LDC4297

Description: LDC4297 is a novel and potent CDK7 (Cyclin-dependent protein kinase 7) inhibitor with IC50 of 0.13+/-0.06 nM for CDK7 and IC50s between 10 nM and 10, 000 nM for all other analyzed CDKs. Cyclin-dependent protein kinase 7 (CDK7) plays crucial regulatory roles in cell cycle and transcription, both connected with the replication of many viruses. The affinity of LDC4297 for CDK7 proves to be extremely high. The replication of HCMV in cultured primary human fibroblasts (HFFs) is inhibited by LDC4297 in a concentration-dependent manner with a 50% effective concentration (EC50) value of 24.5 +/- 1.3 nM. Notably, CDK7 inhibition by LDC4297 is not associated with general cytotoxicity at submicromolar concentrations. Summarized, the CDK7 inhibitor LDC4297 is a promising candidate for further antiviral drug development, possibly offering new options for a comprehensive approach to antiviral therapy.

References: Antimicrob Agents Chemother. 2015 Apr; 59(4):2062-71.