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 (205)
Related Products (205)
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Antibodies (3)
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SJ988497
0 ImagesSJ988497 is a PROTAC degrader targeting JAK2. SJ988497 induces the proteasomal degradation of CRBN-mediated JAK2, JAK1, JAK3, GSPT1, and IKZF1, and functions as a CRBN neosubstrate for GSPT1. SJ988497 retains binding affinity for the kinase domain of JAK2. SJ988497 can be used in studies related to cancers such as crlf2-rearranged acute lymphoblastic leukemia.
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Telocinobufagin
0 ImagesTelocinobufagin (Telobufotoxin; Telocinobufogenin) is an orally active bufadienolide with potential anti-tumor effects. Telocinobufagin exerts its anti-cancer effects on non-small cell carcinoma, osteosarcoma, thyroid cancer, breast cancer and head and neck squamous cell carcinoma by inhibiting the STAT3, JAK2/STAT3, LARP1-mTOR, PI3K/Akt/Snail and PLK1 pathways, and can also induce tumor cell apoptosis. Telocinobufagin enhances the Th1 immune response and protects against Salmonella typhimurium infection. Telocinobufagin has a strong cardiac-stimulating effect by inhibiting the activity of Na+/K+-ATPase, and it can promote renal fibrosis. Telocinobufagin demonstrates non-opioid analgesic effects in various acute pain models.
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Broussonin E
0 ImagesBroussonin E is a phenolic compound and shows anti-inflammatory activity. Broussonin E can suppress inflammation by modulating macrophages activation statevia inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway. Broussonin E can be used for the research of inflammation-related diseases such as atherosclerosis.
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Ivarmacitinib
0 ImagesSynonyms: SHR0302Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects.
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AZ960
0 ImagesCat. No.: HY-10411CAS No.: 905586-69-8AZ960 is a potent and specific inhibitor of the JAK2 kinase with a Ki of 0.45 nM.
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Protosappanin A
0 ImagesSynonyms: PTA
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XL019
0 ImagesXL019?is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.
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Cadefrecitinib
0 ImagesSynonyms: GLPG3667Cadefrecitinib (GLPG3667) is a reversible, ATP-competitive and orally active TYK2 inhibitor with an IC50 of 2.3 nM. Cadefrecitinib inhibits IFNα/pSTAT1, and the IC50 values in human peripheral blood mononuclear cell (PBMC) and whole blood assays are 70 nM and 623 nM, respectively. Cadefrecitinib has the potential for the study of inflammatory and autoimmune diseases.
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(E/Z)-Zotiraciclib hydrochloride
0 ImagesSynonyms: (E/Z)-TG02 hydrochloride; (E/Z)-SB1317 hydrochloride
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Zotiraciclib
0 ImagesSynonyms: TG02; SB1317Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC50 values of 13 nM, 73 nM and 56 nM, respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia and multiple myeloma.
