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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JAK2-IN-22
0 ImagesCat. No.: HY-188001CAS No.: 3057053-13-8
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Tyk2-IN-28
0 ImagesCat. No.: HY-187467Tyk2-IN-28 is an orally active and selective TYK2 inhibitor with an IC50 of 0.9 nM. Tyk2-IN-28 also inhibits JAK2 kinase activity with an IC50 of 4 nM. Tyk2-IN-28 blocks inflammatory cytokine signaling. Tyk2-IN-28 reduces paw swelling in mouse models. Tyk2-IN-28 can be used for research on psoriasis.
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JAK1-IN-9
0 ImagesCat. No.: HY-144440CAS No.: 2875041-96-4JAK1-IN-9 (compound 23a) is a potent and selective JAK1 inhibitor with an IC50 of 72 nM. JAK1-IN-9 shows selective against other JAKs by 12 times or more.
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WWQ-131
0 ImagesCat. No.: HY-174430CAS No.: 1558007-80-9WWQ-131 is a potent selective JAK2 inhibitor with an IC50 of 2.56 nM. WWQ-131 shows >252-fold selectivity over JAK1, JAK3, and TYK2. WWQ-131 exhibits antiproliferative activity against cancer cells. WWQ-131 is the ligand for target protein for PROTAC JAK2 degrader-1 (HY-174428). WWQ-131 can be used for the research of myeloproliferative neoplasms (MPNs).
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NVP-BVB808
0 ImagesCat. No.: HY-182430CAS No.: 1180158-99-9NVP-BVB808 is a selective and ATP-competitive JAK2 inhibitor with an IC50 of 0.35 nM. NVP-BVB808 binds to JAK2’s ATP-binding site, stabilizes JAK2’s active conformation, increases JAK2 activation loop phosphorylation, and blocks downstream kinase function. NVP-BVB808 exhibits antiproliferative and pro-apoptosis effects, suppresses constitutive STAT5a phosphorylation. NVP-BVB808 can be used for the research of cancer, such as leukemia.
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Soficitinib
0 ImagesSoficitinib (Compound 20) is a selective tyrosine kinase 2 (TYK2) and Janus kinase 2 (JAK2) inhibitor, with IC50 values of 0.5 nM and 1.2 nM, respectively. Soficitinib shows promise for research into autoimmune diseases (such as psoriasis, rheumatoid arthritis) and inflammatory diseases.
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FLT3/JAK2/BRD4 ligand-1
0 ImagesCat. No.: HY-175611CAS No.: 3067695-60-4
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JAK2-IN-9
0 ImagesCat. No.: HY-155746CAS No.: 2568842-26-0JAK2-IN-9 is an orally active selective JAK2 inhibitor with a human IC50 of 5 nM. JAK2-IN-9 inhibits JAK2 kinase activity, blocks JAK2 phosphorylation, and suppresses the activation of the downstream JAK2-STAT signaling pathway. JAK2-IN-9 inhibits the phosphorylation of STAT3, STAT5 and AKT in cancer cells. JAK2-IN-9 induces cancer cell apoptosis (apoptosis) and cell cycle arrest. JAK2-IN-9 can be used for the research of myeloproliferative neoplasms.
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NSC 33994
0 ImagesCat. No.: HY-18293CAS No.: 82058-16-0NSC 33994 (G6) is a selective JAK2 inhibitor, with an IC50 of 60 nM.
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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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JAK2-IN-21
0 ImagesCat. No.: HY-183670CAS No.: 3038340-43-8JAK2-IN-21 is a Janus kinase 2 (JAK2) inhibitor with an IC50 of 12.25 nM. JAK2-IN-21 inhibits the JAK2/STAT3/STAT5 tumor-promoting signaling pathway and reduces JAK2 protein expression. JAK2-IN-21 exhibits selective cytotoxicity against HPV-positive cancer cells and induces cancer cell apoptosis. JAK2-IN-21 can be used in the research of HPV-positive cervical cancer.
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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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PI3K/Akt/mTOR-IN-7
0 ImagesCat. No.: HY-183272CAS No.: 2925588-01-6PI3K/Akt/mTOR-IN-7 is an AKT/mTOR and JAK2/STAT3 inhibitor. PI3K/Akt/mTOR-IN-7 restores p-Akt, p-mTOR, and p-STAT3 expression, reduces pro-apoptotic Caspase-3 mRNA expression. PI3K/Akt/mTOR-IN-7 reduces intracellular ROS accumulation and inhibits NO production. PI3K/Akt/mTOR-IN-7 can be used for research on stroke, Alzheimer's disease and Parkinson's disease.
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JAK2-IN-23
0 ImagesCat. No.: HY-188002CAS No.: 3057053-16-1
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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.
