IACS-9571 TRIFLUOROACEATE

IACS-9571 TRIFLUOROACEATE

Stock Code: 3576161
Manufacturer Part No: SML2335-25MG
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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 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.).


IACS-9571 is a dimethylamine analogue.

Colourwhite to beige
ManufacturerSIGMA-ALDRICH
Storage Temp.2-8°C
SolubilityDMSO: 2 mg/mL, clear
Formpowder
Assay≥98% (HPLC)

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