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 > GK921
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:
 
GK921
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。
GK921图片
CAS NO:1025015-40-0
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
GK921 是一种转谷氨酰胺酶2 抑制剂,对人类重组TGase2的IC50=为7.71 μM。

产品描述

GK921 is a transglutaminase 2 (TGase) inhibitor.

体外活性

GK921 inhibits the TGase 2-induced polymerization of I-κBα and p53 in a dose-dependent manner. The cytotoxicity of GK921 ranged from GI50 of 10-10 to 10-4 M. The average GI50 is 9.05×10-7 M. GK921 rescues p53 levels and consequently induces apoptosis. The cleaved poly(ADP-ribose) polymerase (c-PARP) and p53 levels increase in a concentration-dependent manner[1].

体内活性

A single treatment with GK921 almost completely reduces tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models which suggests the possibility of a new therapeutic approach to RCC[1].

激酶实验

TGase 2 from guinea pig liver is preincubated for 10 min with various concentrations of GK13 or GK921 in 0.1 mL of reaction buffer, with or without 10 mM CaCl2, followed by the addition of 0.4 mL of substrate solution containing 2

细胞实验

Cells are transfected with a BAX promoter luciferase reporter construct. After exposure to GK921 (0, 0.5, 1, 2.5, 5 μM), firefly and Renilla luciferase activities are measured using a dual luciferase assay kit and pRL-CMV as an internal control[1].

Cas No.

1025015-40-0

分子式

C21H20N4O

分子量

344.418

储存和溶解度

DMSO:30 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years