Epigenetic Reader Domain

dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.

MZ1 is a potent inducer of reversible, long-lasting and selective removal of BRD4 over BRD2 and BRD3.

ZXH-3-26 is a selective PROTAC BRD4 degrader with a DC50/5h (DC50/5h referring to half-maximal degradation after 5 hours of treatment) of ~ 5 nM.

VZ185 is a potent, fast, and selective dual BRD7/9 PROTAC degrader with DC50s of 4.5 and 1.8 nM, respectively.

dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology.

MZP-55 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 8 nM for Brd4BD2.

MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 4 nM for Brd4BD2.

AT6 is a PROTAC AT1 analogue, which is a highly selective bromodomain (Brd4) degrader.

BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.

PROTAC BET Degrader-1 is a potent BET degrader based on PROTAC, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.

PROTAC BRD9 Degrader-1 is a lead PROTAC BRD9 chemical degrader (IC50=13.5 nM), which can be used as a selective probe useful for the study of BAF complex biology.

dBET6 is a highly potent, selective and cell-permeable degrader of BET based on PROTAC, with an IC50 of 14 nM, and has antitumor activity.

TMX1 is a covalent molecular glue degrader targeting BRD4. It selectively recruits DCAF16 to the BRD4BD2 domain, inducing BRD4 degradation.

CBPD-409 is an orally active PROTAC degrader targeting CBP/p300, with a DC₅₀ of 0.2–0.4 nM. It shows potent antiproliferative activity in AR⁺ prostate cancer cell lines (VCaP, LNCaP, 22Rv1) with IC₅₀ values of 1.2–2.0 nM and demonstrates significant antitumor efficacy.

JET-209 is a potent PROTAC degrader targeting CBP and p300, with DC₅₀ values of 0.05 nM and 0.2 nM, respectively. It is composed of lenalidomide, a linker, and the bromodomain inhibitor GNE-207. JET-209 is a valuable tool for cancer research involving epigenetic regulation.

AU-15330 is a PROTAC degrader targeting the SWI/SNF chromatin remodeling ATPase subunits SMARCA2 and SMARCA4. It effectively suppresses tumor growth in prostate cancer xenograft models and enhances the therapeutic efficacy of the AR antagonist enzalutamide. AU-15330 also induces remission in castration-resistant prostate cancer models, demonstrating strong antitumor activity with a favorable safety profile.

AU-24118 is an orally bioavailable PROTAC degrader targeting the mSWI/SNF chromatin remodeling complex ATPases SMARCA2 and SMARCA4, as well as PBRM1. It offers a powerful approach for modulating epigenetic regulation and holds promise for the treatment of cancers driven by alterations in SWI/SNF complex components.