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| 品牌 | absin | CAS | 354812-17-2 |
|---|---|---|---|
| 分子式 | C9H8N2OS2 | 纯度 | ＞98% |
| 分子量 | 224.3 | 货号 | abs810561 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | is a selective inhibitor of IKK-2 | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
SC-514 (GK 01140) 354812-17-2
| 产品描述 | |
| 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. |
| 纯度 | >98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | GK 01140; SC 514; SC514; GK-01140; GK01140 |
| 外观 | white to light brown Powder |
| 可溶性/溶解性 | DMSO : 22.4 mg/mL (100 mM) Ethanol : 2.2 mg/mL (10 mM) |
| 生物活性 | |
| 靶点 | IKK2,CDK2/CyclinA,AUR2,PRAK,MSK |
| 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%. |
| 研究领域 | |
| 研究领域 | CancerTumor biomarkers CancerTumor immunology Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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