Synonyms: IACS 009571-001-4 trifluoroacetate; N-(6-(3-(4-(Dimethylamino)butoxy)-5-propoxyphenoxy)-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-3,4-dimethoxybenzenesulfonamide trifluoroacetate; N-[6-[3-[4-(Dimethylamino)butoxy]-5-propoxyphenoxy]-2,3-dihydro-1,3-dimethyl-2-oxo-1H-benzimidazol-5-yl]-3,4-dimethoxybenzenesulfonamide trifluoroacetate
Molecular Formula: C32H42N4O8S · CF3CO2H
Molecular Weight: 756.79
Linear Structural Formula: C32H42N4O8S · CF3CO2H
Purity: >=98% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: IACS-9571 is a high-affinity, potent TRIM24/BRPF1 bromodomain (BrD) inhibitor (Kd = 1.3/2.1 nM by DiscoveRx) with good selectivity over other BrDs (BRPF2/3 Kd = 12/27 nM, BAZ2B/TAF1 BrD2/BRD4 BrD1,2 Kd = 0.4/1.8/>10 muM by DiscoveRx; <=63% binding inhibition of 25 other BrDs at 1 muM). IACS-9571 potently blocks H3K23Ac peptide from TRIM24 BrD binding (IC50 = 7.6 nM) and displaces ectopically expressed TRIM24 PHD-BrD from endogenous histone H3 in 2-hr 5 muM SAHA-stimulated HeLa cells (IC50 = 50 nM). When adiministered in mice, IACS-9571 exhibits good pharmacokinetics and oral availability in vivo (F = 29%, 10 mg/kg p.o.).