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IACS-9571

Chemical Structure : IACS-9571

CAS No.: 1800477-30-8

IACS-9571 (IACS9571)

Catalog No.: PC-63216Not For Human Use, Lab Use Only.

IACS-9571 is a potent, selective dual TRIM24-BRPF1 bromodomain inhibitor with Kd of 31 and 14 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

IACS-9571 is a potent, selective dual TRIM24-BRPF1 bromodomain inhibitor with Kd of 31 and 14 nM, respectively.
IACS-9571 displays 9- and 21-fold selectivity against BRPF2 and BRPF3, weaker affinities with BAZ2B (Kd= 400 nM) and the second domain of TAF1 (Kd=1,800 nM), and >7,700-fold selectivity versus BRD4 BD1 and BD2.
IACS-9571 demonstrates excellent cellular potency (EC50= 50 nM) and favorable pharmacokinetic properties.
IACS-9571 is a chemical probe to investigate biological and pharmacological role of TRIM24 and/or BRPF1 bromodomain inhibition in vitro and in vivo.

Physicochemical Properties

M.Wt 642.768
Formula C32H42N4O8S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Benzenesulfonamide, N-[6-[3-[4-(dimethylamino)butoxy]-5-propoxyphenoxy]-2,3-dihydro-1,3-dimethyl-2-oxo-1H-benzimidazol-5-yl]-3,4-dimethoxy-

References

1. Gechijian LN, et al. Nat Chem Biol. 2018 Mar 5. doi: 10.1038/s41589-018-0010-y.

2. Palmer WS, et al. J Med Chem. 2016 Feb 25;59(4):1440-54.

3. Zhan Y, et al. Epigenetics Chromatin. 2015 Sep 21;8:37.

4. Appikonda S, et al. J Biol Chem. 2018 Mar 9. pii: jbc.RA118.002233.

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