Uses
A cell-permeable, selective blocker of nuclear translocation of NF-KB p65. NF-KB activation inhibitor II, JSH-23
Definition
ChEBI: JSH-23 is a diamine that is 1,2-phenylenediamine carrying a methyl substituent at position 4 and a 3-phenylpropyl substituent at position N1. It has a role as a NF-kappaB inhibitor. It is a diamine and a substituted aniline. It is functionally related to a 1,2-phenylenediamine.
General Description
A cell-permeable diamino compound that selectively blocks nuclear translocation of NF-κB p65 and its transcription activity (IC50 = 7.1 μM in a NF-κB reporter assay using RAW 264.7) without affecting IκB degradation. Shown to suppress DNA-binding of NF-κB and downregulate LPS-induced gene expression and apoptotic chromatin condensation.
Biological Activity
jsh-23 is an inhibitor of nf-κb transcriptional activity with ic50 value of 7.1μm [1].jsh-23 is developed to inhibit nf-κb transcriptional activity in lps-stimulated macrophages raw 264.7. it shows a dose-dependent inhibition. this effect is not due to its cytotoxicity. in the same condition, jsh-23 is found to significantly decrease the lps-induced dna binding activity of nf-κb while decrease nuclear amount of nf-κb p65. jsh-23 plays these roles without affecting iκb degradation. in addition, jsh-23 also shows inhibition effects on the expression of the pro-inflammatory transcripts and enzymes, including il-6, il-1β, cox-2 and tnf-α. furthermore, jsh-23 inhibits lps-induced apoptotic chromatin condensation [1].
Biochem/physiol Actions
Primary TargetBlocks nuclear translocation of NF-κB p65 and its transcription activity
References
[1] shin hm, kim mh, kim bh, jung sh, kim ys, park hj, hong jt, min kr, kim y. inhibitory action of novel aromatic diamine compound on lipopolysaccharide-induced nuclear translocation of nf-kappab without affecting ikappab degradation. febs lett. 2004 jul 30;571(1-3):50-4.
