| 产品描述： | SC-514 is a selective IKK-2 inhibitor (IC50=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases. |
| 靶点： |
IKK-2:11.2 μM (IC50);CDK2/A:61 μM (IC50);AUR2:71 μM (IC50);PRAK:75 μM (IC50);MSK:123 μM (IC50);IκB/IKK;p38MAPK;SerineProtease;CDK;AuroraKinase |
| 体内研究： |
SC-514 is efficacious in an acute model of inflammation, namely LPS-induced serum TNFα production in the rat. SC-514 shows a dose-dependent inhibition of TNFα production, validating IKK-2 as a potential anti-inflammatory drug target in vivo. To obtain in vivo evidence for the implication of SC-514 in the response of cancer cells to Fotemustine, the xenograft mouse model of melanoma is used. Nude mice engrafted with A375 or G361 tumors are treated with vehicle control and 25 mg/kg SC-514 and/or 25 mg/kg Fotemustine daily for 13-15 consecutive days and the tumor behavior is monitored. Fotemustine treatment with SC-514 shows a clear combined effect and reduces the size of tumors in mice |
| 参考文献： |
1. Kishore N, et al. A selective IKK-2 inhibitor blocks NF-kappa B-dependent gene expression in interleukin-1 beta-stimulated synovial fibroblasts. J Biol Chem. 2003 Aug 29;278(35):32861-71. 2. Tse AK, et al. Sensitization of melanoma cells to alkylating agent-induced DNA damage and cell death via orchestrating oxidative stress and IKKβ inhibition. Redox Biol. 2017 Apr;11:562-576. |
| 溶解性： |
DMSO : 50 mg/mL (222.92 mM; Need ultrasonic) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
4.458 ml |
22.292 ml |
44.583 ml |
| 5 mM |
0.892 ml |
4.458 ml |
8.917 ml |
| 10 mM |
0.446 ml |
2.229 ml |
4.458 ml |
| 50 mM |
0.089 ml |
0.446 ml |
0.892 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京