|XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity.
|THAL-SNS-032 is a selective PROTAC, consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN), targeting on CDK9.
|PROTAC CDK9 degrader-2
|PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC.
|CDK9 PROTAC compound 3
|PROTAC CDK9 Degrader-1 is a CRBN-recruiting PROTAC selectively targeting on CDK9, consist of a CDK9 ligand (aminopyrazole analog) linked to a CRBN E3 ligand thalidomide.
|JH-XI-10-02 is a PROTAC selectively targeting on CDK8 with IC50 value of 159nM, and is consist of a warhead target on CDK8 (a Cortistatin A derivate) linked to CRBN ligand Pomalidomide.
|CP-10 is a PROTAC targeting on CDK4/6 with DC50 values of 150-180 nM and 2.1 nM, respectively. It was generated by linking CDK6 inhibitor palbociclib and E3 ligase CRBN recruiter pomalidomide.
|BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC), with IC50s of 50.6 nM and 30 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-04-132 does not induce CDK6 and IKZF1/3 degradation. BSJ-04-132 has anti-cancer activity.
|BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 does not induce IKZF1/3 degradation and has anti-cancer activity.
|BSJ-03-123 is a PROTAC selectively targeting on CDK6, consist of a warhead palbociclib (a CDK inhibitor) linked to a CRBN ligand pomalidomide.