CDK

PHA-848125 (Milciclib) is an orally bioavailable inhibitor of CDKs and TRKA with potential antineoplastic activity.

Cdc7-IN-1 (Compound 13) is a highly potent, selective and ATP competitive inhibitor of Cdc7 kinase, with an IC50 value of 0.6 nM at 1 mM ATP and with slow off-rate characteristics.

CDK8-IN-1 is a potent and selective CDK8 inhibitor with an IC50 of 3 nM.

PHA-690509 is a ATP-competitive CDK inhibitor.

FN-1501 is a potent inhibitor of FLT3 and CDK, with IC50s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively. FN-1501 has anticancer activity.

CDK9-IN-2 is a novel cyclin-dependent kinase 9(CDK9) inhibitor.

NVP-LCQ195 is a small molecule heterocyclic inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM.

LY2857785 is a potent and selective CDK9 inhibitor; significantly reduces RNAP II CTD phosphorylation and dramatically decreases MCL1 protein levels to result in apoptosis in a variety of leukemia and solid tumor cell lines.

CDK2-IN-4 is a potent and selective CDK2 inhibitor with an IC50 of 44 nM for CDK2/cyclin A, shows 2,000-fold selectivity over CDK1/cyclin B (IC50=86 uM).

BSJ-03-123 is a potent and novel CDK6-selective small-molecule degrader (PROTAC).