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GSK591
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。
GSK591图片
CAS NO:1616391-87-7
包装与价格:
包装价格(元)
5mg电议
25mg电议

产品介绍
GSK591 (EPZ015866) 是一种有效的选择性蛋白质甲基转移酶 5 (PRMT5) 抑制剂,IC50 为 4 nM。
Cas No.1616391-87-7
别名EPZ015866; GSK3203591
化学名(S)-2-(cyclobutylamino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)isonicotinamide
Canonical SMILESO=C(C1=CC(NC2CCC2)=NC=C1)NC[C@H](O)CN3CC4=C(C=CC=C4)CC3
分子式C22H28N4O2
分子量380.48
溶解度≥ 38mg/mL in DMSO
储存条件Store at -20℃
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

IC50: 4 nM

GSK591 is a PRMT5 inhibitor.

Protein arginine methyltransferase-5 (PRMT5) is found to have a critical role in various cellular processes such as tumorigenesis, and the overexpression of PRMT5 is observed in cell lines and primary patient samples derived from lymphomas, especially mantle cell lymphoma.

In vitro: By further optimization of EPZ015666, an extremely potent in vitro tool analog of EPZ015666, GSK591, was identified. GSK591 was found to maintain excellent selectivity against other PMT enzymes, which was similar to that of EPZ015666. In addition, GSK591 was shown to be an extremely potent compound suitable for in vitro studies with excellent HLM stability [1].

In vivo: In mouse PK studies, GSK591, EPZ015666 and their analogs showed moderate to high plasma clearance and a wide range of oral bioavailability. The volume of distribution values in these studies were from 0.6 to 45 L/kg. Further PK studies demonstrated that at 100 mg/kg in mouse, the unbound plasma concentration was equivalent to or above the IC90 for a period of 12 h, therefore, indicating that the BID dosing regimen of EPZ015666 was able to effectively inhibit PRMT5 in vivo [1].

Clinical trial: Up to now, GSK591 is still in the preclinical development stage.

Reference:
[1] Duncan KW et al.  Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666. ACS Med Chem Lett. 2015 Dec 2;7(2):162-6.