cdk9-in-11

CDK9-IN-11 is a potent CDK9 inhibitor and serves as the ligand for the PROTAC CDK9 Degrader-1 [1].

E3 Ligase Ligand 56 is a ligand for the E3 ligase Cereblon, and it can be utilized in the synthesis of [PROTACCDK9degrader-11].

PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC CDK9 degrader with a DC50 of 1.09 nM. This compound exhibits cytotoxicity in small cell lung cancer (SCLC) cells, with IC50 values in the nanomolar range. It induces cell cycle arrest at the G0 G1 phase and inhibits cell invasion in DMS114 and DMS53 cells. In addition, PROTAC CDK9 degrader-11 shows antitumor activity in an NCI-H446 xenograft mouse model. (Pink: ligand for target protein CDK9 ligand 3; Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56)

CDK9ligand 3 is a ligand for CDK9 and can be utilized in the synthesis of PROTAC degraders, specifically PROTAC CDK9degrader-11.