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SC-514 (GK 01140)
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产品介绍
产品介绍
产品信息
抗原名称
IKK2,CDK2/CyclinA,AUR2,PRAK,MSK
商品描述
SC-514 (GK 01140), a small molecule, is a selective inhibitor of IKK-2; does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.
分子量
224.3
纯度
>98%
可溶性
DMSO : 22.4 mg/mL (100 mM)
Ethanol : 2.2 mg/mL (10 mM)
Ethanol : 2.2 mg/mL (10 mM)
外观
white to light brown Powder
In vitro(体外研究)
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.
In vivo(体内研究)
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%.
背景
别名
GK 01140; SC 514; SC514; GK-01140; GK01140
分子式
C9H8N2OS2
CAS号
354812-17-2
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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