Potent, high affinity, selective BET bromodomain inhibitor (IC
values are 17.7, 32.6, 76.9 and 12942 nM for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively; K
values are 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). Induces squamous differentiation in NUT midline carcinoma (NMC) cell lines; inhibits tumor growth in NMC xenograft models
. Exhibits reversible contraceptive effects in germ cells from male mice.
Inactive Analog also available.
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This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the
(+)-JQ1 probe summary
on the SGC website.
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