您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > ML241
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:
 
ML241
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。
ML241图片
CAS NO:1346528-06-0
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
p97 ATPase inhibitor
Cas No.1346528-06-0
化学名2-(2H-benzo[b][1,4]oxazin-4(3H)-yl)-N-benzyl-5,6,7,8-tetrahydroquinazolin-4-amine
Canonical SMILESC1(CNC2=NC(N3CCOC4=CC=CC=C43)=NC5=C2CCCC5)=CC=CC=C1
分子式C23H24N4O
分子量372.46
溶解度Soluble 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: 100 nM

ML241 is identified as a potent and selective inhibitors of p97 ATPase.

The p97 AAA (ATPase associated with diverse cellular activities), also called VCP (valosin-containing protein), is an critical therapeutic target for cancer and neurodegenerative diseases. p97 plays important roles in a broad array of cellular processes, such as degradation of misfolded membrane and secretory proteins, homotypic fusion of endoplasmic reticulum and Golgi membranes, membrane transport, Golgi membrane reassembly, cell division, regulation of myofibril assembly, regulation of protein aggregates, as well as autophagosome maturation.

In vitro: Previous study showed that both ML241 and its analog ML240 were able to inhibit p97 ATPase with IC(50) values of around 100 nM. Both ML241 and ML240 could inhibit degradation of a p97-dependent but not a p97-independent proteasome substrate in a dual-reporter cell line. In addition, both ML241 and ML240 could impair the endoplasmic-reticulum-associated degradation (ERAD) pathway. Unexpectedly, ML240 could potently stimulate the accumulation of LC3-II within minutes, inhibit cancer cell growth, and mobilize the executioner caspases 3 and 7 rapidly, whereas ML241 could not [1].

In vivo: Currently, there is no animal in vivo data published.

Clinical trial: Up to now, ML241 is still in the preclinical development stage.

Reference:
[1] Chou TF, et al.  Structure-activity relationship study reveals ML240 and ML241 as potent and selective inhibitors of p97 ATPase. ChemMedChem. 2013 Feb;8(2):297-312.