Selective CBP/p300 bromodomain inhibitor (IC50
values are 125 and 363 nM, respectively). Exhibits >100-fold selectivity for CBP over BRD4. Also exhibits selectivity over a panel of other bromodomains. Reduces LPS-induced IL-1β
expression in macrophages in vitro
. Also downregulates RGS4
expression in primary cortical neurons in vitro
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Other Product-Specific Information:
Transcriptional profiling of a selective CREB binding protein bromodomain inhibitor highlights therapeutic opportunities.
Chekler et al.