RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2 . RVX-297 shows IC 50 s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models.
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