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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MS-1020
0 ImagesCat. No.: HY-123099CAS No.: 1255516-86-9MS-1020 is a potent and ATP-competitive JAK3 inhibitor. MS-1020 inhibits JAK3/STAT signaling and induces apoptosis. MS-1020 promotes cell death. MS-1020 decreases the expression of tyrosine phosphorylated STAT3 levels. MS-1020 has the potential for the research of cancers harboring aberrant JAK3 signaling.
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Tofacitinib-13C3,15N
0 ImagesCat. No.: HY-40354S1Purity: 99.57%Synonyms: Tasocitinib-13C3,15N; CP-690550-13C3,15NTofacitinib-13C3,15N (Tasocitinib-13C3,15N; CP-690550-13C3,15N) is the 15N, 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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PJ27
0 ImagesCat. No.: HY-181663PJ27 is a dual PD-1/PD-L1/JAK1 inhibitor, with an IC50 of 414 nM against PD-1/PD-L1, an IC50 of 786 nM against JAK1, a Ka of 294 nM for human PD-1/PD-L1, and a Ka of 473 nM for murine PD-1/PD-L1. PJ27 promotes the infiltration of CD3+CD8+ and CD3+CD4+ cells into the tumor microenvironment and exerts a significant immune activation effect. PJ27 inhibits tumor growth in a dose-dependent manner in the LLC lung cancer mouse model. PJ27 is applicable to relevant research on lung cancer.
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JI6
0 ImagesCat. No.: HY-18949CAS No.: 856436-16-3JI6 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ～40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits JAK3 and c-Kit, with IC50s of ～250 and ～500 nM, respectively. JI6 can be used for the research of acute myeloid leukemia.
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JAK3-IN-18
0 ImagesCat. No.: HY-174999CAS No.: 2914873-59-7JAK3-IN-18 is an orally active JAK3 and TEC inhibitor, with IC50s of 0.5391 nM and 12.40 nM, respectively. JAK3-IN-18 demonstrates outstanding selectivity over AK1, AK2, and TYk2, with selectivity ratios exceeding 10,000-fold. JAK3-IN-18 demonstrates excellent therapeutic efficacy in the experimental autoimmune encephalomyelitis (EAE) mouse model. JAK3-IN-18 can be used for the study of multiple sclerosis.
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JNK-IN-17
0 ImagesCat. No.: HY-164111CAS No.: 1128096-58-1JNK-IN-17 (Compound 9J) is a selective and potent JNK inhibitor with IC50 values of 0.039, 0.079 μM for JNK1 and JNK3. JNK-IN-17 can inhibit c-Jun phosphorylation with an IC50 of 0.082 μM in Streptozotocin (HY-13753)-infuced INS-1 pancreatic islet β cells. JNK-IN-17 shows inhibition rate ≤ 33% on the four main P450 subtypes (2C9, 2D6, 3A4, 1A2) in human liver microsomes, indicating a relatively low risk of drug interactions. JNK-IN-17 can be used for researches of neurological and metabolic disease, such as Parkinson's disease.
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JAK/HDAC-IN-2
0 ImagesCat. No.: HY-149283CAS No.: 3029138-43-7JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers.
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JAK3/BTK-IN-6
0 ImagesCat. No.: HY-147754CAS No.: 2243136-03-8
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TK4g
0 ImagesCat. No.: HY-151258CAS No.: 2232890-86-5TK4g is a Janus kinase (JAK) inhibitor with the IC50 values of 12.61 nM and 15.80 nM for JAK2 and JAK3, respectively. TK4g can be used in lymphoid-derived diseases and leukemia cancer research.
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AUH-6-96
0 ImagesCat. No.: HY-115438CAS No.: 1005144-85-3AUH-6-96 is a JAK/STAT signaling inhibitor. AUH-6-96 reduces Unpaired-induced transcriptional activity in Drosophila cells and blocks tyrosine phosphorylation of STAT92E. AUH-6-96 blocks both constitutive and IL-6-induced phosphorylation of STAT3. AUH-6-96 decreases the level of tyrosine-phosphorylated JAK3. AUH-6-96 induces cancer cell Apoptosis by downregulating the expression of anti-apoptotic genes downstream of STAT3. AUH-6-96 selectively reduces the viability of cancer cells with abnormal JAK/STAT signaling pathway. AUH-6-96 is applicable to related research on Hodgkin's lymphoma, breast cancer, and prostate cancer.
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PRN-371
0 ImagesCat. No.: HY-124657CAS No.: 1610974-55-4PRN-371 is a potent and selective JAK3 inhibitor. PRN371 effectively suppresses natural killer/T-cell lymphoma cell proliferation and induces apoptosis through abrogation of the JAK3-STAT signaling. PRN-371 exhibits antitumor activity and can be used for the research of cancer, such as hematological malignancies.
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JAK2-IN-14
0 ImagesCat. No.: HY-175684CAS No.: 3087335-24-5JAK2-IN-14 is an orally active JAK2 inhibitor with an IC50 of 2 nM. JAK2-IN-14 demonstrates 89.5-, 80.5-, and 51-fold selectivity over JAK1, JAK3, and TYK2, respectively. JAK2-IN-14 inhibits STAT5 signaling pathway. JAK2-IN-14 causes tumor cell cycle arrest and apoptosis. JAK2-IN-14 can used for the study of myeloproliferative neoplasms (MPNs).
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LAS194046
0 ImagesCat. No.: HY-150101CAS No.: 1798578-61-6LAS194046 is a selective pan-JAK inhibitor, with an IC50 of 5.46 nM against JAK1, 0.4 nM against JAK2, and 2.07 nM against JAK3. LAS194046 reduces the levels of IL-8 and MMP-9. LAS194046 enhances the activation of glucocorticoid response elements by Fluticasone propionate. LAS194046 inhibits T2-type allergic pulmonary inflammation, allergen-induced airway inflammation, and late-phase asthmatic responses in rats. LAS194046 can be used in research related to non-T2 severe asthma, chronic obstructive pulmonary disease, and asthma.
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JAK3-IN-12
0 ImagesCat. No.: HY-147975CAS No.: 1430095-86-5JAK3-IN-12 (compound 5k) is a highly potent JAK3 inhibitor with IC50 values of 9.5 nM, 18 nM and 42 nM for JAK3, JAK1 and JAK2, respectively. JAK3-IN-12 can be used for researching rheumatoid arthritis.
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JAK1-IN-19
0 ImagesCat. No.: HY-178282CAS No.: 2169271-17-2
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JAK-IN-44
0 ImagesCat. No.: HY-188034CAS No.: 2119040-02-5JAK-IN-44 is an orally active and selective JAK2 inhibitor, with IC50 values of 0.2 nM, 7.3 nM, 21 nM and 27 nM against JAK2, TYK2, JAK1 and JAK3, respectively. JAK-IN-44 inhibits disease phenotypes in adjuvant-induced arthritis, systemic lupus erythematosus and experimental autoimmune uveitis models, and improves the survival rate of mice in LPS (HY-D1056)-induced sepsis models. JAK-IN-44 can be used in the research of autoimmune and inflammatory diseases such as systemic lupus erythematosus, uveitis, rheumatoid arthritis and sepsis.
