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Wnt-C59 Porcn/Wnt抑制劑
目錄號 MZ1001-10MG 售價 1480.00元
規格 10mg 運輸溫度 冰袋
其他名稱 Wnt C59; C59, Wnt Antagonist; PORCN Inhibitor II; 保存溫度 -20ºC干燥保存
CAS號 1243243-89-1 有效期 2年
應用 Porcn/Wnt抑制劑 訂購數量
產品簡介:

Wnt-C59 Porcn/Wnt抑制劑

 

產品標簽

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

 

產品信息

產品名稱                               

產品編號          

CAS NO.         

規格           

價格(元)  

Wnt-C59 Porcn/Wnt抑制劑

MZ1001-5MG

1243243-89-1

5mg

880

Wnt-C59 Porcn/Wnt抑制劑

MZ1001-10MG

1243243-89-1

10mg

1480

Wnt-C59 Porcn/Wnt抑制劑

MZ1001-25MG

1243243-89-1

25mg

2880

 

產品描述

Porcupine(Porcn)是一種膜結合O-脂肪酰轉移酶,介導Wnt家族蛋白的棕櫚?;揎?,這一步對Wnt蛋白的分泌和生物活性是必要的,Wnt蛋白在胚胎發育和癌癥中發揮重要作用。

 

Wnt-C59是一種非常有效和高度選擇性的Wnt信號通路拮抗劑,IC50約為74pM(Wnt信號報告基因實驗)。Wnt-C59通過Porcupine(Porcn)防止Wnt蛋白的棕櫚?;?,從而阻斷Wnt分泌和活性,作用方式類似于Wnt抑制劑IWP-2,IWP-3和IWP-4。但是Wnt-C59更加有效和選擇性更高,同時具更好的化學/物理特性,適合體外/體內研究。不管靜脈注射(2.5mg/kg)或口腔給藥(5mg/kg),血液中Wnt-C59的半衰期約1.94h。單一口服至少16h,血液中Wnt-C59仍維持高于體外IC50濃度的10倍以上。小鼠中Wnt-C59下調Wnt/ β- catenin通路靶向基因,同時能阻斷基底細胞樣(basal-like)和三陰性(triple-negative)乳腺癌。

 

產品特性

1)CAS NO:1243243-89-1

2)化學名:2-(4-(2-methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide

3)同義名:Wnt C59;C59, Wnt Antagonist;PORCN Inhibitor II;

4)分子式:C25H21N3O

5)分子量:379.45

6)純度:>98%

7)外觀:淺黃色固體

8)溶解性:溶于DMSO(50mM)

9)化學結構圖:

 

保存與運輸方法

保存:-20oC干燥保存,至少2年有效。

運輸:室溫運輸。

 

使用建議

體外:Wnt-C59(0.1-0.2 μM)用來完全阻斷Wnt蛋白分泌。當使用濃度為0.5 μM,許多實驗條件中Wnt-C59功能上能替代Dkk蛋白。

體內:小鼠口服Wnt-C59以每天每次5-10 mg/kg的用量或每天兩次5mg/kg的用量。

 

驗數據(文獻來源)

[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.

 

注意事項

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