GSK778 (iBET-BD1), a chemical probe, is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC 50 s of 75 nM ( BRD2 BD1 ), 41 nM ( BRD3 BD1 ), 41 nM ( BRD4 BD1 ), and 143 nM ( BRDT BD1 ), respectively. GSK778 phenocopies the effects of pan- BET inhibitors in cancer models.
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