产品说明
一般描述
A cell-permeable phenylimidazopyridinyl-methoxy coumarin compound that inhibits caspase-3 and caspase-6 activities (IC50 = 35 and 38 µM, respectively) by targeting both the large and small subunit active sites. Kinetic studies with 1541 and its 8-Hydroxy analog (Cat. No. 529663) indicate that at suboptimal inhibitor : proenzyme molar ratio (100:1 or less), the compound does not effectively occupies both active sites of and stabilizes the proenzyme in an “on-state” conformation that facilitates the subsequent autoproteolysis or autoactivation process via the unoccupied active site of procaspase-3 and -6 (EC50 = 2.4 and 2.8 µM, respectively). Shown to effectively induce apoptosis (up to 50 µM) in various cancer cell lines (IC50 ranges from 3.8 to 8.7 µM) in a caspase-3-dependent, but p53-, caspase-8-, and Bak-independent manner. Exhibits little inhibitory effect against active caspase-7 (30 nM) even at concentrations as high as 50 µM, nor does it activate procaspase-1 or -7 even after prolonged incubations upto 4 and 24 h, respectively.
A cell-permeable phenylimidazopyridinyl-methoxy coumarin compound that inhibits caspase-3 and caspase-6 activities (IC50 = 35 and 38 µM, respectively) by targeting both the large and small subunit active sites. Kinetic studies with 1541 and its 8-Hydroxy analog (Cat. No. 529663) indicate that at suboptimal inhibitor : proenzyme molar ratio (100:1 or less), the compound does not effectively occupies both active sites of and stabilizes the proenzyme in an “on-state” conformation that facilitates the subsequent autoproteolysis or autoactivation process via the unoccupied active site of procaspase-3 and -6 (EC50 = 2.4 and 2.8 µM, respectively). Shown to effectively induce apoptosis (up to 50 µM) in various cancer cell lines (IC50 ranges from 3.8 to 8.7 µM) in a caspase-3-dependent, but p53-, caspase-8-, and Bak-independent manner. Exhibits little inhibitory effect against active caspase-7 (30 nM) even at concentrations as high as 50 µM, nor does it activate procaspase-1 or -7 even after prolonged incubations upto 4 and 24 h, respectively.
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C24H17N3O4 |
分子量 | 411.41 |
产品性质
质量水平 | 100 |
测定 | ≥95% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
颜色 | yellow |
溶解性 | DMSO: 5 mg/mL |
运输 | ambient |
储存温度 | 2-8℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |