SC-514;IKK-2抑制劑  354812-17-2

 SC-514;IKK-2抑制劑
分子式： C9H8N2OS2   分子量：224.30
 
產(chǎn)品描述
SC-514是口服有效的，ATP競(jìng)爭(zhēng)性IKK-2抑制劑，IC50為3-12 μM，抑制NF-κB依賴性的基因表達(dá),不抑制其他IKK異構(gòu)體或其他絲-蘇氨酸和酪氨酸激酶。
靶點(diǎn)
IKK-2
         
IC50
3-12 μM
         
體外研究
SC-514 inhibits the native IKK complex or recombinant human IKK-1/IKK-2 heterodimer and IKK-2 homodimer similarly. SC-514 inhibits transcription of NF-κB-dependent IL-6, IL-8, and COX-2 genes in IL-1β-induced rheumatoid arthritis-derived synovial fibroblasts (RASFs) with IC50s of 20, 20 and 8 μM. 100 μM SC-514 blocks the phosphorylation and degradation of IκBα and also reduces the level of translocation of p65 into the nucleus in IL-1β-treated RASFs SC-514 does not inhibit the phosphorylation and activation of the IKK complex. SC-514 induces a delay but not a complete blockade in IκBα phosphorylation and degradation. SC-514 treatment cells shows a slightly slowed, decreased import of p65 into the nucleus and a faster export of p65 from the nucleus. SC-514 inhibits the phosphorylation of either IκBα or p65 similarly.
體內(nèi)研究
SC-514 is efficacious in an acute model of inflammation, namely LPS-induced serum TNF-α production. SC-514 (50 mg/kg, i.p.) inhibits TNF-αproduction in vivo by ~70%
溶解性
DMSO 45 mg/mL，水 <1 mg/mL，乙醇 <1 mg/mL
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO