Wnt信號通路是一個復(fù)雜的蛋白質(zhì)作用網(wǎng)絡(luò)，其功能zui常見于胚胎發(fā)育和癌癥，但也參與成年動物的正常生理過程。Wnt信號通路包括許多可調(diào)控Wnt信號分子合成的蛋白質(zhì)，它們與靶細(xì)胞上的受體相互作用，而靶細(xì)胞的生理反應(yīng)則來源于細(xì)胞和胞外Wnt配體的相互作用。

IWP-2:
N-(6-Methyl-2-benzothiazolyl)-2-[(3,4,6,7-tetrahydro-4-oxo-3-phenylthieno[3,2-d]pyrimidin-2-yl)thio]-acetamide, is a specific inhibitor of the O-acyltransferase Porcupine with IC50=27nM (Ref.). Inhibition blocks the production of Wnt proteins that require fatty acid modifications, thus disrupting Wnt-dependent signaling. Porcupine inhibitor represent a novel class of potential therapeutics for cancer and other WNT dependent diseases.

Ref: B. Chen, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat. Chem. Biol. 5, 100 (2009)

Purity:
Greater than 99.5% as determined by LC/MS analysis. LC/MS and/or NMR data available upon request.
Biological Activity:
In a cell-based assay measuring the activation of the TCF reporter gene, this compound gives IC50 of 30 nM.

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