您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > PAC-1
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
PAC-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PAC-1图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
PAC-1 是一种 procaspase-3 激活剂,可诱导癌细胞凋亡,EC50 为 2.08 μM。

Cell lines

Several cancer cell lines (leukemia, lymphoma, melanoma, neuroblastoma, breast cancer, lung cancer, adrenal cancer and renal cancer)

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 ℃ for several months.

Reaction Conditions

72 hrs

Applications

PAC-1 induces cell death in a procaspase-3-dependant manner. PAC-1 is most potent against the lung cancer cell line NCI-H226, with an IC50 value of 0.35 μM.

Animal models

Mice s.c. injected with NCI-H226 (lung cancer) cells

Dosage form

0, 50 or 100 mg/kg; p.o.; q.d., for 21 days

Applications

In mice s.c. injected with NCI-H226 (lung cancer) cells, PAC-1 significantly retarded tumor growth in a dose-dependent manner.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

First procaspase-activating compound (PAC-1) is a small-molecule activator of procaspase-3 that directly catalyzes the maturation of procaspase-3 to the active caspase-3 by inducing the cleavage of procaspase-3 in a time-dependent manner. As a result of the direct and immediate activation of procaspase-3, PAC-1 potently induces apoptosis in cancer cell lines. The PAC-1 induced apoptosis has been observed to be proportional to the concentrations of procaspase-3 inside the cells of primary colon cancer isolates. Study results have demonstrated that PAC-1 is able to induce cell death in both primary cancerous cells and adjacent normal tissues with 50% inhibition concentration IC50values ranging from 0.003 to 1.41 μM and 5.02 to 9.98 μM respectively.

Reference

[1].Putt KS, Chen GW, Pearson JM, Sandhorst JS, Hoagland MS, Kwon JT, Hwang SK, Jin H, Churchwell MI, Cho MH, Doerge DR, Helferich WG, Hergenrother PJ. Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy. Nat Chem Biol. 2006 Oct;2(10):543-50. Epub 2006 Aug 27.