degrader

Homo-PROTAC pVHL30 degrader 1 is a potent PROTAC-based degrader of pVHL30.

PROTAC Bcl2 degrader-1 is a PROTAC, which potently and selectively induces the degradation of Mcl-1 (IC50: 11.81 μM) and Bcl-2 (IC50: 4.94 μM; DC50: 3.0 μM).

PROTAC CDK2/9 Degrader-1 is a potent CDK2 and CDK9 dual degrader(DC50 of 62 nM and 33 nM).

PROTAC EED degrader-1, a PROTAC targeting EED (pKD = 9.02), is an inhibitor of polycomb repressive complex 2 (PRC2) with a pIC50 of 8.17.

PROTAC EED degrader-2 is a PROTAC targeting EED (pKD of 9.27) and an inhibitor of polycomb repressive complex 2 (PRC2) with a pIC50 of 8.11.

PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD) with an IC50 of 0.6 nM and exhibits anti-proliferative activity.

PROTAC B-Raf degrader 1 is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf,PROTAC B-Raf degrader 1 With anti-cancer activity.

PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins, with an IC50 of 9.6 nM.

PROTAC BRD9 Degrader-1 is a leading PROTAC BRD9 chemical degrader with an IC50 of 13.5 nM.

PROTAC BRD4 Degrader-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 nM).

PROTAC BRD4 Degrader-2 is an efficacious degrader of PROTAC BRD4(BRD4 BD1,IC50 of 14.2 nM).

PROTAC BRD4 Degrader-3 is an efficacious degrader of PROTAC BRD4.

PROTAC CRABP-II Degrader-1 is a potent degrader of cellular retinoic acid binding protein (CRABP-II) based on cIAp1.

PROTAC CRABP-II Degrader-2 is a potent cIAp1-based degrader of cellular retinoic acid binding protein (CRABP-II).

PROTAC CRABP-II Degrader-3 is a potent degrader of cellular retinoic acid binding protein (CRABP-II) based on [cIAp1].

PROTAC ER Degrader-4 is a PROTAC degrader of the estrogen receptor (ER) with an IC50 of 0.8 nM.

PROTAC FAK degrader 1 is a selective and potent degrader of focal adhesion kinase (Fak) with an IC50 of 6.5 nM.

PROTAC IRAK4 degrader-1 (compound I-210) is a Cereblon based PROTAC consisting of the PROTAC IRAK4 ligand-1, the E3 ligase ligand Pomalidomide and the PROTAC linker AM-Imidazole-PA-Boc.

PROTAC K-Ras Degrader-1 is a PROTAC degrader based on the Cereblon E3 ligand, capable of degrading K-Ras.

PROTAC RIPK degrader-2 is a nonpeptidic PROTAC ,and potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation.

PROTAC BET Degrader-1 is a potent BET degrader utilizing the PROTAC mechanism.

PROTAC BET Degrader-3 is a potent degrader of BET proteins based on the PROTAC (PROteolysis TArgeting Chimera) technology.

PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC that acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s > 100 μM)[1].

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[1].