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 > IWP-3
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:
 
IWP-3
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。
IWP-3图片
CAS NO:687561-60-0
规格:98%
分子量:484.6
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
inhibitor of Wnt production
CAS:687561-60-0
分子式:C22H17FN4O2S3
分子量:484.6
纯度:98%
存储:Store at -20°C

Background:

IC50: 40 nM


IWP-3 is an inhibitor of Wnt production.


Wnt signaling proteins, a group of small secreted proteins, are active in tissue homeostasis, embryonic development, as well as tumorigenesis. Wnt proteins can bind to the cell surface receptors, initiating a signaling cascade that results in the β-catenin activation of gene transcription.


In vitro: In previous study, IWP-3 was identified as an inhibitor of Wnt production that could regulate in vitro Wnt pathway activity with an IC50 value of 40 nM. In addition, IWP-3 was found to be able to inactivate porcupine, a O-acyltransferase for palmitoylating Wnt proteins that was critical for the signaling ability and secretion. Moreover, IWP-3 at 5 μM was found to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 and the scaffold protein Dishevelled, resulting in preventing the accumulation of β-catenin [1]. In another study, IWP-3 was applied to promote cardiomyocyte generation from human embryonic stem cells by inhibiting Wnt signaling [2].


In vivo: So far, there is no animal in vivo data reported.


Clinical trial: Up to now, IWP-3 is still in the preclinical development stage.


参考文献:
[1] B.  Chen, M. E. Dodge, W. Tang, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nature Chemical Biology 5(2), 100-107 (2009).
[2] E.  Willems, S. Spiering, H. Davidovics, et al. Small molecule inhibitors of the Wnt pathway potently promote cardiomyocytes from human embryonic stem cell derived mesoderm. Circulation Research 109(4), 360-364 (2011).