SP600125
别名: Nsc75890
SP600125 (Nsc75890)是一种广谱JNK抑制剂，作用于JNK1、JNK2和JNK3，无细胞试验中IC50分别为40 nM、40 nM和90 nM，比作用于MKK4选择性高10倍，比作用于MKK3、MKK6、PKB和PKCα选择性高25倍，比作用于ERK2、p38、Chk1、EGFR等选择性高100倍。SP600125也是一种广谱的serine/threonine kinases抑制剂，包括Aurora kinase A、FLT3和TRKA，对应的IC50值为60 nM、90 nM和70 nM。SP600125可抑制自噬而激活细胞凋亡。
SP600125 Chemical Structure
CAS: 129-56-6
客户使用Selleck的SP600125发表文献989篇
产品质控
常与SP600125一起在实验中被使用的化合物
Choi Y, et al. World J Gastroenterol. 2016 Nov 7; 22(41): 9141–9153.
SP600125相关产品
| 相关靶点 | JNK1 JNK2 JNK3 | 点击展开 |
|---|---|---|
| 相关化合物库 | 激酶抑制剂库 MAPK抑制剂库 细胞周期化合物库 TGF-beta/Smad信号通路库 抗阿尔茨海默病化合物库 | 点击展开 |
相关信号通路图
JNK抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| PC12 | Function Assay | 10 μM | 5 h | Activation of Nrf2/ARE assessed as HO-1 protein induction pretreated with SB203580 | 21345685 |
| PC12 | Function Assay | 10 μM | 5 h | Activation of Nrf2/ARE assessed as HO-1 protein induction pretreated with SP600125 | 21345685 |
| PC12 | Function Assay | 10 μM | 5 h | Activation of Nrf2/ARE assessed as HO-1 protein induction pretreated with U0126 | 21345685 |
| PC12 | Function Assay | 10 μM | 5 h | Activation of Nrf2/ARE assessed as HO-1 protein induction pretreated with PD98059 | 21345685 |
| A549 | Function Assay | 20 μM | 1 h | Inhibition of TPA-induced MMP-2 and u-PA expression | 20492175 |
| HaCaT | Function Assay | 20 μM | 24 h | Blocks the phosphorylation of c-Jun protein | 19812349 |
| HaCaT | Function Assay | 20 μM | 4 h | Blocks the TNF-α-induced CYP4F11 transcription | 19812349 |
| PC3 | Function Assay | 20 μM | 1 h | Decreases the MMP2 and MMP9 expression | 19633975 |
| RAW264.7 | Function Assay | 10 μM | 12 h | Antiinflammatory activity assessed as inhibition of LPS-induced NO production with IC50 of 17μM | 19497418 |
| BV-2 | Function Assay | 2 μM | 1 h | Inhibits the increase of sBAFF release in Gmix-treated BV-2 cells | 19406831 |
| Hep3B | Function Assay | 10 μM | 1 h | Blocks autophagy and upregulation of Beclin 1 expression induced by ceramide | 19060920 |
| LoVo | Function Assay | 1 μM | 1 h | Inhibition of PGE2-induced expression of uPA and MMP-9 significantly | 21859479 |
| LoVo | Function Assay | 1 μM | 1 h | BlocksPGE2-induced cell migration significantly | 21859479 |
| THP-1 | Function Assay | 90 nM | 30 min | Inhibition of tissue factor expression | 22940059 |
| PC3 | Function Assay | 25 μM | 24 h | Inhibition of AP-1 and p21 luciferase activity induced by S179D PRL | 23162652 |
| SH-SY5Y | Function Assay | 10 μM | 1 h | Neuroprotective activity assessed as reduction of anisomycin-induced cell death | 23498914 |
| SH-SY5Y | Kinase Assay | 10 μM | 1 h | Inhibition of JNK3 assessed as blockade of anisomycin-induced c-jun phosphorylation at ser73 | 23498914 |
| RAW264.7 | Function Assay | 10 μM | 24 h | Antiinflammatory activity assessed as inhibition of IL-1beta release | 23791078 |
