REVIEW Cyclin-dependent kinases (CDKs) are key regulators of cell progression. CDK2 and CDK4 are responsible for phosphorylation of the Retinoblastoma (RB) protein causing activation of the E2F transcription factor and transcription of genes involved in the G1/S transition and initiation of DNA replication. Several CDK inhibitors are thus being developed as potential anti-cancer agents. PHA-690509 on such CDK inhibitor. PHA-690509 is a ATP-competitive CDK inhibitor with submicromolar IC50 against multiple CDKs, in particular CDK2, its primary target (IC50 31nM). In cell proliferation assays, PHA-690509 demonstrated marked potency against several cells lines with IC50 values in the submicromolar range primarily.
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