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 µM) on the activities of PKC, p38, PDGFRβ, 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, PDGFRβ, or EGFR (IC50 >10 µM). 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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target Cdk2/A
Product competes with ATP.
Reversible: yes
Target IC50: 22 nM for Cdk2/A; 40 nM for Cdk1/B; 200 nM for Cdk4/D1
Warning
Toxicity: Carcinogenic / Teratogenic (D)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Yu, B., et al. 2002. Biochem. Pharmacol.64, 1091. Lane, M.E., et al. 2001. Cancer Res.61, 6170.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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