IACS-9571 TRIFLUOROACEATE (C005B-310838)

Biochem/physiol Actions

IACS-9571 is a dimethylamine analogue.

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 μM by DiscoveRx; ≤63% binding inhibition of 25 other BrDs at 1 μM). 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 μM 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.).

UPC:

12352200

Condition:

New

Weight:

1.00 Ounces

HazmatClass:

No

Quantity:

5

Unit of Measurement:

MG

MPN:

SML2335-5MG

CAS:

1883598-69-3

Controlled Substances and Cyanide:

Yes