SU 9516

SU 9516 is a 3-substituted indolinone that has anti-proliferative and pro-apoptotic activity in tumor cells. It is a potent inhibitor of several cyclin-dependent kinases (CDKs) with selectivity for Cdk2 (IC50s = 22, 40, and 200 nM for Cdk2/cyclin A, Cdk1/cyclin B, and Cdk4/cyclin D1).1 It does not inhibit PKC, p38, PDGFR, or EGFR (IC50s = >10 µM).1 SU 9516 inhibits phosphorylation of the retinoblastoma protein pRb, resulting in increased pRb/E2F complex formation, cell-cycle arrest, and subsequent apoptosis.1,2 In leukemia cells (U937, Jurkat, and HL-60 cells) SU 9516 downregulates transcription of the antiapoptotic protein Mcl-1, leading to mitochondrial injury and cell death.3WARNING This product is not for human or veterinary use.

A pro-apoptotic Cdk2/cyclin A inhibitor

241.3

≥98%

Biochemicals/Kinase Inhibitors/CDKs/Small Molecule Inhibitors/Kinases

Formal_Name:1,3-dihydro-3Z-(1H-imidazol-5-ylmethylene)-5-methoxy-2H-indol-2-one

O=C1NC2=CC=C(OC)C=C2/C1=C/C3=CNC=N3

C13H11N3O2

377090-84-1

≥ 4 years

DMF: 5 mg/ml DMSO: 5 mg/ml DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml

1.Lane, M.E.,Yu, B.,Rice, A., et al. A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Cancer Research 61(16), 6170-6177 (2001).
2.Yu, B.,Lane, M.E. and Wadler, S. SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells. Biochemical Pharmacology 64(7), 1091-1100 (2002).
3.Gao, N.,Kramer, L.,Rahmani, M., et al. 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. Molecular Pharmacology 70(2), 645-655 (2006).