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簡要描述：SP600125是一種廣譜JNK抑制劑，作用于JNK1，JNK2和JNK3，無細(xì)胞試驗(yàn)中IC50分別為40nM，40nM和90nM，比作用于MKK4選擇性高10倍，比作用于MKK3，MKK6，PKB，和PKCα選擇性高25倍，比作用于ERK2，p38，Chk1，EGFR等選擇性高100倍。
產(chǎn)品型號：abs810008廠商性質(zhì)：生產(chǎn)廠家更新時間：2024-10-21訪 問 量：874產(chǎn)品分類
Product Category詳細(xì)介紹
| 品牌 | absin | CAS | 129-56-6 |
|---|---|---|---|
| 純度 | >98 % | 貨號 | abs810008 |
| 規(guī)格 | 10mg;50mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | - | 應(yīng)用領(lǐng)域 | 生物產(chǎn)業(yè),綜合 |
| 產(chǎn)品描述 | |
| 描述 | SP600125是一種廣譜JNK抑制劑，作用于JNK1，JNK2和JNK3，無細(xì)胞試驗(yàn)中IC50分別為40nM，40nM和90nM，比作用于MKK4選擇性高10倍，比作用于MKK3，MKK6，PKB，和PKCα選擇性高25倍，比作用于ERK2，p38，Chk1，EGFR等選擇性高100倍。 |
| 純度 | >98 % |
| 儲存/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 | |
| 別名 | SP 600125；SP-600125；Nsc75890 |
| 外觀 | Lyophilized powder |
| 可溶性/溶解性 | DMSO: ≥ 44 mg/mL |
| 生物活性 | |
| 靶點(diǎn) | JNK1；JNK2；Aurora A；TrkA ；JNK3 |
| In vitro(體外研究) | SP600125 is originally characterized as a selective ATP-competitive inhibitor of c-Jun N-terminal kinase JNK. In Jurkat T cells, SP600125 inhibits the phosphorylation of c-Jun with IC50 of 5 μM to 10 μM. In CD4+ cells, such as Th0 cells isolated from either human cord or peripheral blood, SP600125 blocks cell activation and differentiation and inhibits the expression of inflammatory genes COX-2, IL-2, IL-10, IFN-γ, and TNF-α, with IC50 of 5 μM to 12 μM. However, later studies reveal that SP600125 also suppresses aryl hydrocarbon receptor (AhR) , Mps1 , and a panel of other serine/threonine kinases, including Aurora kinase A, FLT3, MELK, and TRKA .In a mouse beta cells MIN6, SP600125 (20 μM) induces the phosphorylation of p38 MAPK and its downstream CREB-dependent promoter activation. In HCT116 cells, SP600125 (20 μM) blocks the G2 phase to mitosis transition and induces endoreplication. This ability of SP600125 is independent of JNK inhibition, but due to its inhibition of CDK1-cyclin B activation upstream of Aurora A and Polo-like kinase 1. |
| In vivo(體內(nèi)研究) | In mice, SP600125 (15 mg/kg or 30 mg/kg) significantly inhibits lipopolysaccharide (LPS)-induced TNF-α expression and anti-CD3-induced apoptosis of CD4+ CD8+ thymocytes. |
| 參考文獻(xiàn) | |
| 參考文獻(xiàn) | [1] Bennett BL, et al. Proc Natl Acad Sci U S A, 2001, 98(24), 13681-13686. [2] Joiakim A, et al. Drug Metab Dispos, 2003, 31(11), 1279-1282. [3] Schmidt M, et al. EMBO Rep, 2005, 6(9), 866-872. |
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