ZEN-3219 is a BET inhibitor with IC50 s of 0.48, 0.16 and 0.47 μM for BRD4 (BD1), BRD4 (BD2) and BRD4 (BD1BD2), respectively. ZEN-3219 can be used to form PROTAC s to induce degradation of BRD4 [1].
References:
[1]. Kharenko OA, et al. Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine. J Med Chem. 2018 Sep 27;61(18):8202-8211.
References:
[1]. Kharenko OA, et al. Design and Characterization of Novel Covalent Bromodomain and Extra-Terminal Domain (BET) Inhibitors Targeting a Methionine. J Med Chem. 2018 Sep 27;61(18):8202-8211.
















