您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > LY2940680
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:
 
LY2940680
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。
LY2940680图片
CAS NO:1258861-20-9
规格:98%
分子量:512.5
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
200mg电议

产品介绍
Hedgehog/SMO antagonist,inhibits Hh signaling
CAS:1258861-20-9
分子式:C26H24F4N6O
分子量:512.5
纯度:98%
存储:Store at -20°C

Background:

LY2940680 is a selective inhibitor of Smo receptor and thus inhibits Hh signaling pathway [1].


Smoothened(Smo) receptor is a member of class F G protein-coupled receptors, which plays an important role in the main transducer of the Hedgehog (Hh) signaling pathway that implicated in a wide range of developmental and adult processes [2].


LY2940680 is a potent Smo receptor inhibitor that binds mostly to extracelluar loops and has a different functioning site with the reported Smo receptor inhibitor SANT-1 which binds to 7TM [2]. When tested with cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patient with cancer who developed resistance to vismodegib, LY2940680 inhibited cell proliferation [3].


Many studies have shown that Hh signaling pathway plays a pivotal role in CSCs and Hh inhibition caused many aspects of transformation attributed to CSCs. In patients with basal cell carcinoma and medulloblastoma, LY2940680 showed good efficacy as a monotherapy [1].


参考文献:
[1].  Justilien, V. and A.P. Fields, Molecular pathways: novel approaches for improved therapeutic targeting of Hedgehog signaling in cancer stem cells. Clin Cancer Res, 2015. 21(3): p. 505-13.
[2].  Hoch, L., et al., MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor. Faseb j, 2015. 29(5): p. 1817-29.
[3].  Redmond, E.M., et al., Investigational Notch and Hedgehog inhibitors--therapies for cardiovascular disease. Expert Opin Investig Drugs, 2011. 20(12): p. 1649-64.