质量水平
检测方案
≥98% (HPLC)
形式
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。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。
WGK
WGK 3
个人防护装备
dust mask type N95 (US), Eyeshields, Gloves
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)
Ai-Ming Zhou et al.
BMC cardiovascular disorders, 20(1), 15-15 (2020-01-15)
Platelets in patients with type 2 diabetes mellitus (DM2) are characterized by increased activation and aggregation, which tends to be associated with a high morbidity and mortality due to cardiovascular disease (CVD). Moreover, a large proportion of DM2 patients show
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)
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
我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.
联系技术服务部门