2074607-48-8|2-(5-Phenyl-4-(pyridin-4-yl)-1H-1,2,3-triazol-1-yl)-N-(5-phenylpyridin-2-yl)acetamide|CsnPharm

CAS No.: 2074607-48-8

IWP-O1 is highly potent Porcn inhibitor with EC50 value of 80 pM.

规格	价格	促销价格	库存	数量

400-920-2911

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生物活性

描述The acyltransferase Porcupine (Porcn) is essential for the secretion of Wnt proteins which contribute to embryonic development, tissue regeneration, and tumorigenesis^[1]. IWP-O1 is a Porcn inhibitor which suppresses Wnt signaling in L-Wnt-STF cells with an EC₅₀ value of 80 pM, 2.5 times more active than the investigational drug LGK974^[1]. IWP-O1 effectively suppressed the phosphorylation of Dvl2/3 in HeLa cells. At the same time, the phosphorylation of low density lipoprotein receptor-related protein 6 (LRP6), a hallmark of the Wnt/β-catenin pathway activity, was also suppressed by IWP-O1 treatment^[1]. IWP-O1, with a 1,2,3-triazole core, is much more stable in murine liver S9 fractions and plasma. In particular, no degradation was observed with IWP-O1 after incubation with murine liver S9 fractions for 4 h. With significantly improved metabolic stability, IWP-O1 is more suitable for model studies in mice^[1].
参考文献

实验方案

技术信息

CAS号

2074607-48-8

储存条件

分子式

C26H20N6O

运输

蓝冰

分子量

432.48

别名

溶解度

DMSO	36.0 mg/mL (83.2 mM)
Water	insoluble

动物实验配方

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