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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 : 379.454
MDL号 : MFCD22201167
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(131.77 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：

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].
作用机制 Serine acylation in Wnt protein is essential in Wnt secretion. PORCN is a key enzyme that resides in the endoplasmic reticulum, adding palmitate to a serine in Wnt protein. Wnt-C59 acts as a nanomolar inhibitor of the acyltransferase activity of PORCN.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 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.