• 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: 95%+ (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: 6-Substituted indolocarbazoles were found to be potent and selective D1/CDK4 inhibitors and exhibited potent and ATP-competitive D1/CDK4 activities (IC50 values of 76 and 42 nM). Two compoundts had high selectivity against the other kinases. These D1/CDK4 inhibitors inhibited tumor cell growth, arrested tumor cells at the G1 phase, and inhibited pRb phosphorylation.