IKKβ-IN-1 是一种有效且具有口服活性的IkappaB(IKK-β) 抑制剂，IC50为 0.20 μM。IKKβ-IN-1 可以减少小鼠巨噬细胞中PGE2和TNF-α的产生。IKKβ-IN-1 能保护小鼠免受感染性休克诱导的死亡。

IKKβ-IN-1 is a potent and orally active IkappaB ( IKK-β ) inhibitor with IC 50 of 0.20 μM. IKKβ-IN-1 can reduce PGE 2 and TNF-α production in mouse macrophage cells. IKKβ-IN-1 has the ability to protect mice against septic shock induced mortality [1].

IKKβ-IN-1 (compound 7a) (0.1, 1 and 10 μM; 24 hours) does not show significant cytotoxicity at the tested three concentrations [1]. IKKβ-IN-1 (0.1, 1 and 10 μM; 1 hours) significantly reduces PGE 2 production even at the low 0.1 μM concentration, and IC 50 is 9.83 μM [1]. IKKβ-IN-1 (0.1, 1 and 10 μM; 1 hours) elicits 44% reduction of TNF-α production at 10 μM concentration, and IC 50 is 6.27 μM [1]. Cell Viability Assay Cell Line: RAW 264.7 macrophage cells [1] Concentration: 0.1, 1 and 10 μM Incubation Time: 24 hours Result: Did not show significant cytotoxicity at the tested three concentrations.

IKKβ-IN-1 (5 or 50 mg/kg; PO, single) exhibits an efficient protection of LPS-induced production of the inflammatory mediators at both of the two administered doses [1]. Animal Model: C57BL/6 male mice (6 or 10 weeks; LPS-induced production of the inflammatory mediators) [1] Dosage: 5 or 50 mg/kg Administration: PO, single (1 hour before LPS injection; survival was monitored for 36 hours) Result: Exhibited an efficient protection of LPS-induced production of the inflammatory mediators at both of the two administered doses.

2410423-31-1

C31H30N4O4S

554.66

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years