H4541
HPI-4
≥98% (HPLC)
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
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关于此项目
经验公式（希尔记法）:
C17H9Cl2N3O2
化学文摘社编号:
分子量:
358.18
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
51111800
MDL number:
Quality Level
assay
≥98% (HPLC)
form
powder
color
off-white, off-white to orange
solubility
DMSO: 10 mg/mL, clear
storage temp.
2-8°C
SMILES string
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
Application
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。
Biochem/physiol Actions
HPI-4 是一种 Hedgehog 途径抑制剂；纤毛生成抑制剂。
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。
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral - Aquatic Acute 1 - Aquatic Chronic 1
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Wei Xiang et al.
Oncology reports, 32(4), 1622-1630 (2014-08-12)
Chondrosarcoma is a type of malignant bone tumor secreting cartilage-like matrix. In clinical treatment, there is no frequently used drug treatment option except for surgical resection. Hedgehog (HH) pathway is a classical signaling pathway that regulates normal cartilage cell development.
Ivonne Bernal et al.
Protein science : a publication of the Protein Society, 28(10), 1888-1901 (2019-08-09)
Translocation of virulence effector proteins through the type III secretion system (T3SS) is essential for the virulence of many medically relevant Gram-negative bacteria. The T3SS ATPases are conserved components that specifically recognize chaperone-effector complexes and energize effector secretion through the
Ivonne Bernal et al.
Journal of molecular biology, 431(19), 3787-3803 (2019-07-10)
Many medically relevant Gram-negative bacteria use the type III secretion system (T3SS) to translocate effector proteins into the host for their invasion and intracellular survival. A multi-protein complex located at the cytosolic interface of the T3SS is proposed to act
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| H4541-25MG | 04061833218983 |
| H4541-5MG | 04061833218990 |