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-23
0 ImagesJAK-IN-23 is an orally active double inhibitor of JAK/STAT and NF-κB. JAK-IN-23 can inhibit JAK1/2/3 with IC50 values of 8.9 nM, 15 nM and 46.2 nM, respectively. JAK-IN-23 has potent inhibitory activities against interferon-stimulated genes (ISG) and NF-κB pathways with IC50 values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 has great anti-inflammatory that decreases the release of various proinflammatory factors. JAK-IN-23 can be used for the research of inflammatory bowel disease (IBD).
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ZM39923 hydrochloride
0 ImagesZM39923 hydrochloride is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 hydrochloride also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM.
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Envudeucitinibum
0 ImagesSynonyms: Envudeucitinib; ESK-001Envudeucitinibum (Envudeucitinib) is a highly selective, allosteric and orally active TYK2 inhibitor binding to the JH2 domain of TYK2. Envudeucitinibum has no off-target effects on other kinases (JAK1-3). Envudeucitinibum reduces signaling and production of proinflammatory cytokines including IL-12, IL-23, IL-17, and type I interferons (IFNs). Envudeucitinibum can be used for the research of plaque psoriasis, systemic lupus erythematosus (SLE), and other immune-mediated diseases.
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Filgotinib maleate
0 ImagesSynonyms: GLPG0634 maleateFilgotinib maleate (GLPG0634 maleate) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib maleate can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib maleate also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib maleate can be used in the study of rheumatoid arthritis and inflammatory bowel disease.
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Modzatinib
0 ImagesCat. No.: HY-174280CAS No.: 2411407-25-3Synonyms: ITK kinase-IN-1Modzatinib (ITK kinase-IN-1) is an oral active, selective, covalent ITK/JAK3 dual-target inhibitor with IC50 values of 8 nM and 23 nM, respectively. Modzatinib exhibits anti-inflammatory activity and can be used in the research of autoimmune and inflammatory diseases.
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Tofacitinib-13C3
0 ImagesSynonyms: Tasocitinib-13C3; CP-690550-13C3Tofacitinib-13C3 (Tasocitinib-13C3; CP-690550-13C3) 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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Cerdulatinib hydrochloride
0 ImagesSynonyms: PRT062070 hydrochloride; PRT2070 hydrochlorideCerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC50s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies.
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JAK2-IN-7
0 ImagesJAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities.
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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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Ilginatinib hydrochloride
0 ImagesSynonyms: NS-018 hydrochloride
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BI-1622
0 ImagesBI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile.
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