GNE-049 (GNE049) is a potent, selective, orally available inhibitor of CBP/p300 bromodomain with biochemical IC50 of 1.1/2.3 nM, respectively.
GNE-049 displays 3,850-fold selectivity over BRD4.
GNE-049 shows excellent potency (12 nM) in a BRET cellular assay and inhibits the expression of MYC with EC50 of 14 nM in MV-4-11 cells.
GNE-049 demonstrates significant dose-dependent inhibition of AR signaling and PC proliferation in vitro and in vivo.
