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SP 600125

现货
Catalog No.
A4604
JNK1/2/3抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
10mg
¥ 500.00
现货
50mg
¥ 650.00
现货
100mg
¥ 850.00
现货

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Background

SP600125 is a selective, reversible and ATP-competitive inhibitor of Jun N-terminal kinase (JNK) with IC50 values of 40, 40 and 90 nM for JNK1, 2 and 3, respectively [1].

SP600125 was screened out from a time-resolved f luorescence assay using the GST-c-Jun and recombinant human JNK2. In this assay, SP600125 showed a Ki value of 190 nM. SP600125 was also found to inhibit JNK1, 2 and 3 isoforms in the selectivity tests. The selectivity of SP600125 for JNK is 300-fold greater than that for ERK1 and p38-2. In Jurkat T cells, SP600125 suppressed the phosphorylation of c-Jun with IC50 of 5-10 μM. SP600125 also inhibited the expression of IL-2 and IFN-γ in cells stimulated with PMA and phytohemagglutinin, since JNK had been reported to regulate the transcription of IL-2. Besides that, SP600125 exerted differential inhibition of cytokines in CD4+ cells as well as inflammatory genes in monocytes. Moreover, SP600125 administration significantly inhibited TNF-α expression induced by LPS in a mouse model, suggesting that it had efficacy in endotoxin-induced inf lammation in vivo [1].

References:
[1] Bennett B L, Sasaki D T, Murray B W, et al. SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase. Proceedings of the National Academy of Sciences, 2001, 98(24): 13681-13686.

文献引用

Chemical Properties

Physical AppearanceA solid
StorageDesiccate at -20°C
M.Wt220.23
Cas No.129-56-6
FormulaC14H8N2O
Solubility≥11mg/mL in DMSO, ≥2.56 mg/mL in EtOH with gentle warming, <2.27 mg/mL in H2O
Chemical Namedibenzo[cd,g]indazol-6(2H)-one
SDFDownload SDF
Canonical SMILESO=C1C2=CC=CC3=C2C(C4=CC=CC=C41)=NN3
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

MIN6细胞

制备方法

该化合物在DMSO中的溶解度大于10 mM,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

40 μM,36 hours

实验结果

在Gal4质粒和CREB质粒转染的MIN6细胞中,SP600125以剂量依赖性方式显著刺激CREB介导的启动子活性。在转染的MIN6细胞中,20 μM SP600125将报告基因的活性增加2.8倍。

动物实验: [1]

动物模型

雄性C57BL/6 小鼠

给药剂量

皮下注射,15 mg/kg,在0、12、24和36 h给药

实验结果

在0时刻给药SP600125后,腹腔注射单剂量的50 μg抗CD3。48小时后,杀死小鼠,并切除胸腺以分离胸腺细胞。SP600125给药的小鼠对CD3 Ab介导的凋亡产生完全的抗性,CD4+CD8+数目与对照动物相同。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1] Vaishnav D, Jambal P, Reusch J E B, et al. SP600125, an inhibitor of c-jun N-terminal kinase, activates CREB by a p38 MAPK-mediated pathway. Biochemical and biophysical research communications, 2003, 307(4): 855-860.

[2] Bennett B L, Sasaki D T, Murray B W, et al. SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase. Proceedings of the National Academy of Sciences, 2001, 98(24): 13681-13686.

生物活性

描述 SP600125是JNK的广谱抑制剂,作用于JNK1、JNK2和JNK3,IC50值分别为40 nM、40 nM和90 nM。
靶点 JNK1 JNK2 JNK3 Aurora A Flt3 TRKA
IC50 40 nM 40 nM 90 nM 60 nM 90 nM 70 nM

质量控制

化学结构

SP 600125

相关生物数据

SP 600125

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SP 600125

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SP 600125

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SP 600125

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SP 600125

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SP 600125

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SP 600125