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ABBV-744 is an inhibitor of the bromodomain and extra-terminal domain (BET) family protein bromodomain 2 (BD2; Kis = 4.6, 4.9, 1.6, and 1 nM for BRD2, -3, -4, and -T, respectively).1 It is selective for BD2 over BD1 bromodomains in a time-resolved FRET (TR-FRET) assay (Kis = 1,162, 3,140, 521, and 917 nM for BRD2, -3, -4, and -T, respectively). ABBV-744 inhibits proliferation of SKM-1 leukemia cells (IC50 = 6.7 nM). It induces cell cycle arrest at the G1 phase in LNCaP prostate cancer cells.2 ABBV-744 (18.8 mg/kg) reduces tumor volume in a SKM-1 mouse xenograft model.1 It also reduces tumor growth in LNCaP and MDA PCa 2b mouse xenograft models when administered at doses of 1 and 4.7 mg/kg.2
WARNING This product is not for human or veterinary use.
1. Discovery of N-
2. Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer. Nature 578(7794), 306-310 (2020).