JAK2
JAK2 is a non-receptor tyrosine kinase in the JAK1-JAK2-JAK3-TYK2 family and acts as a cytoplasmic signaling component of cytokine receptors[1]. Mechanistically, cytokine-mediated activation of JAK2 promotes receptor phosphorylation, recruits STAT proteins, and drives STAT phosphorylation-dependent transcriptional signaling[1][2]. This pathway supports cell growth, survival, development, differentiation, hematopoiesis, immune regulation, and homeostasis[2][3]. In disease models, gain-of-function JAK2 V617F in the pseudokinase domain causes constitutive activity and is strongly linked to myeloproliferative neoplasms and leukemias[1][4]. Compared with related isoforms, JAK3 is essential for common γ-chain cytokine receptor signaling in T- and B-cell development, whereas complete mouse deletion of JAK1 or JAK2 is not compatible with life[5][6]. For experimental applications, ruxolitinib is a selective oral JAK1/JAK2 inhibitor, and JAK2-focused compounds support studies of mutant signaling, cytokine responses, splenomegaly, angiogenesis, and inhibitor resistance[7][8][9].
References:
- [1]. Hubbard SR. Mechanistic Insights into Regulation of JAK2 Tyrosine Kinase. Front Endocrinol (Lausanne). 2018 Jan 5;8:361. doi: 10.3389/fendo.2017.00361. PMID: 29379470; PMCID: PMC5770812. et al. Mechanistic Insights into Regulation of JAK2 Tyrosine Kinase. Front Endocrinol (Lausanne). 2018 Jan 5;8:361. [Content Brief]
- [2]. Ihle JN, et al. Jaks and Stats in signaling by the cytokine receptor superfamily. Trends Genet. 1995 Feb;11(2):69-74. [Content Brief]
- [3]. Rawlings JS, et al. The JAK/STAT signaling pathway. J Cell Sci. 2004 Mar 15;117(Pt 8):1281-3. [Content Brief]
- [4]. Gäbler K, et al. JAK2 mutants (e.g., JAK2V617F) and their importance as drug targets in myeloproliferative neoplasms. JAKSTAT. 2013 Jul 1;2(3):e25025. [Content Brief]
- [5]. Suzuki K, et al. Janus kinase 3 (Jak3) is essential for common cytokine receptor gamma chain (gamma(c))-dependent signaling: comparative analysis of gamma(c), Jak3, and gamma(c) and Jak3 double-deficient mice. Int Immunol. 2000 Feb;12(2):123-32. [Content Brief]
- [6]. Ghoreschi K, et al. Janus kinases in immune cell signaling. Immunol Rev. 2009 Mar;228(1):273-87. [Content Brief]
- [7]. Naqvi K, et al. A potential role of ruxolitinib in leukemia. Expert Opin Investig Drugs. 2011 Aug;20(8):1159-66. [Content Brief]
- [8]. Hart S, et al. SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies. Leukemia. 2011 Nov;25(11):1751-9. [Content Brief]
- [9]. Cheng Z, et al. Angiogenesis in JAK2 V617F positive myeloproliferative neoplasms and ruxolitinib decrease VEGF, HIF-1 enesis in JAK2 V617F positive cells. Leuk Lymphoma. 2018 Jan;59(1):196-203. [Content Brief]
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JAK2 Related Products (209)
Related Products (209)
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Antibodies (3)
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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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JAK2/STAT3-IN-2
0 ImagesCat. No.: HY-183370JAK2/STAT3-IN-2 is an orally active JAK2/STAT3 inhibitor. JAK2/STAT3-IN-2 inhibits the phosphorylation of tyrosine residues in JAK2 and STAT3, blocks downstream signal transduction, disrupts the dimerization and nuclear translocation of STAT3, and suppresses pro-inflammatory transcriptional activity. JAK2/STAT3-IN-2 inhibits the expression of IL-17A and IL-17F, reduces immune cell infiltration, and inhibits the production of NO simultaneously. JAK2/STAT3-IN-2 exerts a protective effect in a mouse model of ulcerative colitis induced by DSS (HY-116282C). JAK2/STAT3-IN-2 can be used for the research of ulcerative colitis.
