Chemical Structure : IACS-9571
CAS No.: 1800477-30-8
货号: 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.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥2580 | In stock | |
10 mg | ¥3980 | In stock | |
25 mg | ¥5880 | In stock | |
50 mg | Get quote | ||
100 mg | Get quote |
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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.
分子量 | 642.768 | |
分子式 | C32H42N4O8S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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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- |
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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