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| | N′-(2-ヒドロキシ-3-アリルベンジリデン)(4-ベンジルピペラジノ)アセトヒドラジド 製品概要 |
| 化学名: | N′-(2-ヒドロキシ-3-アリルベンジリデン)(4-ベンジルピペラジノ)アセトヒドラジド | | 英語化学名: | PAC1 | | 别名: | PAC1;4-(Phenylmethyl)-1-piperazineaceticacid[[2-hydroxy-3-(2-propenyl)phenyl]methylene]hydrazide;PAC1,4-(PhenylMethyl)-1-piperazineaceticacid[[2-hydroxy-3-(2-propenyl)phenyl]Methylene]hydrazide;4-(Phenylmethyl)-1-piperazineacetic acid 2-[[2-hydroxy-3-(2-propen-1-yl)phenyl]methylene]hydrazide;PAC-1,PAC1;Procaspase activating coMpound 1;(E)-N'-(3-allyl-2-hydroxybenzylidene)-2-(4-benzylpiperazin-1-yl)acetohydrazide;4-(Phenylmethyl)-1-piperazineacetic acid 2-[[2-hydroxy-3-(2-propen-1-yl)phenyl]methylene]hydrazide PAC-1 | | CAS番号: | 315183-21-2 | | 分子式: | C23H28N4O2 | | 分子量: | 392.49 | | EINECS: | | | カテゴリ情報: | Inhibitor;Inhibitors | | Mol File: | 315183-21-2.mol |  |
| | N′-(2-ヒドロキシ-3-アリルベンジリデン)(4-ベンジルピペラジノ)アセトヒドラジド 物理性質 |
| 比重(密度) | 1.14 | | 貯蔵温度 | Store at +4°C | | 溶解性 | DMSO: ≥10mg/mL | | 外見 | solid | | 酸解離定数(Pka) | 8.82±0.40(Predicted) | | 色 | white | | 安定性： | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol must be stored under inert gas at -80°C and will be stable for up to 2 months. |
| | N′-(2-ヒドロキシ-3-アリルベンジリデン)(4-ベンジルピペラジノ)アセトヒドラジド Usage And Synthesis |
| 説明 | PAC-1 (315183-21-2) is a procaspase-activating compound, directly activating procaspase-3, producing caspase-3, EC50=0.22 μM.1 It is less potent at activating procaspase-7, EC50=4.5 μM. It induces apoptosis in a variety of cancer cell lines. The mechanism of activation involves sequestering inhibitory zinc ions thus allowing procaspase-3 to autoactivate.2?? Sensitizes cancer cells to various chemotherapeutic agents.3 | | 使用 | PAC-1 is a potent procaspase-3 activator with EC50 of 0.22 μM. | | 生物活性 | Procaspase-activating compound; activates procaspase-3 to produce caspase-3 (EC 50 = 0.22 μ M). Also activates procaspase-7 in a less efficient manner (EC 50 = 4.5 μ M). Pro-apoptotic; induces apoptosis in both cancerous and non-cancerous cells dependent on procaspase-3 concentration (IC 50 values are 0.003-1.41 and 5.02-9.98 μ M respectively). | | 貯蔵 | +4°C | | 参考文献 | 1) Putt et al. (2006), Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy; Nat. Chem. Biol., 2 543
2) Peterson et al. (2009), PAC-1 activates procaspase-3 in vitro through relief of zinc-mediated inhibition; J. Mol. Biol., 388 144
3) Bolham et al. (2016), Small-Molecule Procaspase-3 Activation Sensitizes Cancer to Treatment with diverse Chemotherapeutics; ACS Cent. Sci., 2 545 |
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