PROTAC CDK4/6 degrader 1

PROTAC CDK4/6 degrader 1 (Compound 7f) is a dual degrader for CDK4 and CDK6 with DC50 of 10.5 and 2.5 nM. PROTAC CDK4/6 degrader 1 inhibits the proliferation of cell Jurkat (IC50 is 0.18 μM), arrests the cell cycle at G1 phase and induces apoptosis. (Pink: ligand for target protein YY173 (HY-163787); Black: linker (HY-163788); Blue: ligand for E3 ligase (HY-10984))[1]

CDK4: 10.5 nM (DC₅₀); CDK6: 2.5 nM (DC₅₀)

[1] He H, et al., Development of Degraders of Cyclin-Dependent Kinases 4 and 6 Based on Rational Drug Design. J Med Chem. 2024 Jul 11;67(13):11354-11364. DOI:10.1021/acs.jmedchem.4c00965