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Wnt-C59

Wnt-C59

产品编号 T2242   CAS 1243243-89-1
别名: 4-(2-甲基-4-吡啶基)-N-[4-(3-吡啶基)苯基]苯乙酰胺, C59

Wnt-C59 (C59) 是一种高效的、口服具有活力的PORCN 抑制剂(IC50:74 pM)。

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Wnt-C59 Chemical Structure
Wnt-C59, CAS 1243243-89-1
规格 价格/CNY 货期 数量
1 mg ¥ 233 现货
2 mg ¥ 329 现货
5 mg ¥ 536 现货
10 mg ¥ 828 现货
25 mg ¥ 1,590 现货
50 mg ¥ 2,480 现货
100 mg ¥ 3,880 现货
1 mL * 10 mM (in DMSO) ¥ 659 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: Wnt-C59 (T2242)
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纯度: 99.91%
纯度: 99.56%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Wnt-C59 (C59)(C59) is a highly effective and specific Wnt signaling antagonis with PORCN enzymatic activity.
靶点活性 Porcn:74 pM
体外活性 在原位移植独立性MMTV-WNT1肿瘤的雌性裸鼠中,Wnt-C59(10 mg/kg)能够降低β-catenin靶向基因的表达,降低Wnt通路活性,抑制肿瘤细胞生长.14CREER/Rosa-SmoM2小鼠中,Wnt-C59(5 mg/kg)局部给药能够抑制细胞增殖.
体内活性 在转染PORCN的无PORCN HT1080细胞中,Wnt-C59(100 nM )抑制PORCN活性。在转染WNT3A-V5的HeLa细胞中,Wnt-C59(10 -100 nM)能够抑制PORCN酰基转移酶活性。
激酶实验 Aurora A radioactive Flashplate enzyme assay: Aurora A radioactive Flashplate enzyme assay is conducted to determine the nature and degree of MLN8237-mediated inhibition in vitro. Recombinant Aurora A is expressed in Sf9 cells and purified with GST affinity chromatography. The peptide substrate for Aurora A is conjugated with biotin (Biotin-GLRRASLG). Aurora A kinase (5 nM) is assayed in 50 mM Hepes (pH 7.5), 10 mM MgCl2, 5 mM DTT, 0.05% Tween 20, 2 μM peptide substrate, 3.3 μCi/mL [γ-33P]ATP at 2 μM, and increasing concentrations of MLN8237 by using Image FlashPlates.
细胞实验 Wnt-C59 (C59) is dissolved in DMSO (10 mM) and stored, and then diluted with appropriate medium before use[1]. Approximately, 1×104 cells are seeded in 24-well plates, and Wnt-C59 (5 μM, 10 μM, and 20 μM) is added the next day. Each group is tested in triplicate and control groups with addition of DMSO are also established. Cell confluence is determined by microscopy at 24, 48, 72, and 96 hours after seeding of cells. The IC50 of Wnt-C59 is determined by MTT assay, using 96-well dishes. Next day, various concentrations of Wnt-C59 are added, and cellular viabilities are measured by a spectrophotometer at both 24 and 48 hours. For sphere formation, approximately one hundred cells are seeded onto the Low Cell Bind Surface 24-well Nunc dish. Each group is done in triplicate and each well had 2 mL medium. Media are changed twice a week, and only half of the media is changed each time. Approximately, 1×103 cells are 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) is added into experimental groups. Abilities for cell growth and sphere images are compared and recorded at the end of the first, second, and third weeks after addition of Wnt-C59, or DMSO in control groups. The sphere growths are observed and recorded daily under microscopy, and the area of spheres is analyzed using Metamorph and recorded as average area (μm2)[1].
别名 4-(2-甲基-4-吡啶基)-N-[4-(3-吡啶基)苯基]苯乙酰胺, C59
分子量 379.45
分子式 C25H21N3O
CAS No. 1243243-89-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 7.6 mg/mL (20 mM)

DMSO: 7.6 mg/mL (20 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.6354 mL 13.177 mL 26.3539 mL 65.8848 mL
5 mM 0.5271 mL 2.6354 mL 5.2708 mL 13.177 mL
10 mM 0.2635 mL 1.3177 mL 2.6354 mL 6.5885 mL
20 mM 0.1318 mL 0.6588 mL 1.3177 mL 3.2942 mL

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TargetMol Library Books参考文献

1. Proffitt KD, et al. Cancer Res, 2013, 73(2), 502-507. 2. Wend P, et al. EMBO Mol Med, 2013, 5(2), 264-279. 3. Petrova E, et al. Nat Chem Biol, 2013, 9(4), 247-249. 4. Youssef KK, et al. Nat Cell Biol, 2012, 14(12), 1282-1294.

TargetMol Library Books文献引用

1. Zhang, Linhao, et al. Inhibition of cyclooxygenase‐2 enhanced intestinal epithelial homeostasis via suppressing β‐catenin signalling pathway in experimental liver fibrosis. Journal of Cellular and Molecular Medicine. 2021
DK419 β-catenin modulator IIa-661 Astragaloside I Wogonin KY1220 BML-284 JW 55 4,10-Aromadendranediol

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 神经元分化化合物库 细胞骨架化合物库 抗衰老化合物库 细胞重编程化合物库 抗肺癌化合物库 口服活性化合物库 Wnt/Hedgehog/Notch 通路化合物库 干细胞分化化合物库 抗卵巢癌化合物库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Wnt-C59 1243243-89-1 Cytoskeletal Signaling Stem Cells Wnt/beta-catenin Porcupine Wnt WntC59 Inhibitor 4-(2-甲基-4-吡啶基)-N-[4-(3-吡啶基)苯基]苯乙酰胺 C59 Wnt-C-59 inhibit C 59 C-59 Wnt C59 inhibitor

 

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