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SU9516 is a 3-substituted indolinone compound displaying anti-proliferative and proapoptotic properties in tumor cells. SU9516 displays activity as a selectively potent ATP-competitive inhibitor of CDKs. It also shows no significant effect (IC50 >10 μM) on the activities of PKC, p38, PDGFRβ, or EGFR. SU9516 has an Inhibitory effect on proliferation of growth-factor stimulated colon carcinoma cells by binding to Cdk2 and preventing the phosphorylation of pRb and its dissociation from E2F. SU9516 is an inhibitor of Cdc2, Cdk2 and Cdk4.
1. Lane, M E., et al., 2001. A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Cancer research. 61(16): 6170-7. PMID: 11507069
2. Yu, Bo., et al., 2002. SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells. Biochemical pharmacology. 64(7): 1091-100. PMID: 12234612
See how others have used SU9516. Click on the entry to view the PubMed entry .
PMID: # 25394488
Su, M. et al. 2015. MicroRNA-221 inhibits autophagy and promotes heart failure by modulating the p27/CDK2/mTOR axis. Cell death and differentiation. 22: 986-99.
PMID: # 24101496
Bogdanow, et al. 2013. Human cytomegalovirus tegument protein pp150 acts as a cyclin A2-CDK-dependent sensor of the host cell cycle and differentiation state. Proc Natl Acad Sci U S A. 110: 17510-5.
PMID: # 20844576
Zydek, M. et al. 2010. Cyclin-dependent kinase activity controls the onset of the HCMV lytic cycle. PLoS Pathog.. 6: -.
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