PROTAC CDK6 Degrader 1 (compound 48a) is a potent and selective PROTAC CDK6 degrader with a DC50 of 0.037 μM. PROTAC CDK6 Degrader 1 exhibits selectivity over CDK4 ( DC50 > 10 μM). PROTAC CDK6 Degrader 1 induces G0/G1 cell-cycle arrest and apoptosis through inhibition of CDK6 downstream signaling. PROTAC CDK6 Degrader 1 reduces tumor burden and CDK6 levels in a MOLM-14 xenograft mouse model. PROTAC CDK6 Degrader 1 can be used for CDK6-driven cancers research, such as acute myeloid leukemia (AML) [1]. (Pink: CDK6 ligand; Blue: KLHDC2 ligand; Black: linker).
References:
[1]. Jeon E, et al. Selective CDK6 Degradation via the KLHDC2 E3 Ubiquitin Ligase. J Med Chem. 2025 Dec 11;68(23):25539-25568.
References:
[1]. Jeon E, et al. Selective CDK6 Degradation via the KLHDC2 E3 Ubiquitin Ligase. J Med Chem. 2025 Dec 11;68(23):25539-25568.