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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JAK1/TYK2-IN-3
0 ImagesCat. No.: HY-143885CAS No.: 2734918-37-5JAK1/TYK2-IN-3 is a potent, selective and orally active dual TYK2/JAK1 inhibitor with IC50 values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC50=140 nM) and JAK3 (IC50=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related TYK2/JAK1-regulated genes, as well as the formation of Th1, Th2, and Th17 cells.
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Tubulosine
0 ImagesTubulosine is an alkaloid. Tubulosine can be isolated from Pogonopus tubulosus (DC.) Schumann. Tubulosine is an ATP-competitive, selective JAK3 inhibitor with an IC50 value of 9.9 nM. Tubulosine also inhibits the kinase activities of other JAK family members, the extent of inhibition is less than that of JAK3, with IC50 values of 69.5, 84.9 and 76.3 nM for JAK1, JAK2 and TYK2, respectively. Tubulosine selectively inhibits JAK3 signalling by binding to the ATP-binding site of the kinase of JAK3. Tubulosine induces apoptotic and necrotic/autophagic cell death. Tubulosine inhibits the process of peptide chain elongation by eukaryotic polysomes by, specifically preventing the elongation-factor-2-dependent step of translocation. Tubulosine exhibits anticancer activity in breast cancer cells.
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Ovalicin
0 ImagesCat. No.: HY-156959CAS No.: 19683-98-8Ovalicin is a multi-target inhibitor that targets MetAP2, HRH2, JAK2 and TRPV1, with anti-inflammatory and anti-atopic dermatitis activities. Ovalicin covalently binds to MetAP2 to inhibit its function, thereby blocking the replication of Enterocytozoon bieneusi and Vittaforma corneae. Ovalicin alleviates intestinal injury and prolongs survival in infected mouse models, without showing obvious hepatorenal toxicity. Ovalicin attenuates LPS-induced calcium influx, reduces the infiltration of macrophages and mast cells in the skin, and regulates the expression of inflammation-related genes such as IL-31, effectively relieving allergic symptoms in mouse models. Ovalicin can be used for the research of microsporidiosis and atopic dermatitis.
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JAK1/2-IN-3
0 ImagesCat. No.: HY-180274JAK1/2-IN-3 is a JAK1 and JAK2 inhibitor with IC50 values of 14.73 nM and 10.03 nM, respectively. JAK1/2-IN-3 induces G2/M cell cycle arrest, and induces intrinsic apoptosis via increased Bax and caspase 3/7 levels and reduced Bcl2 expression. JAK1/2-IN-3 can be used for the study of leukemia cancer, breast cancer and colon cancer.
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JAK2-IN-18
0 ImagesCat. No.: HY-179687CAS No.: 3108318-77-7JAK2-IN-18 (Compound example1) is a selective JAK2 inhibitor. JAK2-IN-18 can inhibit JAK-STAT signaling and shows an IC50 of <100 nM for pSTAT5 in HEL9217 cells. JAK2-IN-18 can inhibit the proliferation of abnormally proliferating myeloid cells and can be used for the research of myeloproliferative disorders, such as essential thrombocythemia.
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JAK2-IN-13
0 ImagesCat. No.: HY-174988JAK2-IN-13 is a potent and orally active JAK2 inhibitor with an IC50 of 54.7 nM. JAK2-IN-13 downregulates the expressions of p-STAT3 and p-STAT5. JAK2-IN-13 exhibits good bioavailability and potent inhibition of rhEPO-induced extramedullary erythropoiesis and polycythemia vera. JAK2-IN-13 can be used for the study of myeloproliferative neoplasms.
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PROTAC JAK2 degrader-1
0 ImagesCat. No.: HY-174428PROTAC JAK2 degrader-1 is a JAK2 PROTAC degrader, with a DC50 of 27.35 nM. PROTAC JAK2 degrader-1 induces JAK2 degradation via the ubiquitin-proteasome pathway. PROTAC JAK2 degrader-1 inhibits the JAK2-STAT signaling pathway. PROTAC JAK2 degrader-1 induces G2/M phase arrest and apoptosis in cancer cells. PROTAC JAK2 degrader-1 exhibits antiproliferative activity against cancer cells. PROTAC JAK2 degrader-1 inhibits recombinant human erythropoietin (rhEPO)-mediated polycythemia and splenomegaly in mice. PROTAC JAK2 degrader-1 can be used for research on myeloproliferative neoplasms, including polycythemia vera.
