2-Bromo-12,13-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable, unsymmetrical indolocarbazole compound that displays antiproliferative properties. Acts as a potent, selective, 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-3b (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. Purity: ≥95% by HPLC. CAS 546102-60-7. Ref.: Zhu, G., et al. 2003. J. Med. Chem. 46, 2027. |
