Chemical Information
M.Wt |
240.34 |
Storage |
Please store the product under the recommended conditions in the Certificate of Analysis. |
Formula |
C16H20N2 |
CAS No |
749886-87-1 |
Solubility |
DMSO 48 mg/mL; Water <1 mg/mL
|
Biological Activity of JSH-23
JSH-23 is an inhibitor of NF-κB transcriptional activity with IC50 of 7.1 μM.
IC50 Value: 7.1 μM
Target: NF-κB
in vitro: JSH-23 exhibited inhibitory effect with an IC(50) value of 7.1 microM on nuclear factor (NF)-kappaB transcriptional activity in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7, and interfered LPS-induced nuclear translocation of NF-kappaB without affecting IkappaB degradation. JSH-23 inhibits LPS-induced nuclear translocation of NF-κB p65 without affecting IκBα degradation. JSH-23 inhibits LPS-induced apoptotic chromatin condensation, while does not show significant cytotoxic effects on the RAW 264.7 cells at <100 μM [1]. JSH-23 also decreases NO production and neuronal migration in LPS activated cultures primary cultures from developing mouse cerebellum [2]. JSH-23 augments cisplatin cytotoxicity in ovarian cancer cells with CI values ranging from 0.35 to 0.85 [3].
in vivo: JSH-23 treatment significantly reversed the nerve conduction and nerve blood flow deficits seen in diabetic animals. JSH-23 (3 mg/kg) significantly reverses the nerve conduction and nerve blood flow deficits by decreasing neuroinflammation and improving antioxidant defence in diabetic rats [4].
[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., G. Negi, and S.S. Sharma, 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.