3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable 3-substituted indolinone compound that displays anti-proliferative and proapoptotic properties in tumor cells. Acts as a potent, selective, and ATP-competitive inhibitor of cyclin dependent kinases (Cdks; IC50 = 22 nM for Cdk2/A; 40 nM for Cdk1/B; 200 nM for Cdk4/D1). It shows no significant effect (IC50 >10 µM) on the activities of PKC, p38, PDGFRb, or EGFR. Inhibits the proliferation of growth factor-stimulated colon carcinoma cells by binding to Cdk2 and preventing the phosphorylation of pRb and its dissociation from E2F. Purity: ≥95% by HPLC. CAS 666837-93-0. Ref.: Yu, B., et al. 2002. Biochem. Pharmacol. 64, 1091. Lane, M.E., et al. 2001. Cancer Res. 61, 6170. |
