(+)-JQ1

(+)-JQ1 binds to all bromodomains of the BET family with IC50 values of 17.7, 32.6, 76.9 and 12942 nM for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively; Kd values of 49, 59.5, 82, 90.1, 128 and 190 nM for BRD4 (N), BRD3 (N), BRD3 (C), BRD4 (C), BRD2 (N) and BRDT (N) respectively. (+)-JQ1 inhibits tumor growth in NMC xenograft models in vivo. (+)-JQ1 induces squamous differentiation in NUT midline carcinoma (NMC) cell lines. The BET bromodomain inhibitor (+)-JQ1 (5 μM) dissociates Brd4 from the HIV promoter to allow Tat recruitment of SEC to stimulate HIV elongation. (+)-JQ1 has been used as a chemical probe to investigate the role of BET bromodomains in the transcriptional regulation of oncogenesis. (+)-JQ1 (50 mg/kg i.p.) leads to a highly significant increase in survival of mice bearing Raji xenografts. (+)-JQ1 is more effective than (-)-JQ1.