生物活性

• 靶点

  COX2 IC50:1.77μM

  COX1 IC50:75μM

• 描述NS-398 is a novel anti-inflammatory and analgesic agent. The COX-1 activity was completely unaffected by 100μ M NS-398, whereas the COX-2 activity was concentration-dependently inhibited with IC50 of 3.8μ M. NS-398 shows the anti-inflammatory and analgesic effects with the effective dose range being 0.3∼5 mg/kg in rats.In vitro experiments, NS-398 inhibited the proliferation and maturation of differentiated myogenic precursor cells, which suggested a detrimental effect on skeletal muscle healing. In the NS-398-treated mice, muscle regeneration delayed at early time points after injury.NS-398 decreased the regeneration of injured muscle by delaying the maturation of regenerating myofibers, and promoted fibrosis by up-regulating TGF-β1 expression. NS-398 administration also reduced the inflammatory response and up-regulated myostatin expression. NS-398 (10 mM) can induce apoptosis in LNCaP cells. When treated with NS-398, the C4-2b cells were observed to continue to proliferate and continued to retain malignant phenotype characteristics. NS-398 treatment resulted in C4-2b cell differentiation into an unusual neuroendocrine-like cell which produced both epithelial and neuronal proteins. Moreover, this C4-2b cellular response to NS-398 was mediated by NF-kappa beta transcription factor activation. Cox-2 is involved in the pathogenesis of Noise-induced hearing loss (NIHL), and pre-treatment with the Cox-2 inhibitor NS398 could inhibit Cox-2 expression during noise overstimulation attenuating noise-induced hearing loss and hair cell damage.