Background Information: A cell-permeable, unsymmetrical indolocarbazole compound that displays antiproliferative properties. Acts as a potent, selective, reversible and ATP-competitive inhibitor of Cdk4/D1 (IC50 = 76 nM). It inhibits the activity of other Cdk’s only at much higher concentrations (IC50 = 520 nM and 2.1 µM for Cdk2/E and Cdk1/B, respectively) and shows little activity towards CaMKII, PKA, or GSK-3β (IC50 ≥ 12.4 µM). Shown to inhibit tumor cells growth (IC50 < 3.0 µM in HCT-116 and NCI-H460 cells) by blocking Rb phosphorylation and inducing G1 cell cycle arrest.
Empirical Formula: C20H10BrN3O2
Gene Symbol: CDK4
Properties: Solubility: DMSO (1 mg/ml).
Presentation: Yellow solid. Packaged under inert gas.
Molecular Weight: 404.2
Storage Conditions: Shipped at Ambient Temperature. Store at +2 - 8°C.