| Hazard Information | Back Directory | [Uses]
A bromodomain Inhibitor. This domain contains proteins that are involved in the epigenetic regulation of gene expression and have been implicated in human cancer. | [Biological Activity]
IACS-9571 is a dimethylamine analogue.''IACS-9571 is a high-affinitypotent TRIM24/BRPF1 bromodomain (BrD) inhibitor (Kd = 1.3/2.1 nM by DiscoveRx) with good selectivity over other BrDs (BRPF2/3 Kd = 12/27 nMBAZ2B/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 miceIACS-9571 exhibits good pharmacokinetics and oral availability in vivo (F = 29%10 mg/kg p.o.). |
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| Company Name: |
Merck KGaA
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| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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