SRX3254

SRX3254 is a novel small-molecule, highly potent and selective inhibitor of the binding domain 1 (BD1) of the bromodomain protein BRD4 (BRD4-BD1). It was discovered through in silico design using SignalRx Pharmaceuticals Inc.'s proprietary CRIMP technology platform. The drug exhibits 41-fold selectivity over the closely related binding domain 2 of BRD4 (BRD4-BD2). This selectivity is considered a significant breakthrough, as the inhibition of BRD4-BD1 alone is deemed necessary and sufficient for anti-cancer activity, while the simultaneous inhibition of BRD4-BD2 has been associated with toxicity issues in preclinical and clinical trials. SignalRx Pharmaceuticals Inc. is developing SRX3254 for the treatment of cancer.