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IACS-9571 Hydrochloride(ASIS-P040 Hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
IACS-9571 Hydrochloride(ASIS-P040 Hydrochloride)图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)询价
1mg询价
5mg询价
10mg询价
50mg询价
100mg询价

IACS-9571Hydrochloride是溴结构域蛋白TRIM24和BRPF1的抑制剂,对TRIM24的IC50和Kd值分别为8nM和31nM,对BRPF1的Kd值为14nM。
Canonical SMILES[H]Cl.O=S(C1=CC=C(OC)C(OC)=C1)(NC2=C(OC3=CC(OCCC)=CC(OCCCCN(C)C)=C3)C=C(N4C)C(N(C)C4=O)=C2)=O
分子式C32H43ClN4O8S
分子量679.22
溶解度DMSO : 125 mg/mL (184.03 mM);Water : 10 mg/mL (14.72 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IACS-9571 Hydrochloride is a potent and selective inhibitor of TRIM24 and BRPF1, with an IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.

IACS-9571 Hydrochloride shows excellent cellular potency with EC50 of 50 nM. IACS-9571 Hydrochloride (1 μM) has potent activities against a panel of 32 bromodomains. IACS-9571 Hydrochloride is a selective dual TRIM24/BRPF1 inhibitor (Kd=1.3/2.1 nM) with 9- and 21-fold selectivity against BRPF2 and BRPF3, respectively. IACS-9571 Hydrochloride does not interact with the BET sub-family of bromodomains, displaying greater than 7700-fold selectivity versus BRD4 (1, 2) relative to TRIM24[1].

[1]. Palmer WS, et al. Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. J Med Chem. 2016 Feb 25;59(4):1440-54.

 
 
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