cdk4/6-in-3

CDK4/6-IN-3, a brain-penetrant CDK4/CDK6 inhibitor (Kis: <0.3 nM and 2.2 nM), is used for the treatment of glioblastoma and inhibits CDK1 with a Ki of 110 nM.

CDK4/6-IN-23 (Compound 42) is a potent and selective inhibitor of CDK4/6, displaying an IC50 of 11 nM for CDK6. This compound significantly activates immune cells and enhances IL-3 production. In mice undergoing 5-FU chemotherapy, CDK4/6-IN-23 demonstrates dual bone marrow protection and immunomodulatory effects.

LO-3-63 is a Ribociclib analogue featuring a truncated fumaramide group and acts as a CDK4/6 degrader with PROTAC properties. It degrades CDK4/6 in cells via a CUL4DCAF16-dependent pathway.