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IWP-O1

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Chemical Structure| 2074607-48-8 同义名 : -
CAS号 : 2074607-48-8
货号 : A1145740
分子式 : C26H20N6O
纯度 : 99%+
分子量 : 432.477
MDL号 : MFCD31697718
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(277.47 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.56mL

2.31mL

1.16mL

23.12mL

4.62mL

2.31mL
参考文献

[1]You L, Zhang C, Yarravarapu N, Morlock L, Wang X, Zhang L, Williams NS, Lum L, Chen C. Development of a triazole class of highly potent Porcn inhibitors. Bioorg Med Chem Lett. 2016 Dec 15;26(24):5891-5895. doi: 10.1016/j.bmcl.2016.11.012. Epub 2016 Nov 11. PMID: 27876319; PMCID: PMC5142825.