描述

Wnt-C59 Porcn/Wnt抑制剂

 

产品标签

Wnt-C59；Porcupine（Porcn）；IWP-2, Porcupine (Wnt) Inhibitor；Autophagy Inhibitor 自吞噬；CAS NO：1243243-89-1；

 

产品信息

产品名称	产品编号	CAS NO.	规格	价格（元）
Wnt-C59 Porcn/Wnt抑制剂	MZ1001-5MG	1243243-89-1	5mg	880
Wnt-C59 Porcn/Wnt抑制剂	MZ1001-10MG	1243243-89-1	10mg	1480
Wnt-C59 Porcn/Wnt抑制剂	MZ1001-25MG	1243243-89-1	25mg	2880

 

产品描述

Porcupine（Porcn）是一种膜结合O-脂肪酰转移酶，介导Wnt家族蛋白的棕榈酰化修饰，这一步对Wnt蛋白的分泌和生物活性是必要的，Wnt蛋白在胚胎发育和癌症中发挥重要作用。

 

Wnt-C59是一种非常有效和高度选择性的Wnt信号通路拮抗剂，IC50约为74pM（Wnt信号报告基因实验）。Wnt-C59通过Porcupine（Porcn）防止Wnt蛋白的棕榈酰化，从而阻断Wnt分泌和活性，作用方式类似于Wnt抑制剂IWP-2，IWP-3和IWP-4。但是Wnt-C59更加有效和选择性更高，同时具更好的化学/物理特性，适合体外/体内研究。不管静脉注射（2.5mg/kg）或口腔给药（5mg/kg），血液中Wnt-C59的半衰期约1.94h。单一口服至少16h，血液中Wnt-C59仍维持高于体外IC50浓度的10倍以上。小鼠中Wnt-C59下调Wnt/ β- catenin通路靶向基因，同时能阻断基底细胞样（basal-like）和三阴性（triple-negative）乳腺癌。

 

产品特性

1）CAS NO：1243243-89-1

2）化学名：2-(4-(2-methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide

3）同义名：Wnt C59;C59, Wnt Antagonist;PORCN Inhibitor II;

4）分子式：C25H21N3O

5）分子量：379.45

6）纯度：>98%

7）外观：浅黄色固体

8）溶解性：溶于DMSO（50mM）

9）化学结构图：

 

保存与运输方法

保存：-20ºC干燥保存，至少2年有效。

运输：室温运输。

 

使用建议

体外：Wnt-C59（0.1-0.2 µM）用来完全阻断Wnt蛋白分泌。当使用浓度为0.5 µM，许多实验条件中Wnt-C59功能上能替代Dkk蛋白。

体内：小鼠口服Wnt-C59以每天每次5-10 mg/kg的用量或每天两次5mg/kg的用量。

 

实验数据（文献来源）

[1] Chen B, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009;5(2):100-7.

[2]Dai Chen et al. (N-(HETERO)ARYL,2-(HETERO)ARYL-SUBSTITUTED ACETAMIDES FOR USE AS WNT SIGNALING MODULATORS. PCT WO/2010/101849.

[3] Willems E, et al. Small-molecule inhibitors of the Wnt pathway potently promote cardiomyocytes from human embryonic stem cell-derived mesoderm. (2011) Circ Res.109(4):360-4.

 

[4] 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.

In vitro assay: Stemness activity and Wnt-C59 treatment in NPC (nasopharyngeal carcinoma) cells. Method: 1 × 103cells were seeded for each well in the sphere inhibition assay. At 1 to 5 days after plating, all tested cells formed small spheres. Five days later, Wnt-C59 (1 μM, 5 μM, and 20 μM) wasadded into experimental groups. Abilities for cell growth and sphere images were compared and recorded at the end of the first, second, and third weeks after addition of Wnt-C59, or DMSO in control groups.

In vivo assay: Wnt-C59 suppresses tumor growth in animals. Method: A total of 1 × 107 cells in 200 μl DMEM were injected into 4-8 week old nude mice subcutaneously. Next day, mice were randomly divided into two groups, experimental and control, and were given Wnt-C59 via vein injection. Based on previous reports, Wnt-C59 was dissolved in 30% propylene glycol for intravenous tail vein administration (2.5 mg/kg). After 48 hours, Wnt-C59 was added into drinking water (5 mg/kg/day) for experimental groups. Fresh water with Wnt-C59 was changed every 48 hours in dark bottles avoiding light; water consumption was recorded and calculated. Mice in control groups were treated with injection of 30% propylene glycol and given fresh water containing DMSO.

 

[5] Motono M et al.WNT-C59, a Small-Molecule WNT Inhibitor, Efficiently Induces Anterior Cortex That Includes Cortical Motor Neurons From Human Pluripotent Stem Cells. Stem Cells Transl Med. 2016 Apr;5(4):552-60.

 

注意事项

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