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JAK2-IN-1
0 ImagesCat. No.: HY-117810CAS No.: 1361415-84-0JAK2-IN-1 (eExample 2) is a JAK2 inhibitor, and can be used for research of proliferative disease, inflammatory disease, or renal disease.
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JAK3-IN-11
0 ImagesCat. No.: HY-146727CAS No.: 2412734-00-8JAK3-IN-11 (Compound 12), a potent, noncytotoxic, irreversible, orally active JAK3 inhibitor with IC50 value of 1.7 nM, has excellent selectivity (>588-fold compared to other JAK isoforms), covalently bind to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T cell proliferation, is a promising tool for study autoimmune diseases.
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JAK2-IN-20
0 ImagesCat. No.: HY-181691JAK2-IN-20 is an orally active dual inhibitor targeting JAK2 kinase (IC50=49.17 nM) and influenza A virus PB2 protein (IC50=3.337 μM, Kd=2.82 μM). JAK2-IN-20 effectively blocks the JAK/STAT signaling pathway by reducing the phosphorylation levels of STAT1 and STAT3, thereby inhibiting viral replication and downregulating the expression of viral NP and PB2 proteins. In addition, JAK2-IN-20 significantly inhibits the mRNA expression of key inflammatory cytokines such as IL-6, TNF-α and IFN-β in inflammation and influenza infection models. JAK2-IN-20 serves as an important tool molecule for the study of influenza A virus infection and related pathologies.
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JAK2-IN-19
0 ImagesCat. No.: HY-180766JAK2-IN-19 (Compound 3p) is a JAK2 inhibitor with a KD value of 1.11 μM. JAK2-IN-19 inhibits the proliferation of K562 cells and HeLa cells. JAK2-IN-19 significantly reduces the level of p-JAK2. JAK2-IN-19 can be used for research on cervical cancer and leukemia.
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JAK-2/3-IN-2
0 ImagesCat. No.: HY-151256CAS No.: 2170398-48-6
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Envudeucitinibum hydrochloride
0 ImagesCat. No.: HY-153701S1CAS No.: 3009133-87-0Synonyms: Envudeucitinib hydrochloride; ESK-001 hydrochlorideEnvudeucitinibum (Envudeucitinib; ESK-001) hydrochloride is an orally active and selective TYK2 allosteric inhibitor with an IC50 range of 104-149 nM. Envudeucitinibum hydrochloride blocks JH1 catalytic activity by specifically binding to the JH2 domain of TYK2, thereby inhibiting downstream signaling pathways. Envudeucitinibum hydrochloride is used for research on plaque psoriasis, systemic lupus erythematosus, and other immune-mediated diseases.
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JAK2-IN-16
0 ImagesCat. No.: HY-160919CAS No.: 2982846-48-8
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Embricitinib
0 ImagesCat. No.: HY-176793CAS No.: 2459377-98-9Synonyms: JAK1-IN-18Embricitinib (JAK1-IN-18) (Example 2) is a selective JAK1 inhibitor with an IC50 of 0.15 nM for JAK1 over JAK2 and JAK3. Embricitinib significantly reduces inflammation in DSS (HY-116282C)-induced ulcerative colitis (UC) mouse models and DNBS(HY-W324435)-induced Crohn's disease (CD) rat models. Embricitinib can be used for autoimmune diseases (such as inflammatory bowel disease), viral infections (such as HBV infection) and cancers (such as blood cancer) research.
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AC-430
0 ImagesCat. No.: HY-16021CAS No.: 1241914-87-3AC-430 is a JAK2 inhibitor. AC-430 can be used in the research of rheumatoid arthritis.
