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
CAS Number:
分子量:
392.49
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
质量水平
方案
≥98% (HPLC)
表单
solid
颜色
white
溶解性
DMSO: ≥10 mg/mL
deionized water: ≤2 mg/mL
储存温度
room temp
SMILES字符串
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+
InChI key
YQNRVGJCPCNMKT-LFVJCYFKSA-N
一般描述
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。
生化/生理作用
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。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
个人防护装备
dust mask type N95 (US), Eyeshields, Gloves
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
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)
Yingxue Qi et al.
Journal of hematology & oncology, 11(1), 117-117 (2018-09-19)
Platelet glycoprotein Ibα (GPIbα) extracellular domain, which is part of the receptor complex GPIb-IX-V, plays an important role in tumor metastasis. However, the mechanism through which GPIbα participates in the metastatic process remains unclear. In addition, potential bleeding complication remains
Amelie Vallet-Courbin et al.
PloS one, 12(1), e0170305-e0170305 (2017-01-27)
Cells of the innate and adaptive immune system are key factors in the progression of atherosclerotic plaque, leading to plaque instability and rupture, potentially resulting in acute atherothrombotic events such as coronary artery disease, cerebrovascular disease and peripheral arterial disease.
Derivatives of procaspase-activating compound 1 (PAC-1) and their anticancer activities
Roth SH and Hergenrother JP
Current Medicinal Chemistry, 23(3), 201-241 (2016)
Patrice Marques et al.
Frontiers in immunology, 8, 1766-1766 (2018-01-13)
Cardiovascular disease (CVD) is a major comorbidity in chronic obstructive pulmonary disease (COPD). Although the mechanism of its development remains largely unknown, it appears to be associated with cigarette consumption and reduced lung function. Therefore, the aim of this study
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