I-BET469，5MG，SML2825-5MG，Sigma

Biochem/physiol Actions

I-BET469 is an orally active bromodomain (BrD) inhibitor with selectivity toward a subset of bromodomain-containng proteins (BCPs) and BrDs (K_d in nM: BRD4 BrD1/2 = 1.5/2.9, BRD3 BrD1/2 = 2/2.3, BRD2 BrD1/2 = 2.3/2.8, BRDT BrD1/2 = 12/100, CREBBP = 37, EP300 = 49; K_d ≥4.8 μM toward 22 other BCPs). I-BET469 targets cellular BRD4 with high affinity (pK_d = 8.3 or K_d = 5.0 nM by NanoBRET) and shows in vivo efficacy in a murine acute endotoxic shock model (1, 3, 10 mg/kg po. 30 min prior to LPS) and a chronic T cell-dependent immunization model (IgG suppression on day 14 = 24% and 65%, respectively, with 0.3 mg/kg or 3 mg/kg daily po.).
Orally active bromodomain (BrD) inhibitor with in vivo efficacy and selectivity for BRD2/3/4, BRDT, CREBBP, EP300 over 22 other BCPs.