SP 600125
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SP600125是一种选择性的、可逆的和ATP竞争性的Jun N-端激酶（JNK）抑制剂，作用于JNK1、2和3，IC50值分别为40 nM、40 nM和90 nM[1]。
SP600125是用GST-c-Jun和重组人JNK2通过时间分辨荧光实验筛选得到的。在该实验中，SP600125的Ki值为190 nM。在选择性实验中发现，SP600125也抑制JNK1、2和3亚型。SP600125对JNK的选择性比对ERK1和p38-2高300倍。在Jurkat T细胞中，SP600125抑制c-Jun的磷酸化，IC50值为5-10 μM。据报道，JNK调节IL-2的转录，因而SP600125也抑制PMA和植物血凝素刺激的细胞中IL-2和IFN-γ的表达。此外，SP600125对CD4+细胞中的细胞因子及单核细胞中的炎症基因具有不同的抑制效应。而且，在小鼠模型中，SP600125显著抑制LPS诱导的TNF-α的表达，表明SP600125在体内对内毒素诱导的炎症有疗效[1]。
参考文献：
[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.
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| Physical Appearance | A solid |
| Storage | Desiccate at -20°C |
| M.Wt | 220.23 |
| Cas No. | 129-56-6 |
| Formula | C14H8N2O |
| Solubility | insoluble in H2O; ≥11 mg/mL in DMSO; ≥2.56 mg/mL in EtOH with gentle warming |
| Chemical Name | dibenzo[cd,g]indazol-6(2H)-one |
| SDF | Download SDF |
| Canonical SMILES | O=C1C2=CC=CC3=C2C(C4=CC=CC=C41)=NN3 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]: | |
|
细胞系 |
MIN6细胞 |
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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] | |
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动物模型 |
雄性C57BL/6 小鼠 |
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给药剂量 |
皮下注射，15 mg/kg，在0、12、24和36 h给药 |
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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。 |
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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. |
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| 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 |
质量控制和MSDS
- 批次:
化学结构
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