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HI-TOPK-032
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。
HI-TOPK-032图片
CAS NO:487020-03-1
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
HI-TOPK-032 是一种特异性 TOPK 有效抑制剂。

产品描述

HI-TOPK-032 is an effective and specific inhibitor of TOPK.

体外活性

HI-TOPK-032 inhibits anchorage-dependent and -independent colon cancer cell growth by reducing ERK-RSK phosphorylation as well as increasing colon cancer cell apoptosis through regulation of the abundance of p53, cleaved caspase-7, and cleaved PARP. However, HI-TOPK-032 at the highest concentration (5 μM) also inhibits MEK1 activity by 40%. HI-TOPK-032 strongly inhibits TOPK kinase activity. However, it also has little effect on extracellular signal-regulated kinase 1 (ERK1), c-jun-NH2-kinase 1, or p38 kinase activities. HI-TOPK-032 occupies the ATP-binding site of TOPK and fits the binding site very well. The compound forms hydrogen bonds with GLY83 and ASP151 and has a hydrophobic interaction with LYS30.

体内活性

HI-TOPK-032 (1 or 10 mg/kg; mice) treatment, obviously inhibits HCT-116 tumor growth by more than 60% relative to the vehicle-treated group. Mice are well tolerated with HI-TOPK-032 treatment. The expression of p53 is strongly caused, and phosphorylation of ERK and RSK, a direct downstream protein of ERK. Which is markedly inhibited in the HI-TOPK-032-treated group.

Cas No.

487020-03-1

分子式

C20H11N5OS

分子量

369.4

储存和溶解度

DMSO:7 mg/mL (18.94 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years