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产品介绍
产品介绍
产品信息
简单描述
SU 9516 is a cell permeable, potent, selective and ATP-competitive inhibitor of Cdk2/cyclin A (IC50=22nM), Cdk1/cyclin B (IC50=40nM) and Cdk4/cyclin D1 (IC50=200nM). SU9516 has no effect on the activity of PKC, p38, PDGFRβ and EGFR (IC50>10μM). The compound displays anti-proliferative and pro-apoptotic properties in tumor cells and inhibits proliferation of growth factor-stimulated colon carcinoma cells. SU 9516 does this by binding to Cdk2 and thus preventing the phosphorylation of pRb and its dissociation from E2F.
参考文献 M.E. Lane, et al.; Cancer Res. 61, 6170 (2001). B. Yu, et al.; Biochem Pharmacol. 64, 1091 (2002). D.J. Moshinsky, et al.; BBRC 310, 1026 (2003). X. Li, et al.; Bioorg. Med. Chem. Lett. 13, 1939 (2003).
分子量
241.25
应用
实验应用
SU 9516 is a cell permeable, potent, selective and ATP-competitive inhibitor
背景
别名
3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one
结构式
COC1=CC\2=C(C=C1)NC(=O)/C2=C\C3=CN=CN3
分子式
C13H11N3O2
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