(R)-CR8

Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy.{21810} (R)-CR8 is a second-generation analog of (R)-roscovitine (Item No. 10009569) that inhibits Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p25, and Cdk9/cyclin T with IC50 values of 0.09, 0.072, 0.041, 0.11, and 0.18 ?M, respectively.{21811,21809} (R)-CR8 has 2- to 4-fold improved potency for the inhibition of CDKs over (R)-roscovitine and can inhibit the proliferation of various cancer cell lines with ~40-fold more potency than (R)-roscovitine (IC50s ~ 0.39 versus 27.8 ?M, respectively).{21811,21809} (R)-CR8 also inhibits casein kinase 1 (CK1d/?) with an IC50 value of 0.40 ?M and inhibits GSK3a/B with an IC50 value of 12 ?M.{21811}