Synonyms: 5-(1-(1,3-Dimethoxypropan-2-yl)-5-morpholino-1H-benzo[d]imidazol-2-yl)-1,3-dimethylpyridin-2(1H)-one; 5-[1-[2-Methoxy-1-(methoxymethyl)ethyl]-5-(4-morpholinyl)-1H-benzimidazol-2-yl]-1,3-dimethyl-2(1H)-pyridinone
Molecular Formula: C23H30N4O4
Molecular Weight: 426.51
Linear Structural Formula: C23H30N4O4
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: I-BET469 is an orally active bromodomain (BrD) inhibitor with selectivity toward a subset of bromodomain-containng proteins (BCPs) and BrDs (Kd 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; Kd >=4.8 muM toward 22 other BCPs). I-BET469 targets cellular BRD4 with high affinity (pKd = 8.3 or Kd = 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.).