family members[2][3]. This lineage-associated distribution links JAK3 more closely to adaptive immune regulation and supports its relevance in immune system research models[3]. For experimental applications, JAK3 has attracted substantial interest as a drug target because selective inhibition of cytokine-triggered JAK/STAT signaling can modulate immune responses while exploiting the relatively restricted cellular distribution of this isoform[3][4]. Consequently, the development of selective JAK3 inhibitors continues to provide valuable tools for investigating cytokine signaling mechanisms and immune-related disease biology[3][4].
References:
- [1]. Kawamura M, et al. Molecular cloning of L-JAK, a Janus family protein-tyrosine kinase expressed in natural killer cells and activated leukocytes. Proc Natl Acad Sci U S A. 1994 Jul 5;91(14):6374-8. [Content Brief]
- [2]. Hu X, et al. The JAK/STAT signaling pathway: from bench to clinic. Signal Transduct Target Ther. 2021 Nov 26;6(1):402. [Content Brief]
- [3]. Kwon S. Molecular dissection of Janus kinases as drug targets for inflammatory diseases. Front Immunol. 2022 Dec 8;13:1075192. doi: 10.3389/fimmu.2022.1075192. PMID: 36569926; PMCID: PMC9773558. et al. Molecular dissection of Janus kinases as drug targets for inflammatory diseases. Front Immunol. 2022 Dec 8;13:1075192. [Content Brief]
- [4]. Chen C, et al. A highly selective JAK3 inhibitor is developed for treating rheumatoid arthritis by suppressing γc cytokine-related JAK-STAT signal. Sci Adv. 2022 Aug 19;8(33):eabo4363. [Content Brief]
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JAK3 Related Products (156)
Related Products (156)
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JAK-IN-38
0 ImagesCat. No.: HY-162862JAK-IN-38 (Compound 1) is a JAK inhibitor, with IC50s of 0.03, 0.06, 0.12, 0.44 μM for Tyk2, JAK3, JAK2, JAK1 respectively. JAK-IN-38 is a collagen VII (C7) inducer and has anti-inflammatory activity. JAK-IN-38 can upregulate the expression of COL7A1 mRNA in donor-derived keratinocytes and works together with Gentamicin (HY-A0276A) to boost overall C7 levels.
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Tofacitinib hydrochloride
0 ImagesCat. No.: HY-40354HCAS No.: 1803005-18-6Synonyms: Tasocitinib hydrochloride; CP-690550 hydrochlorideTofacitinib hydrochloride (Tasocitinib hydrochloride) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib hydrochloride blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib hydrochloride can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.
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JAK1/3-IN-1
0 ImagesCat. No.: HY-123939CAS No.: 1400687-19-5JAK1/3-IN-1 is a selective, orally active JAK1/3 inhibitor with IC50 values of 1.9 nM and 0.9 nM, respectively. JAK1/3-IN-1 significantly reduces the mean arterial blood pressure and significantly increases the heart rate in rabbits. JAK1/3-IN-1 decreases the mean arterial blood pressure in conscious telemetered rats and induces lethal cardiovascular effects.
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Tofacitinib-13C
0 ImagesCat. No.: HY-40354S3Synonyms: Tasocitinib-13C; CP-690550-13CTofacitinib-13C (Tasocitinib-13C; CP-690550-13C) is the 13C-labeled Tofacitinib (HY-40354). Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.
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Tofacitinib-d3
0 ImagesCat. No.: HY-40354S5Synonyms: Tasocitinib-d3; CP-690550-d3Tofacitinib-d3 (Tasocitinib-d3; CP-690550-d3) is the deuterated-labeled Tofacitinib (HY-40354). Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.
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Flonoltinib monomaleate
0 ImagesCat. No.: HY-130247BCAS No.: 3062214-21-2Synonyms: JAK2/FLT3-IN-1 monomaleate
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Momelotinib mesylate
0 ImagesCat. No.: HY-10963CAS No.: 1056636-07-7Synonyms: CYT387 mesylateMomelotinib mesylate (CYT387 mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.
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ZM39923
0 ImagesCat. No.: HY-12589ACAS No.: 273727-89-2ZM39923 is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM.
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CT 2576
0 ImagesCat. No.: HY-187609CAS No.: 166981-11-9CT 2576 is a phospholipid signaling inhibitor as well as a Jak3/STAT5 inhibitor. CT 2576 suppresses gene expression and replication of human immunodeficiency virus (HIV) at the post-transcriptional level by interfering with phospholipid metabolism in host cells, particularly by inhibiting the production of phosphatidic acid PA. CT-2576 completely inhibits the growth and proliferation of malignant T-cell lymphoma cells by suppressing phospholipid signaling and blocking the Jak/STAT signaling pathway associated with IL-2R. CT 2576 can be used in research related to human immunodeficiency virus (HIV) infection and cutaneous T-cell lymphoma (CTCL).
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JAK3-IN-19
0 ImagesCat. No.: HY-180512CAS No.: 2478991-58-9
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NSC114792
0 ImagesCat. No.: HY-122101CAS No.: 17392-79-9
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AS2553627
0 ImagesCat. No.: HY-123187CAS No.: 1251906-10-1AS2553627 is a type of JAK inhibitor, with IC50 values of 0.46, 0.30, 0.14, and 2.0 nM for JAK1, JAK2, JAK3 and TYK2, respectively. AS2553627 can inhibit the proliferation of human and rat T cells stimulated by IL-2, with IC50 values of 2.4 and 4.3 nM, respectively. AS2553627 can reduce cardiac allograft vasculopathy and fibrosis in a rat heart transplant model, effectively extending survival rates. AS2553627 can be used to prevent acute and chronic rejection in heart transplants.
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JAK3-IN-7
0 ImagesCat. No.: HY-U00390CAS No.: 1263774-57-7JAK3-IN-7 is a potent and selective JAK3 inhibitor extracted from patent WO2011013785A1, has an IC50 of <0.01 μM.
