Description
K00546 is a potent CDK1 and CDK2 inhibitor with IC 50 s of 0.6 nM and 0.5 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. K00546 is also a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC 50 s of 8.9 nM and 29.2 nM, respectively. In VitroK00546 binds to the SLK ATP-binding site forming three hydrogen bonds with the kinase hinge residues E109 and C111. The sulphamoyl moiety of K00546 also interacts with the main chain of L40. K00546 (compound 3n) also inhibits PKA, casein kinase-1, MAP kinase (ERK-2), calmodulin kinase, VEGF-R2, GSK-3 and PDGF-Rβ with IC 50 values of 5.2 µM, 2.8 µM, 1.0 µM, 8.9 µM, 0.032 µM, 0.14 µM and 1.6 µM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only