Cdk4 Inhibitor
     
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Cdk4 Inhibitor

12,13-Dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione (Arcyriaflavin A)
Inhibitor of cdk4/cyclin D1 (IC50 = 59 nM). Active against CaM kinase II (IC50 = 25 nM) but displays selectivity over several other kinases in vitro (IC50 values for inhibition of PKA and PKC are > 2 and > 100 ?M respectively). Inhibits human cytomegalovirus (HCMV) replication in vitro (IC50 = 200 nM).

Cdk4_Inhibitor_2
OTAVAchemicals Catalogue Number: 7070707137
CAS Registry Number: 118458-54-1
Purity: 95%+ (HPLC)


Ref.: Zhu et al. Synthesis of quinolinyl/isoquinolinyl[a]pyrrolo [3,4-c] carbazoles as cyclin D1/CDK4 inhibitors. Bioorganic & Medicinal Chemistry Letters (2003), 13, 1231-1235


Abstract: A novel series of pyrrolo[3,4-c] carbazoles fused with a quinolinyl/isoquinolinyl moiety were synthesized and their D1/CDK4 inhibitory and antiproliferative activity were evaluated. Compound 8H,14H-isoquinolinyl[6,5-a]-pyrrolo[3,4-c]carbazole-7,9-dione (1d) was found to be a highly potent D1/CDK4 inhibitor with an IC50 of 69 nM. Compound 1d also inhibited tumor cell growth, arrested tumor cells in G1 phase and inhibited pRb phosphorylation.

 
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