R547 is a potent and selective ATP-competitive inhibitor of Cyclin-Dependent Kinases (CDK) 1, 2 and 4 with Ki of 2 nM for CDK1/cyclin B, 3 nM for CDK2/cyclin E, and 1 nM for CDK4/cyclin D1. R547 is less potent for CDK7 and GSK3α/β, and inactive (Ki > 5,000 nmol/L) against a panel of >120 unrelated kinases. R547 was shown to inhibit retinoblastoma protein in tumor cells and xenografts and showed up to 95% tumor growth inhibition in the HCT116 human colorectal tumor xenograft model in nude mice.
R547 is a potent and selective ATP-competitive inhibitor of Cyclin-Dependent Kinases (CDK) 1, 2 and 4.
The causative agent of the coronavirus disease 2019 (COVID-19) pandemic, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has infected millions and killed hundreds of thousands of people worldwide, highlighting an urgent need to develop antiviral therapies. Here we present a
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