dBET1 是一种由 BRD4 抑制剂 JQ1 与 NSC 527179 衍生物通过 linker 产生的 PROTAC，可诱导 BRD4 降解。它是由Cereblon配体和BRD4配体相连的PROTAC，其EC50值为 430 nM。

dBET1 is a hybrid molecule that combines (+)-JQ1 and thalidomide. It induces cereblon-dependent BET protein degradation in vitro (EC50: 430 nM) and induces apoptosis.

dBET1 induced a potent and superior inhibitory effect on MV4;11 cell proliferation at 24 hours (measured by ATP content, IC50 = 0.14 μM, compared to IC50 = 1.1 μM with JQ1) consistent with the reported, pronounced inhibitory effect of RNA silencing of BRD4 in this and other models of MLL-rearranged leukemia.

1799711-21-9

C38H37ClN8O7S

785.27

DMSO:50 mg/mL
H2O:Insoluble
Ethanol:5 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years