JSH-23

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NF-κB-

JSH-23 ?????????NF-??B????????????IC50?????? 7.1 ??M???

NF-κB

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生物活性

Description

JSH-23 is an inhibitor ofNF-??Bwith anIC50value of 7.1 ??M.

IC50& Target

IC50: 7.1 ??M (NF-??B)

In Vitro

JSH-23 inhibits LPS-induced chromatin condensation in a dose-dependent manner, corresponding to 44??4% inhibition at 3 ??M, 63??5% at 10 ??M and 93??3% at 30 ??M[1]. JSH-23 (5, 10, and 15 ??M) significantly reduces mean neuronal migration in LPS-activated cells[2]. Co-treatment of A2780 cells with JSH-23 and clinically ineffective transplatin at their IC50concentrations (130 ??M transplatin and 20 ??M JSH-23) for 72 h also causes a more pronounced decrease in cell viability compared to the effects of transplatin or JSH-23 alone[3].

In Vivo

JSH-23 (1 and 3 mg/kg, p.o.) significantly reverses the nerve conduction and nerve blood flow deficits seen in diabetic animals and decreases the nerve lipid peroxidation, partially replenishes the depleted levels of GSH in nerve of diabetic rats[4].

References

[1].Shin, H.M., et al. Inhibitory action of novel aromatic diamine compound on lipopolysaccharide-induced nuclear translocation of NF-kappaB without affecting IkappaB degradation. FEBS Lett, 2004. 571(1-3): p. 50-4.

[2].Arias-Salvatierra, D., et al. Role of nitric oxide produced by iNOS through NF-kappaB pathway in migration of cerebellar granule neurons induced by Lipopolysaccharide. Cell Signal, 2011. 23(2): p. 425-35.

[3].Kasparkova, J., et al. Different affinity of nuclear factor-kappa B proteins to DNA modified by antitumor cisplatin and its clinically ineffective trans isomer. FEBS J, 2014. 281(5): p. 1393-408.

[4].Kumar, A., et al. JSH-23 targets nuclear factor-kappa B and reverses various deficits in experimental diabetic neuropathy: effect on neuroinflammation and antioxidant defence. Diabetes Obes Metab, 2011. 13(8): p. 750-8.