N-((3-氟-2'-甲基-[2,4'-联吡啶]-5-基)甲基)-9H-咔唑-2-甲酰胺

• 常用名: N-((3-氟-2'-甲基-[2,4'-联吡啶]-5-基)甲基)-9H-咔唑-2-甲酰胺
• 英文名: Porcupine-IN-1
• CAS号: 2036044-77-4
• 分子量: 410.44
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₅H₁₉FN₄O
• 熔点: N/A
• 闪点: N/A

用途

Porcupine-IN-1是有效的 porcupine 抑制剂,IC50 值为0.5±0.2 nM。

名称

• 中文名: 豪猪-IN-1
• 英文名: Porcupine-IN-1

生物活性

• 描述: Porcupine-IN-1是有效的 porcupine 抑制剂,IC50 值为0.5±0.2 nM。
• 相关类别:
  信号通路 >> 干细胞及 Wnt 通路 >> 豪猪
  研究领域 >> 癌症
• 靶点实验:

  IC50: 0.5±0.2 nM (Porcupine inhibitor)[1]

• 体外研究: Porcupine是一种催化棕榈油酸酯加入Wnt蛋白中丝氨酸残基的酶,这是Wnt蛋白分泌所必需的过程。在基于细胞的STF报道基因测定中,Porcupine-IN-1与临床化合物LGK974一样有效。 Porcupine-IN-1有效抑制Wnt3A的分泌,因此被证实是一种豪猪抑制剂[1]。
• 体内研究: Porcupine-IN-1在人肝微粒体(57 mL/min/kg)和大鼠肝微粒体(24 mL/min/kg)处理下表现出中等清除率。当用小鼠微粒体(109 mL/min/kg)处理时,它表现出高清除率[1]。
• 细胞实验: 用pLinbin-Wnt3A质粒或载体对照转染HEK293T细胞。然后用或不用化合物（Porcupine-IN-1）处理HEK293T细胞。 48小时后使用Western Blot分析细胞裂解和培养基[1]。
• 参考文献:

  [1]. Xu Z, et al. Design, synthesis, and evaluation of novel porcupine inhibitors featuring a fused 3-ring system based on the 'reversed' amide scaffold.

物理化学性质

• 分子式: C₂₅H₁₉FN₄O
• 分子量: 410.44
• 储存条件: 2-8°C，干燥密封

靶点实验

查看更多实验

实验名称：Inhibition of smo-mediated hedgehog signaling pathway in mouse NIH3T3-Luc cells asses... 来源：ChEMBL 靶标：Smoothened homolog External Id：CHEMBL4197879

实验名称：Cytotoxicity against human GES-1 cells up to 20 uM by Cell Titer-Glo assay 来源：ChEMBL 靶标：GES1 External Id：CHEMBL4197878

实验名称：Inhibition of smo-mediated hedgehog signaling pathway in mouse NIH3T3-Luc cells asses... 来源：ChEMBL 靶标：Smoothened homolog External Id：CHEMBL4197881

实验名称：Inhibition of porcupine-mediated Wnt/beta-catenin signaling in human PA1 cells assess... 来源：ChEMBL 靶标：Protein-serine O-palmitoleoyltransferase porcupine External Id：CHEMBL4197875

实验名称：Inhibition of porcupine-mediated Wnt/beta-catenin signaling in human PA1 cells assess... 来源：ChEMBL 靶标：Protein-serine O-palmitoleoyltransferase porcupine External Id：CHEMBL4197874

实验名称：Cytotoxicity against primary astrocytes (unknown origin) up to 20 uM after 24 hrs by ... 来源：ChEMBL 靶标：Astrocyte External Id：CHEMBL4197877

实验名称：Inhibition of smo-mediated hedgehog signaling pathway in mouse NIH3T3 cells expressin... 来源：ChEMBL 靶标：Smoothened homolog External Id：CHEMBL4197876

实验名称：Chemical stability in simulated gastric fluid assessed as remaining compound levels a... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3861544

实验名称：Metabolic stability in rat plasma assessed as remaining compound levels at 1 uM after... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3861545

实验名称：Intrinsic clearance in human liver microsomes at 1 uM preincubated for 10 mins follow... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3861546

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英文别名

• MFCD31630804