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Beschreibung

A cell-permeable 3-substituted indolinone compound that displays anti-proliferative and proapoptotic properties in tumor cells. Acts as a potent, selective, reversible, 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 µ,M) on the activities of PKC, p38, PDGFRbeta, 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., A cell-permeable, 3-substituted indolinone compound that displays anti-proliferative and pro-apoptotic properties in tumor cells. Acts as a potent, selective, reversible, 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). Exhibits no significant effect on the activities of PKC, p38, PDGFRbeta, or EGFR (IC50 >10 µ,M). Reported to inhibit the proliferation of growth factor-stimulated colon carcinoma cells by binding to Cdk2 and preventing the phosphorylation of pRb and its dissociation from E2F.