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 > PX-12
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:
 
PX-12
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。
CAS NO:141400-58-0
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
2-[(1-甲基丙基)二硫代]-1H-咪唑
PX12
IV-2
产品介绍
PX-12 是一种可逆的硫氧还蛋白-1(Trx-1)抑制剂,能够抑制MCF-7 细胞(IC50:1.9 μM)和HT-29 细胞(IC50:2.9 μM)的生长。

产品描述

PX-12 (1-methylpropyl 2-imidazolyl disulfide) is a small-molecule inhibitor of Trx-1 (thioredoxin-1), stimulates apoptosis, down-regulates HIF-1α and vascular endothelial growth factor (VEGF) and inhibits tumor growth in animal models. Since high levels of Trx-1 have been associated with colorectal, gastric and lung cancers, PX-12 is indicated as a potential cancer treatment in combination with chemotherapy for patients with advanced metastatic cancer. Initial trials correlated doses of Px-12 with increased patient survival.

体外活性

In MCF-7 and HT-29 cells, PX-12 prevents the hypoxia (1% oxygen)-induced increase in HIF-1alpha protein, and decreases HIF-1-trans-activating activity, VEGF formation, and inducible nitric oxide synthase. PX-12 also inhibits the growth of MCF-7 and HT-29 cells with IC50s of 1.9 μM and 2.9 μM, respectively. [1] PX-12 also inhibits HIF-1α protein levels through an Nrf2/PMF-1-mediated increase. [2] In A549 cells, PX-12 inhibits cell growth via G2/M phase arrest, and Bax-mediated and ROS-dependent apoptosis. [3] In hepatocelluar carcinoma cells, PX-12 exerts a synergistic effect with 5-FU to significantly suppress tumorigenicity. [4]

体内活性

In mice bearing MCF-7 tumor xenografts, PX-12 (12 mg/kg, i.p.) decreases HIF-1α and VEGF protein levels and microvessel density. [1]

细胞实验

Cell growth is measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Cells are exposed to a range of concentrations of PX-12 or pleurotin for 16 h in air or hypoxia (1% oxygen). The cells are then washed with warm drug-free medium and grown in air for the remainder of the 72-h incubation.(Only for Reference)

Cas No.

141400-58-0

分子式

C7H12N2S2

分子量

188.32

别名

2-[(1-甲基丙基)二硫代]-1H-咪唑;PX12;IV-2

储存和溶解度

H2O:<1 mgml
Ethanol:38 mg/mL (201.79 mM)
DMSO:18.8 mg/mL(100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years