Wnt-C59

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Chemical Structure| 1243243-89-1 同义名 : C59; PORCN Inhibitor II
CAS号 : 1243243-89-1
货号 : A321955
分子式 : C25H21N3O
纯度 : 99%+
分子量 : 379.45
MDL号 : MFCD22201167
存储条件：

Pure form Keep in dark place, inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 13 mg/mL clear

PO 0.5% CMC-Na 55 mg/mL suspension

生物活性
描述 Wnt-C59 (C59) effectively suppresses PORCN activity at nanomolar levels in vitro, evidenced by its ability to inhibit Wnt palmitoylation, the interaction of Wnt with its transporter Wntless/WLS, the secretion of Wnt, and the activation of β-catenin reporter activity by Wnt. It prevents WNT3A-induced activation of a TCF-binding site multimer driving luciferase production with an IC50 of 74 pM[1].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
human HT1080 cells Function assay Inhibition of porcupine activity (unknown origin) expressed in human HT1080 cells assessed as suppression of Wnt3A-mediated super top flash activity by STF luciferase assay, IC50=7.4e-05 μM. 26522946
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.64mL

0.53mL

0.26mL

13.18mL

2.64mL

1.32mL

26.35mL

5.27mL

2.64mL
参考文献

[1]Proffitt KD, et al. Pharmacological inhibition of the Wnt acyltransferase PORCN prevents growth of WNT-driven mammary cancer. Cancer Res. 2013 Jan 15;73(2):502-7.

[2]Cheng Y, et al. Wnt-C59 arrests stemness and suppresses growth of nasopharyngeal carcinoma in mice by inhibiting the Wnt pathway in the tumor microenvironment. Oncotarget. 2015 Jun 10;6(16):14428-39.