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IWP-2
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-2图片
CAS NO:686770-61-6
规格:98%
分子量:466.6
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
Wnt production inhibitor,PORCN inhibitor
CAS:686770-61-6
分子式:C22H18N4O2S3
分子量:466.6
纯度:98%
存储:Store at -20°C

Background:

IC50: 27 nM for Wnt pathway activity


The Wnt signaling pathway is important in embryonic devel_x001F_opment as well as the initiation and progression of a number of types of human cancer. Porcn, a member of the membrane-bound O-acyltransferase (MBOAT) family, adds a palmitoyl group to Wnt proteins that is essential to their signaling ability and is required for Wnt secretion. IWP-2 is a small-molecule antagonist of the Wnt/b-catenin pathway.


In vitro: Expression of Porcn but not Evi alleviated the effects of IWP-2 on pathway activity and Wnt secretion, which suggests that in general IWP-2 may act on Porcn [1].


In vivo: In order to test the in vivo activity of IWP-2, the authors turned to a simple and rapid assay of Wnt/b-catenin pathway activity: regeneration of the zebrafish caudal fin following resection. The addition of IWP-2 to the aquarium water of zebrafish failed to suppress fin regeneration after mechanical resection, which suggests either that IWP-2 have poor bioavailability or that the determinants in the gene product that they target are not conserved in zebrafish [1].


Clinical trial: Up to now, IWP-2 is still in the preclinical development stage.


Reference:
[1] Chen B, Dodge ME, Tang W, Lu J, Ma Z, Fan CW, Wei S, Hao W, Kilgore J, Williams NS, Roth MG, Amatruda JF, Chen C, Lum L.  Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7.