SP600125

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Chemical Structure| 129-56-6 同义名 : 蒽[1,9-cd]吡唑-6(2H)-酮 ;NSC 75890;Pyrazolanthrone;1PMV
CAS号 : 129-56-6
货号 : A155219
分子式 : C14H8N2O
纯度 : 98%
分子量 : 220.226
MDL号 : MFCD00022289
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(54.49 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 3 mg/mL clear

PO 0.5% CMC-Na 42 mg/mL suspension

生物活性
靶点

  • JNK1

    JNK1, IC50:40 nM

  • JNK

    MKK4, IC50:0.4 μM

  • JNK2

    JNK2, IC50:40 nM

  • JNK3

    JNK3, IC50:90 nM
描述 c-Jun N-terminal kinase (JNK) is a serine threonine protein kinase that belongs to the mitogen-activated protein kinase family. SP-600125 is an anthrapyrazolone inhibitor of JNK with IC50 values of 40, 40, and 90nM for JNK1, JNK2, and JNK3, respectively. SP-600125 also exhibits inhibitory activity against p56Lck, MMK3, MMK4, MMK6, MM7, PKB/AKT, and PKCα with IC50 values of 4.3, 1.5, 0.4, 1.0, 5.1, 1.0, and 1.5μM, respectively. SP-600125 inhibited JNK2 in an ATP-competitive manner with a Ki value of 0.19±0.06μM. It inhibited the phosphorylation of c-Jun in Jurkat T cells with an IC50 value of 5-10μM. In cells stimulated with PMA and phytohemagglutinin, SP-600125 inhibited both IL-2 and IFN-γ expression in a dose-dependent manner with IC50 values of 6 and 7μM, respectively. The incubation of Th1 cells with SP-600125 for 5 days potently inhibited the expression of IFN-γ, TNF-α, and IL-10 (IC50 = 7-12μM), but only weakly blocked the production of IL-1β and IL-6 (IC50 > 30μM). In primary human peripheral blood mononuclear cells stimulated with LPS (100 ng/ml) for 4 h, treatment with SP-600125 dose-dependently inhibited the mRNA expression of COX-2 and TNF-α with IC50 values of 5 and 10μM. In CD-1 mice induced with LPS, intravenous administration of SP-600125 significantly decreased the serum level of TNF-α at doses of 15 and 30mg/kg, while oral administration of 30mg/kg SP-600125 significantly inhibited TNF-α expression compared to the vehicle-treated group[2].
作用机制 SP-600125 is a small-molecule, ATP-competitive inhibitor of JNK[1].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
A549 20 μM Growth Inhibition Assay 72 h Rapid and potent inhibition of cell proliferation 23912840
A549 20 μM Function Assay 1 h Inhibition of TPA-induced MMP-2 and u-PA expression 20492175
B16-F10 Function Assay 1 h Inhibition of TNF-alpha-induced c-JUN phosphorylation 21815634
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.54mL

0.91mL

0.45mL

22.70mL

4.54mL

2.27mL

45.41mL

9.08mL

4.54mL
参考文献

[1]Bennett BL, Sasaki DT, Murray BW, et al. SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase. Proc Natl Acad Sci U S A. 2001;98(24):13681-13686. doi:10.1073/pnas.251194298