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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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JAK2-IN-26
0 ImagesCat. No.: HY-189581CAS No.: 3047885-19-5
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Bufothionine
0 ImagesBufothionine is an alkaloid. Bufothionine can be isolated from Cinobufacini. Bufothionine induces mitochondria-mediated Apoptosis. Bufothionine significantly reduces serum IL-6 concentration, suppresses p-Stat3tyr705, p-Stat3ser727 and Jak2 expressions. Bufothionine upregulates Atg5, Atg7 and LC3Ⅱ expressions. Bufothionine induces Autophagy. Bufothionine suppresses PIM3 expression. Bufothionine relieves symptoms of H22-tumor-bearing mice and exerts anti-inflammation activity. Bufothionine exerts anti-cancer activities against gastric cancer.
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JAK1/2-IN-2
0 ImagesCat. No.: HY-177006CAS No.: 1470249-04-7JAK1/2-IN-2 (Compound 37) is a potent and selective JAK1/2 inhibitor with Ki values of 2 and 0.6 nM .
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Tkip
0 ImagesCat. No.: HY-P10840CAS No.: 716361-65-8Tkip is a JAK2 specific inhibitor. Tkip can bind the JAK2 autophosphorylation site, inhibit the JAK2 autophosphorylation and the phosphorylation of the IFN-γ receptor subunit IFNGR-1. Tkip inhibits the antiviral activity of IFN-γ and the expression of MHC Class I molecules. Tkip can be used to study the IFN-γ signaling pathway.
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JAK2-IN-5
0 ImagesCat. No.: HY-136734CAS No.: 1110502-30-1JAK2-IN-5 (Compound 13) is a selective JAK kinase inhibitor, with an IC50 of 0.078 μM against JAK-2 and an IC50 of 0.206 μM against JAK-2V617F. JAK2-IN-5 can be used for the research of myeloproliferative disorders.
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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.
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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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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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MPT0B098
0 ImagesCat. No.: HY-124595CAS No.: 1254363-89-7MPT0B098 is a microtubule inhibitor with a Ki of 0.8 μM and an IC50 of 0.8 μM. MPT0B098 inhibits tubulin polymerization, blocks HuR nuclear-cytoplasmic translocation to decrease HIF-1α mRNA stability, suppresses HIF-1α, TGF-β/Smad, JAK2/STAT3 and FAK/actin cytoskeleton signaling pathways, upregulates SOCS3 to reinforce the inhibition of JAK2/STAT3 cascade, and induces apoptosis. MPT0B098 can be used for research on multiple malignancies including head and neck squamous cell carcinoma and human non-small cell lung cancer.
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Deuruxolitinib phosphate
0 ImagesCat. No.: HY-50856BSCAS No.: 2147706-60-1Synonyms: CTP-543 phosphate; Ruxolitinib-d8 phosphate; INCB18424-d8 (phosphaDeuruxolitinib phosphate (CTP-543 phosphate; Ruxolitinib-d8 phosphate) is a deuterated analog of Ruxolitinib (HY-50856) and an orally active, selective inhibitor of JAK1 and JAK2. Deuruxolitinib phosphate blocks Janus kinase-mediated cytokine receptor signaling and proinflammatory cytokine gene expression. Deuruxolitinib phosphate is primarily metabolized in the liver via CYP2C9. Deuruxolitinib phosphate promotes scalp hair regrowth in severe chronic alopecia areata. Deuruxolitinib phosphate is used in alopecia areata-related research.
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Nuvisertib (Standard)
0 ImagesSynonyms: TP-3654 (Standard)Nuvisertib (Standard) (TP-3654 (Standard)) is the analytical standard of Nuvisertib (HY-101126). This product is intended for research and analytical applications. Nuvisertib (TP-3654) is an orally active second-generation pan-PIM kinase inhibitor with Ki values of 5 nM, 239 nM, and 42 nM against PIM-1, PIM-2, and PIM-3, respectively. Nuvisertib inhibits JAK-independent inflammatory and survival signaling pathways, reduces the production of proinflammatory cytokines, restores apoptotic sensitivity, inhibits mTORC1, MYC, and TGF-β signaling pathways, and decreases the expression of fibrosis markers. Nuvisertib selectively impairs the transport function of ABCG2, resensitizes multidrug-resistant cancer cells to cytotoxic drugs, and overcomes JAK2 inhibitor resistance. Nuvisertib can be used in research related to myelofibrosis, renal cell carcinoma, multidrug-resistant cancer, advanced solid tumors, urothelial carcinoma, and prostate adenocarcinoma.
