PAC-1
作者：齐岳
发布时间：2023-08-29
13:40:51
点击数：
产品名称：PAC-1
产品描述：
| 产品描述 | PAC-1 has been used in trials studying the treatment of Lymphoma, Melanoma, Solid Tumors, Breast Cancer, and Thoracic Cancers, among others. |
| 靶点活性 | Procaspase-3:0.22 μM(EC50) |
| 体外活性 | PAC-1由于激活procaspase-3和随后诱导凋亡发挥体内抗效果,与体外活性一致.用5 mg的稳定释放低剂量PAC-1处理小鼠,明显抑制ACHN肾移植瘤生长.用50或100 mg/kg PAC-1口服处理,明显剂量依赖性阻碍NCI-H226肺*移植瘤生长,且明显阻止*细胞浸润肺组织. |
| 体内活性 | PAC-1能够以延迟的方式诱导Bax/Bak双敲除细胞和Bcl-2和Bcl-xL过表达细胞中的细胞死亡,具有与野生型对应物相同的功效。PAC-1按caspase-3 非依赖性方式诱导细胞色素c释放,随后触发下游caspase-3激活和细胞死亡。PAC-1不能诱导Apaf-1敲除细胞中的细胞死亡和半胱天冬酶-3激活,这表明凋亡体形成对于通过PAC-1介导的细胞死亡的胱天蛋白酶-3激活是必需的。PAC-1诱导原发性*细胞凋亡,IC50值为3 nM至1.41 μM,比邻近的非*细胞更有效,IC50为5.02 μM至9.98 μM,这也与procaspase-3的浓度直接相关。PAC-1激活procaspase-3,产生caspase-3,EC50为 0.22 μM,且激活procaspase-7,EC50为 4.5 μM。*细胞系中增高的caspase 3水平使 PAC-1 选择性诱导凋亡,按与procaspase-3 浓度成比例的方式,NCI-H226细胞的IC50为0.35 μM,UACC-62细胞的IC50为约3.5 μM。PAC-1通过螯合锌离子来激活胱天蛋白酶-3,从而减轻锌介导的抑制作用,并允许胱天蛋白酶原-3自身激活为胱天蛋白酶-3。 |
| 激酶实验 | In vitro procaspase-3 activation: Procaspase-3 is expressed and purified in Escherichia coli. Various concentrations of PAC-1 are added to 90 μL of a 50 ng/mL of procaspase-3 in caspase assay buffer in a 96-well plate, The plate is incubated for 12 hours at 37 °C. A 10 μL volume of a 2 mM solution of caspase-3 peptidic substrate acetyl Asp-Glu-Val-Asp-p-nitroanilide (Ac-DEVD-pNa) in caspase assay buffer is then added to each well. The plate is read every 2 minutes at 405 nm for 2 hours in a Spectra Max Plus 384 well plate reader. The slope of the linear portion for each well is determined, and the relative increase in activation from untreated control wells is calculated. |
| 细胞实验 | Cells are exposed to various concentrations of PAC-1 for 72 hours. Cell death is quantified by the addition of MTS/PMS CellTiter 96 Cell Proliferation Assay reagent. The plates are incubated at 37 °C for approximately 1 hour (until the colored product formed), and the absorbance is measured at 490 n(Only for Reference) |
| 别名 | Procaspase activating compound 1 |
| 分子量 | 392.503 |
| 分子式 | C23H28N4O2 |
| CAS No. | 315183-21-2 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
1eq. HCl: 29.4 mg/mL (75 mM)
DMSO: 39.3 mg/mL (100 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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