SP 600125
(Synonyms: 吡唑蒽酮) 目录号 : GC15344
SP 600125是一种具有口服活性的、可逆的、具有选择性的ATP竞争性JNK 抑制剂，对JNK1、JNK2和JNK3的IC50分别为40、40和90nM。SP 600125常用于卵巢癌、肿瘤、帕金森病 (PD)、乳腺癌和哮喘的研究。
Cas No.:129-56-6
Sample solution is provided at 25 µL, 10mM.
SP 600125 is an orally active, reversible, selective, ATP-competitive JNK inhibitor with IC50 of 40, 40, and 90 nM for JNK1, JNK2, and JNK3, respectively. SP 600125 is commonly used in the research of ovarian cancer, tumors, Parkinson's disease (PD), breast cancer, and asthma[1,2].
SP 600125 (10-20 μM; 24 h) reduces PMA-dependent MMP-9 secretion and inhibits c-Jun phosphorylation, and also inhibits PMA-stimulated MMP-9 promoter-driven luciferase reporter gene activity[1].SP 600125 inhibits c-Jun phosphorylation with an IC50 of 5-10 μM. SP 600125(5-10 μM,24h) also inhibits LPS-induced increase COX-2 protein levels and PGE2 production[3].
SP 600125 (10/30/50 mg/kg/day; ip) inhibits MPTP-induced JNK activation and c-Jun phosphorylation in the substantia nigra obturata (SNc) and prevents the decrease in dopamine concentration in the striatum and alleviates behavioral impairment in MPTP-treated mice[2]. SP 600125(30mg/kg/day) can significantly reduce the expression of inflammatory cells in the bronchi and lungs under OVA stimulation[4].
References:
[1]. Shin M, Yan C, Boyd D. An inhibitor of c-jun aminoterminal kinase (SP600125) represses c-Jun activation, DNA-binding and PMA-inducible 92-kDa type IV collagenase expression. Biochim Biophys Acta. 2002 May 8;1589(3):311-6.
[2]. Wang W, Shi L, Xie Y, Ma C, Li W, Su X, Huang S, Chen R, Zhu Z, Mao Z, Han Y, Li M. SP600125, a new JNK inhibitor, protects dopaminergic neurons in the MPTP model of Parkinson's disease. Neurosci Res. 2004 Feb;48(2):195-202.
[3]. Nieminen R, Lahti A, Jalonen U, Kankaanranta H, Moilanen E. JNK inhibitor SP600125 reduces COX-2 expression by attenuating mRNA in activated murine J774 macrophages. Int Immunopharmacol. 2006 Jun;6(6):987-96.
[4].Wu HM, Fang L, Shen QY, Liu RY. SP600125 promotes resolution of allergic airway inflammation via TLR9 in an OVA-induced murine acute asthma model. Mol Immunol. 2015 Oct;67(2 Pt B):311-6.
SP 600125是一种具有口服活性的、可逆的、具有选择性的ATP竞争性JNK 抑制剂，对JNK1、JNK2和JNK3的IC50分别为40、40和90nM。SP 600125常用于卵巢癌、肿瘤、帕金森病 (PD)、乳腺癌和哮喘的研究[1,2]。
SP 600125 （10-20 μM；24 小时） 可降低 PMA 依赖的 MMP-9 分泌并抑制 c-Jun 磷酸化，还可抑制 PMA 刺激的 MMP-9 启动子驱动的荧光素酶报告基因活性[1]。SP600125 抑制 c-Jun 磷酸化的 IC50 为 5-10 μM，SP600125（5-10 μM，24 小时）还可抑制 LPS 诱导的 COX-2 蛋白水平上升和 PGE2 产生[3]。
SP 600125(10/30/50 mg/kg/day；ip)可抑制MPTP诱导的黑质闭孔(SNc)中JNK活化和c-Jun磷酸化，防止纹状体多巴胺浓度下降，减轻MPTP治疗小鼠的行为障碍[2]。SP600125（30mg/kg/day）可显著减少OVA刺激下支气管和肺脏中炎症细胞的表达[4]。
| Cell experiment [1]: | |
Cell lines | OVCAR-3 cells |
Preparation Method | OVCAR3 cells were treated with SP600125(10-20) μM for 24 hours. |
Reaction Conditions | SP600125(10-20) μM ;24h |
Applications | SP600125(10-20μM;24h) reduces PMA-dependent MMP-9 secretion and inhibits c-Jun phosphorylation. |
| Animal experiment [2]: | |
Animal models | MPTP-induced PD in mice |
Preparation Method | MPTP-induced PD in mice that they were given SP600125 (10/30/50 mg/kg;ip) once per day between days 1 and 6, respectively. Mice were sacrificed at day 10 after the final injection of MPTP. |
Dosage form | SP600125 (10/30/50 mg/kg)/ day; ip |
Applications | SP600125 inhibited MPTP-induced JNK activation and c-Jun phosphorylation in SNc;SP600125 prevented the reduction of dopamine concentrations in the striatum and attenuated behavioral impairment in MPTP-treated mice. |
References: | |
| Cas No. | 129-56-6 | SDF | |
| 别名 | 吡唑蒽酮 | ||
| 化学名 | dibenzo[cd,g]indazol-6(2H)-one | ||
| Canonical SMILES | O=C1C2=CC=CC3=C2C(C4=CC=CC=C41)=NN3 | ||
| 分子式 | C14H8N2O | 分子量 | 220.23 |
| 溶解度 | ≥ 11mg/mL in DMSO, ≥ 2.56 mg/mL in EtOH with gentle warming | 储存条件 | Desiccate at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.5407 mL | 22.7035 mL | 45.4071 mL |
| 5 mM | 0.9081 mL | 4.5407 mL | 9.0814 mL |
| 10 mM | 0.4541 mL | 2.2704 mL | 4.5407 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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3. 以上所有助溶剂都可在 GlpBio 网站选购。
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