SU9516
CDK inhibitor (pan-specific) / Cyclin-dependent kinase inhibitor, IC50s= 0.02-0.03, 0.04-0.2, 0.2-1.7 and 0.9 µM for cdk2, cdk1, cdk4, cdk9 respectively.1,2 Inhibits phosphorylation of retinoblastoma protein pRb, causing enhanced pRb/E2f complex formation, cell cycle arrest at G1 and G2-M and apoptosis.3 Down-regulates antiapoptotic protein Mcl-1 expression resulting in mitochondrial injury and cell death.4 Inhibits epithelial-mesenchymal transition (IC50=1.21 µM) a crucial pathological event in tumor cell budding and metastasis.5 Cell permeable.
Biochemicals & reagents
377090-84-1
1 Lane et al. (2001) A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells; Cancer Res. 61 6170 2 Jorda et al. (2018) How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?; J. Med. Chem. 61 9105 3 Yu et al. (2002) SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells; Biochem. Pharmacol. 64 1091 4 Gao et al. (2006) The three-substituted indolinone cyclin-dependent kinase 2 inhibitor 3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one (SU9516) kills human leukemia cells via down-regulation of Mcl-1 through a transcriptional mechanism; Mol. Pharmacol 70 645 5 Arai et al. (2016) A Novel High-Throughput 3D Screening System for EMT Inhibitors: A Pilot Screening Discovered the EMT Inhibitory Activity of CDK2 Inhibitor SU9516; PLoS One 11 e0162394
-20°C
TARGET: Kinase -- PATHWAY: Mitochondrial function; Apoptosis inducer; Cell cycle -- RESEARCH AREA: Cell death -- DISEASE AREA: Cancer