基本信息

产品描述

IKK-16 (IKK Inhibitor VII)是一种选择性的IκB激酶(IKK)抑制剂，作用于IKK-2，IKK complex和IKK-1，无细胞试验中IC50分别为40 nM，70 nM和200 nM。

靶点（IC50 & Targe）

IKK complex,70nM

IKK1,200nM

IKK2,40nM

体外研究

IKK-16抑制HUVEC细胞中TNFα刺激的黏附分子E-selectin, ICAM-1, 和VCAM-1的表达。尽管 IKK-16也具有抑制IFNγ诱导的β2 微球蛋白或HLA-DR表达的活性，但是其效价在这些分析中要低4-10倍。 [1]

体内研究

IKK-16 对大鼠和小鼠具有口服活性，在体内可以抑制脂多糖诱导的TNF-α 的释放，还可以抑制硫胶质诱导的腹膜炎中中性粒细胞外渗[1]。

参考文献

[1] Waelchli R, et al. Bioorg Med Chem Lett, 2006, 16(1), 108-11

安全信息

图形或危害标志
危险说明	H302 H410
防范说明	P264 P270 P273 P301+P312 P330 P391 P501
UN号码	3077
危险分类	9
包装等级	III

产品说明

一般描述

A cell-permeable benzamido-pyrimidine compound that acts as a potent, selective, and ATP-competitive inhibitor of IKK (IC₅₀ = 40 nM, 70 nM, and 200 nM for IKK-2, IKK complex, and IKK-1, respectively). Inhibits cellular IκBα degradation and NF-κB-mediated gene expression in vitro in HUVEC cells and has been shown to exhibit excellent in vivo efficacy both in mice and rats.
A cell-permeable benzamido-pyrimidine compound that acts as a potent, selective, and ATP-competitive inhibitor of IKK (IC₅₀ = 40 nM, 70 nM, and 200 nM for IKK-2, IKK complex, and IKK-1, respectively). Inhibits cellular IκBα degradation and NF-κB-mediated gene expression in vitro in HUVEC cells and has been shown to exhibit excellent in vivo efficacy both in mice and rats. Also available as a 10 mM solution in DMSO (Cat. No. 505378).

包装

1 mg in Glass bottle
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Reversible: no
Target IC₅₀: 40 nM, 70 nM, and 200 nM for IKK-2, IKK complex, and IKK-1, respectively
Product competes with ATP.
Primary Target
IKK

警告

Toxicity: Harmful (C)

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

产品性质

安全信息

产品说明

一般描述

A cell-permeable benzamido-pyrimidine compound that acts as a potent, selective, and ATP-competitive inhibitor of IKK (IC₅₀ = 40, 70, and 200 nM for IKK-2, IKK complex, and IKK-1, respectively). Inhibits cellular IκBα degradation and NF-κB-mediated gene expression in vitro in HUVEC cells and has been shown to exhibit excellent in vivo efficacy both in mice and rats.

生化/生理作用

Cell permeable: yes
Reversible: yes
Primary Target
IKK-2, IKK complex, and IKK-1

包装

Packaged under inert gas

警告

Toxicity: Irritant (B)

外形

A 10 mM (500 µg/103 µL) sterile-filtered solution of IKK Inhibitor VII (Cat. No. 401486) in DMSO.

重悬

Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C.

其他说明

Waelchli, R., et al. 2006. Bioorg. Med. Chem. Lett.16, 108.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

产品性质