您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > GSK-LSD1 2HCl
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
GSK-LSD1 2HCl
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。
GSK-LSD1 2HCl图片
CAS NO:1431368-48-7
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
25mg电议
100mg电议

产品介绍
irreversible, and selective LSD1 inhibitor
Cas No.1431368-48-7
化学名N-((1R,2S)-2-phenylcyclopropyl)piperidin-4-amine
Canonical SMILESC1(N[C@@H]2C[C@H]2C3=CC=CC=C3)CCNCC1
分子式C14H22Cl2N2
分子量289.24
溶解度≥ 11.55mg/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

GSK-LSD1 2HCl is a selective inhibitor of LSD1 with IC50 value of 16 nM [1].

Lysine (K) -specific demethylase 1A (LSD1) is a flavin-dependent histone demethylase that demethylates mono- and di-methylated lysines and plays an important role in oocyte growth, embryogenesis and tissue-specific differentiation. LSD1 plays a role in acute myeloid leukemia (AML).

GSK-LSD1 2HCl irreversibly inhibited LSD1 with IC50 value of 16 nM and is >1000 fold selective over LSD2, MAO-A and MAO-B, which were related to FAD utilizing enzymes. In cancer cell lines, GSK-LSD1 2HCl changed gene expression with average EC50 value< 5 nM and inhibited cells growth with average EC50 value< 5 nM. GSK-LSD1 2HCl (10 ?M) inhibited human recombinant dopamine transporter, 5-HT1A and 5-HT transporter by 39%, 49% and 74%, respectively. And no activity against other 55 recombinant receptors (GPCR, transporters, ion channels). GSK-LSD1 2HCl can be used as a chemical probe and a part of the SGC epigenetics [1].

Reference:
[1].  Structural Genomics Consortium.
http://www. thesgc.org/chemical-probes/LSD1.