首页 工具
登录
购物车
Eprenetapopt

Eprenetapopt

产品编号 T4414   CAS 5291-32-7
别名: APR-246, PRIMA-1Met

Eprenetapopt (PRIMA-1Met) 是一种在 TP53突变细胞中恢复野生型 p53功能的小分子,可引发肿瘤细胞凋亡,还抑制硒蛋白硫氧还蛋白还原酶 1。

TargetMol的所有产品和服务仅用于科学研究,不能被用于人体,我们也不向个人提供产品和服务。
Eprenetapopt Chemical Structure
Eprenetapopt, CAS 5291-32-7
规格 价格/CNY 货期 数量
1 mg ¥ 259 现货
5 mg ¥ 578 现货
10 mg ¥ 913 现货
25 mg ¥ 1,830 现货
50 mg ¥ 3,230 现货
100 mg ¥ 5,730 现货
500 mg ¥ 11,500 现货
1 mL * 10 mM (in DMSO) ¥ 638 现货
产品目录号及名称: Eprenetapopt (T4414)
点击图片重新获取验证码
选择批次  
纯度: 99.57%
纯度: 98.75%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Eprenetapopt (PRIMA-1Met) restores wild-type conformation and function to mutant p53, and triggers apoptosis in tumor cells. PRIMA-1MET also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance.
靶点活性 p53:, TrxR1:
体外活性 APR-246 inhibits both recombinant TrxR1 in vitro and TrxR1 in cells. Cellular TrxR1 activity is inhibited by APR-246 irrespective of p53 status. APR-246 can directly affect cellular redox status via targeting of TrxR1. Several small molecules have been shown to restore wild-type activity to mutant p53, including CP-31398, PRIMA-1 and APR-246 (PRIMA-1MET), MIRA, STIMA, PhiKan-083 and NSC319726. PRIMA-1 and its methylated analog APR-246 promote correct folding of mutant p53, induce cell death by apoptosis, and inhibit tumor growth in mice. APR-246 has also been shown to reactivate mutant forms of the p63 and p73 proteins that share high structural homology with p53. PRIMA-1MET is a powerful apoptosis-inducing agent. PRIMA-1MET can enhance apoptosis in mutant p53 carrying cells, compared to the p53 null parental cells. Most p53 mutants are in complex with Hsp70 proteins. PRIMA-1MET treatment increases Hsp70 expression and nucleolar translocation, in parallel with the induction of nucleolar accumulation of mutant p53. Several lines of evidence suggest that PRIMA-1MET can also act independently of the p53 status of the cell. It can radiosensitize prostate carcinoma cell lines with mutant or wild type p53 and p53-/- cells as well. Introduction of mutant p53 (p53ser249 or p53 gln248) into p53-/- hepatocarcinoma cells increases sensitivity to PRIMA-1MET without the induction of p53 target genes. PRIMA-1MET regularly induces apoptosis in mutant p53 expressing cells.
激酶实验 Cells are plated in six-well plates at a density of 15?000 cells per cm2. Next day, cells are treated with different concentrations of APR-246 (0, 25, 50, 75 and 100 μM) and harvested after 4, 12 and 24?h. The cells are lysed, and the clarified supernatants are used for either analysis of TrxR enzymatic activities or western blot. Total protein concentrations are determined with a Bradford reagent kit. Cellular TrxR activity is measured using an adapted Trx-dependent end point insulin reduction assay for microwell plates.
别名 APR-246, PRIMA-1Met
分子量 199.25
分子式 C10H17NO3
CAS No. 5291-32-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 20 mg/mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
=
X
X
X
=
X
=
/
g/mol

输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Peng X,etal.APR-246/PRIMA-1MET inhibits thioredoxin reductase 1 and converts the enzyme to a dedicated NADPH oxidase.Cell Death Dis. 2013 Oct 24;4:e881. 2. Stuber G,etal.PRIMA-1MET induces nucleolar translocation of Epstein-Barr virus-encoded EBNA-5 protein.Mol Cancer. 2009 Mar 26;8:23.
6-Acetonyldihydrochelerythrine Physalin A Indole-3-carbinol BAY 1892005 ZMC1 Alphitolic acid 7alpha,15-Dihydroxydehydroabietic acid Altholactone

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌活性化合物库 抗癌临床化合物库 抗乳腺癌化合物库 抗结直肠癌化合物库 自噬库 抗癌化合物库 经典已知活性库 代谢化合物库 抑制剂库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Eprenetapopt 5291-32-7 Apoptosis Autophagy Others Ferroptosis p53 APR-246 APR246 Inhibitor APR 246 MDM-2/p53 inhibit PRIMA-1Met inhibitor

 

陶术
生物
TargetMol®中国区唯一合作伙伴
点击进入陶术生物官网陶术生物
联系我们
400-820-0310

上海市静安区江场三路238号8楼