PROTAC CDK2/4 Degrader-1 is a PROTAC degrader of cyclin-dependent kinase 2 ( CDK2 ) and cyclin-dependent kinase 4 ( CDK4 ). PROTAC CDK2/4 Degrader-1 induces degradation via the ubiquitin-proteasome pathway. PROTAC CDK2/4 Degrader-1 can be used in cancer research [1]. (Pink: CDK2 and CDK4 ligand; Blue: Cereblon ligand; Black: linker).
In Vitro, PROTAC CDK2/4 Degrader-1 (compound 5) (24 h) effectively inhibits the kinase activity of CDK2 and CDK4 at the cellular level, showing stronger inhibitory activity against CDK4 (Class AA, < 1 nM)[1].
References:
[1]. Yu Z. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and/or cyclin-dependent kinase 4 via ubiquitin proteasome pathway. WO2025240536 A1. 2025 Nov 20.
In Vitro, PROTAC CDK2/4 Degrader-1 (compound 5) (24 h) effectively inhibits the kinase activity of CDK2 and CDK4 at the cellular level, showing stronger inhibitory activity against CDK4 (Class AA, < 1 nM)[1].
References:
[1]. Yu Z. Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and/or cyclin-dependent kinase 4 via ubiquitin proteasome pathway. WO2025240536 A1. 2025 Nov 20.