NF-κ；β；激活剂 2 抑制 TNF-α-诱导的经典 NF-κB 信号在 PC-3 细胞中。
NF-κβ activator 2 is a potent and orally active NF-?B activator, with an EC50 of 1.58 μM. NF-κβ activator 2 induces SOD2 through increasing NF-?B expression and activation. NF-κβ activator 2 can be used for the research of amyotrophic lateral sclerosis (ALS)[1].
NF-κβ activator 2 (compound 61) (1 μM, 6 h) induces SOD2 mRNA expression in SH-SY5Y neuroblastoma cells[1].
NF-κβ activator 2 (1 mg/kg; i.v.) displays a suitable half-life (0.96 h) in mice[1].NF-κβ activator 2 (5 mg/kg; p.o.) displays a comparable half-life (2.86 h), oral bioavailability (15.6%), and Cmax (92 ng/mL)[1].
[1]. Mathew B, et, al. Structure-activity relationship (SAR) studies of N-(3-methylpyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine (SRI-22819) as NF-?B activators for the treatment of ALS. Eur J Med Chem. 2020 Oct 22;112952.
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