产品名称

BMS-345541

一般描述

BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1.

别 称

N'-(1,8-dimethylimidazo[1,2-a]quinoxalin-4-yl)ethane-1,2-diamine; BMS345541

纯 度

≥98%(HPLC)

CAS NO.

445430-58-0

分子式

C¹⁴H¹⁷N⁵

分子量

255.325

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色至类白色固体

溶解性(25℃)

DMSO

~8mg/mL

乙醇

Insoluble

水

Insoluble

l  生物学信息

生物活性/药理作用

A cell-permeable quinoxaline compound that displays anti-inflammatory properties. Acts as a potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC50 = ~ 300 nM). Exhibits  ~10-fold greater selectivity over IKK-1 (IC50 = ~ 4 µM) and no activity  towards IKKε and a panel of more than 15 unrelated protein kinases even at  concentrations as high as 100 µM. Inhibits cellular IκBα phosphorylation  (IC50 = 4 µM in THP-1 cells) and LPS-induced cytokine production both in vitro (IC50 = 1-5 µM in THP-1 cells) and in vivo (IC50 = 10 mg/kg in mice).  Effectively blocks inflammation and joint destruction in a murine arthritis  model.

A cell-permeable, potent, selective, and allosteric site-binding inhibitor of IKK-2 (IC50 ~300 nM) that displays anti-inflammatory properties. Exhibits ~10-fold greater selectivity for IKK-2 over IKK-1 (IC50 ~4.0 µM) and does not inhibit IKKε and a panel of more than  15 unrelated protein kinases even at concentrations as high as 100 µM.  Inhibits cellular IκBα phosphorylation (IC50 = 4 µM in THP-1 cells) and LPS-induced cytokine production both in vitro (IC50 = 1-5 µM in THP-1 cells)  and in vivo (IC50 = 10 mg/kg in mice). Effectively blocks inflammation and  joint destruction in a murine arthritis model.

l  包装与存储

包 装

5mg;  25mg; 100mg

存储温度

0-5℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.   https://www.ncbi.nlm.nih.gov