所有图片(1)
别名:
2,4-二氯-a-(3,4-二氢-4-氧代-2(1H)-喹唑啉基)-β-氧代苯丙腈, Ciliobrevin A, Hedgehog通路抑制剂4
经验公式（希尔记法）:
C17H9Cl2N3O2
推荐产品
质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
off-white, off-white to orange
溶解性
DMSO: 10 mg/mL, clear
储存温度
2-8°C
SMILES字符串
Clc1ccc(c(Cl)c1)C(=O)\C(C#N)=C2\NC(=O)c3ccccc3N2
InChI
1S/C17H9Cl2N3O2/c18-9-5-6-10(13(19)7-9)15(23)12(8-20)16-21-14-4-2-1-3-11(14)17(24)22-16/h1-7,21H,(H,22,24)/b16-12+
InChI key
SESYPWCSIZUIAS-FOWTUZBSSA-N
应用
Hedgehog 通路抑制剂（HP1-4）已被用于抑制利什曼原虫中的动力蛋白 ATPase。
生化/生理作用
HPI-4 是一种 Hedgehog 途径抑制剂；纤毛生成抑制剂。Hedgehog（HH）信号传导途径是抗癌治疗的靶标。HH 途径中的关键信号分子 Smoothened 蛋白（Smo）已成为药理学干预的靶标，这导致产生了包括环巴胺在内的多种 Smo 拮抗剂。但是，Smo 的致癌形式对环巴胺具有抗性，因此鉴定下游效应蛋白（例如转录因子 Gli1 和 Gli2）的抑制剂非常重要。确定了四个抑制 Smo 下游 HH 途径的小分子，HPI-1、HPI-2、HPI-3 和 HPI-4。HPI-4 阻止了 SAG 激活 HH 途径，降低了 Smo 纤毛的积累，降低了组成型激活 HH 细胞系中的 HH 活性，并降低了 Gli1 和 Gli2 加工和稳定性。HPI-4 抑制小脑颗粒神经元前体细胞（HH 信号的重要模型）的增殖。HPI-4 处理的细胞中的纤毛被截断或缺失。据推测，HPI-4 的作用机制是直接通过纤毛的发生而引起的，从而导致 Gli1/Gli2 活性的破坏，这与环巴胺明显不同。
警示用语：
Warning
危险声明
危险分类
Acute Tox. 4 Oral - Aquatic Acute 1 - Aquatic Chronic 1
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
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