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Merck
CN

P0115

PAC-1

≥98% (HPLC)

别名:

1-哌嗪乙酸,2-(苯基甲基)-,[[2-羟基-3-(2-丙烯基)苯基]亚甲基]肼, (4-苄基哌嗪)乙酸(3-烯丙基-2-羟基亚苄基)酰肼

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关于此项目

经验公式(希尔记法):
C23H28N4O2
化学文摘社编号:
分子量:
392.49
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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产品名称

PAC-1, ≥98% (HPLC)

InChI key

YQNRVGJCPCNMKT-LFVJCYFKSA-N

SMILES string

Oc1c(CC=C)cccc1\C=N\NC(=O)CN2CCN(CC2)Cc3ccccc3

InChI

1S/C23H28N4O2/c1-2-7-20-10-6-11-21(23(20)29)16-24-25-22(28)18-27-14-12-26(13-15-27)17-19-8-4-3-5-9-19/h2-6,8-11,16,29H,1,7,12-15,17-18H2,(H,25,28)/b24-16+

assay

≥98% (HPLC)

form

solid

color

white

solubility

DMSO: ≥10 mg/mL
deionized water: ≤2 mg/mL

storage temp.

room temp

Quality Level

Biochem/physiol Actions

PAC-1是半胱天冬酶3激活剂。
PAC-1是半胱天冬酶3激活剂。半胱天冬酶激活是癌症治疗中的关键策略。半胱天冬酶3是关键的执行子半胱天冬酶和细胞凋亡的直接效应子。许多癌症的标志是在执行子半胱天冬酶的激活和凋亡反应的丧失中规避信号。半胱天冬酶3激活的EC50=0.33 μM,半胱天冬酶7=4.5 μM。凋亡诱导的IC50=0.92 μM。癌细胞系和组织中半胱天冬酶3水平升高使PAC-1选择性诱导组织中的凋亡。

Features and Benefits

该化合物在受体分类和信号转导手册的 半胱天冬酶 页面上有详细描述。如需浏览其他手册页面,请点击此处

General description

蛋白酶激活化合物1(PAC-1)是邻羟基N-酰基肼化合物。它对多种癌细胞具有细胞毒性,例如淋巴瘤,白血病,乳腺癌和胶质母细胞瘤。高剂量的PAC-1可以促进神经兴奋。它有助于作为其他蛋白酶活化化合物原型的蛋白酶原的体外自活化。PAC-1依赖的procaspase-3激活与锌的螯合有关。

存储类别

11 - Combustible Solids

wgk

WGK 3

ppe

dust mask type N95 (US), Eyeshields, Gloves


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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访问文档库

Procaspase-3 activation as an anti-cancer strategy: structure- activity relationship of procaspase-activating compound 1 (PAC-1) and Its cellular co-localization with caspase-3
Peterson QP et al.
Journal of Medicinal Chemistry, 52(18), 5721-5731 (2009)
Philipp Blüm et al.
Cellular & molecular immunology, 14(12), 986-996 (2016-04-19)
Hepatitis C virus (HCV) infection is a major problem worldwide. HCV is not limited to liver disease but is frequently complicated by immune-mediated extrahepatic manifestations such as glomerulonephritis or vasculitis. A fatal complication of HCV-associated vascular disease is thrombosis. Polyriboinosinic:polyribocytidylic
Targeting of C-type lectin-like receptor 2 or P2Y12 for the prevention of platelet activation by immunotherapeutic CpG oligodeoxynucleotides: comment.
U Flierl et al.
Journal of thrombosis and haemostasis : JTH, 16(1), 181-185 (2017-10-21)
Michal Bijak et al.
International journal of biological macromolecules, 106, 878-884 (2017-08-27)
The primary biological function of platelets is to form hemostatic thrombi that prevent blood loss and maintain vascular integrity. These multi-responding cells are activated by different endogenous, physiological agonists due to the vast number of receptors present on the surface
Parallel synthesis and biological evaluation of 837 analogues of procaspase-activating compound 1 (PAC-1)
Hsu DC et al.
ACS Combinatorial Science, 14(1), 44-50 (2011)

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