2-Bromo-12,13-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione

• 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)

OTAVAchemicals Catalogue Number: 7070707035

CAS Registry Number: 546102-60-7

Purity: 97% (HPLC)

Ref.: Zhu et al. Synthesis, Structure-Activity Relationship, and Biological Studies of Indolocarbazoles as Potent Cyclin D1-CDK4 Inhibitors. Journal of Medicinal Chemistry (2003), 46, 2027-2030

Abstract: 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-3ß (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.

DOI: 10.1021/jm0256169

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