AG-490 (Tyrphostin B42) (Synonyms: Tyrphostin AG-490) |
| Catalog No.GC13854 |
AG-490 (Tyrphostin B42) (Tyrphostin AG-490 (Tyrphostin B42))은 EGFR, Stat-3 및 JAK2/3을 억제하는 티로신 키나아제 억제제입니다.
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Cas No.: 133550-30-8
Sample solution is provided at 25 µL, 10mM.
AG-490 (Tyrphostin B42) is EGFR inhibitor with IC50 of 0.1 µM, AG-490 also has an inhibitory effect on JAK2[1-3].
AG-490(5-50 µM;3days) suppresses RANKL-induced osteoclastogenesis in RAW264.7 cells[4]. AG490(20 µM; 4 h) inhibits hOAT3 transport activity[5]. AG-490(10 µM)suppresses interleukin-34-mediated osteoclastogenesis in mice bone marrow macrophages[6].
AG-490(5-15 µM;i.p;) exerted protection effects by preventing the neural apoptosis in vivo[7]. In tumor mice, AG-490(500 µg/mouse;i.p;11days) treatment significantly inhibited subcutaneous tumor growth[8].
References:
[1]. DuhÉ RJ, Clark EA, et,al. Characterization of the in vitro kinase activity of a partially purified soluble GST/JAK2 fusion protein. Mol Cell Biochem. 2002 Jul;236(1-2):23-35. doi: 10.1023/a:1016186907376. PMID: 12190118.
[2]. Luo C, Laaja P. Inhibitors of JAKs/STATs and the kinases: a possible new cluster of drugs. Drug Discov Today. 2004 Mar 15;9(6):268-75. doi: 10.1016/S1359-6446(03)03014-9. PMID: 15003245.
[3]. Gazit A, Osherov N, et,al. Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J Med Chem. 1991 Jun;34(6):1896-907. doi: 10.1021/jm00110a022. PMID: 1676428.
[4]. Li CH, Zhao JX, et,al. AG490 inhibits NFATc1 expression and STAT3 activation during RANKL induced osteoclastogenesis. Biochem Biophys Res Commun. 2013 Jun 14;435(4):533-9. doi: 10.1016/j.bbrc.2013.04.084. Epub 2013 May 7. PMID: 23665018.
[5]. Zhang J, Liu C, et,al. AG490, a JAK2-specific inhibitor, downregulates the expression and activity of organic anion transporter-3. J Pharmacol Sci. 2018 Mar;136(3):142-148. doi: 10.1016/j.jphs.2018.01.006. Epub 2018 Feb 8. PMID: 29487013; PMCID: PMC7863619.
[6]. Cheng X, Wan QL, et,al. AG490 suppresses interleukin-34-mediated osteoclastogenesis in mice bone marrow macrophages. Cell Biol Int. 2017 Jun;41(6):659-668. doi: 10.1002/cbin.10771. Epub 2017 Apr 19. PMID: 28378938.
[7]. Fan L, Zhou L. AG490 protects cerebral ischemia/reperfusion injury via inhibiting the JAK2/3 signaling pathway. Brain Behav. 2021 Jan;11(1):e01911. doi: 10.1002/brb3.1911. Epub 2020 Oct 23. PMID: 33098244; PMCID: PMC7821583.
[8]. Kobayashi A, Tanizaki Y, et,al. AG490, a Jak2 inhibitor, suppressed the progression of murine ovarian cancer. Eur J Pharmacol. 2015 Nov 5;766:63-75. doi: 10.1016/j.ejphar.2015.09.039. Epub 2015 Sep 26. PMID: 26410360.
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