| 应用 |
An anti-inflammatory agent and NFκB inhibitor |
| 产品介绍 |
BAY 11-7082是一种NF-κB抑制剂，抑制TNFα诱导的IκBα磷酸化，IC50为10 μM。同时对泛素化系统的组分也有抑制作用。 |
| 备注 |
BAY 11-7082 is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM. |
| 生化机理 |
BAY 11-7082, a potential anti-inflammatory agent, is an irreversible inhibitor of IKK α and phosphorylation of cytokine-inducible IκBα (nuclear factor of kappa light polypeptide gene enhancer in B-cells inhibitor-α, NFKBIA; IC50=10 μM). In intact HUVECs, it inhibits TNFα-induced phosphorylation and degradation of IκBa (NFKBIA) without affecting constitutive phosphorylation. Inhibition of ιBα phosphorylation and degradation results in the inactivation of NFκB and thereby inhibits the expression of endothelial-leukocyte adhesion molecules: E-selectin, VCAM-1 and ICAM-11. BAY 11-7082 has also demonstrated stimulation of the stress-activated protein kinases, p38 and JNK-1. |
| 别名 |
(E)-3-(对甲苯磺酰基)丙烯腈; (E)-3-甲苯磺酰基丙烯腈;(2E)-3-[(4-甲基苯基)磺酰基]-2-丙烯腈;(E)-3-(4-Methylphenylsulfonyl)-2-propenenitrile;(E)-3-Tosylacrylonitrile;(E)-3-(p-Toluenesulfonyl)acrylonitrile |
