SP 600125 100mg
SP 600125 100mg
SP600125 is a selec
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 ex
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 Natio
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nnect Tissue Res." 2019 Mar 22:1-10. PMID:30897973 - 3. Vincent Picher-Martel. "L’implication de l’ubiquiline-2 dans l’agrégation de TDP- 43 et la pathogénèse de la sclérose latérale amyotrophique." University Laval. 2019.
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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 | ≥11mg/mL in DMSO, ≥2.56 mg/mL in EtOH with gentle warming,insoluble in H2O |
Chemical Name | dibenzo[cd,g]indazol-6(2H)-one |
SDF | Download SDF |
Cano |
O=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限,请添加助溶剂助溶或自行调整浓度。 |
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 Natio |
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 |