| RAW264.7 | Function Assay | 10 μM | 24 h | Antiinflammatory activity assessed as inhibition of LPS-induced iNOS expression | 23791078 |
| RAW264.7 | Function Assay | 10 μM | 2 h | Antiinflammatory activity assessed as inhibition of LPS-induced NO production | 23791078 |
| A549 | Growth Inhibition Assay | 20 μM | 72 h | Rapid and potent inhibition of cell proliferation | 23912840 |
| BMMC | Function assay | 1 to 20 uM | 7 days | Inhibition of RANKL/M-CSF-stimulated osteoclastogenesis in ICR mouse BMMC assessed as reduction in TRAP positive multinucleated cells at 1 to 20 uM incubated for 7 days by light microscopy | 25397676 |
| Plasmodium falciparum GB4 | Antibacterial Assay | 72 h | Antiplasmodial activity with IC50 of 12.5893μM | 19734910 | |
| Plasmodium falciparum 3D7 | Antibacterial Assay | 72 h | Antiplasmodial activity with IC50 of 12.5893 μM | 19734910 | |
| Plasmodium falciparum 7G8 | Antibacterial Assay | 72 h | Antiplasmodial activity with IC50 of 10 μM | 19734910 | |
| Plasmodium falciparum W2 | Antibacterial Assay | 72 h | Antiplasmodial activity with IC50 of 7.94328 μM | 19734910 | |
| Plasmodium falciparum HB3 | Antibacterial Assay | 72 h | Antiplasmodial activity with IC50 of 7.94328 μM | 19734910 | |
| B16-F10 | Function Assay | 1 h | Inhibition of TNF-alpha-induced c-JUN phosphorylation | 21815634 | |
| RAW264.7 | Antiinflammatory assay | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production relative to control, IC50 = 17 μM. | 22831798 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | SP600125 (Nsc75890)是一种广谱JNK抑制剂，作用于JNK1、JNK2和JNK3，无细胞试验中IC50分别为40 nM、40 nM和90 nM，比作用于MKK4选择性高10倍，比作用于MKK3、MKK6、PKB和PKCα选择性高25倍，比作用于ERK2、p38、Chk1、EGFR等选择性高100倍。SP600125也是一种广谱的serine/threonine kinases抑制剂，包括Aurora kinase A、FLT3和TRKA，对应的IC50值为60 nM、90 nM和70 nM。SP600125可抑制自噬而激活细胞凋亡。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | SP600125是丝/苏氨酸激酶广谱抑制剂，有效抑制c-Jun 氨基末端激酶(JNK)。 | |||||||||||
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | SP600125是ATP竞争性的c-Jun氨基末端激酶(JNK)选择性抑制剂，IC50为40 nM 到90 nM。SP600125作用于Jurkat T细胞，抑制c-Jun磷酸化，IC50为5 μM 到10 μM。SP600125作用于CD4+细胞, 如从人脐血或外周血分离的Th0细胞，抑制细胞活化和分化，且抑制炎症基因 COX-2, IL-2, IL-10, IFN-γ,和TNF-α的表达, IC50为5 μM 到 12 μM。[1]然而,后期研究显示 SP600125 也抑制香烃受体(AhR)[2] Mps1,[3] 和一系列其他丝/苏氨酸激酶, 包括Aurora 激酶 A, FLT3, MELK,和 TRKA。[4] 20 μM SP600125作用于小鼠beta 细胞 MIN6, 诱导p38 MAPK 磷酸化，和其下游CREB依赖的 启动子的激活。[5] 20 μM SP600125 作用于HCT116细胞, 使有丝分裂停在G2期，且诱导核内复制。[6] |
|||
|---|---|---|---|---|
| 激酶实验 | 体外激酶实验 | |||
| 根据测量放射性磷酸转移到底物中的量，而测定SP600125作用于激酶的效果，包括MPS1, JNK, 和 Aurora 激酶 A。使用5 nM MPS1 重组蛋白在50 mM HEPES pH 7.5,2.5 mM MgCl2,1 mM MnCl2,1 mM DTT,3 μM NaVO3, 2 mM β-甘油磷酸,0.2 mg/mL BSA, 200 μM P38-βtide 底物-肽(KRQADEEMTGYVATRWYRAE),和含1.5 nM33P-γ-ATP的8 μM ATP中测量MPS1活性。使用1:3 稀释的(从30 μM 稀释成 1.5 nM) SP600125进行实验，然后测定IC50值。 | ||||
| 细胞实验 | 细胞系 | HCT116, A2780, 和U2OS细胞 | ||
| 浓度 | 0-5 μM | |||
| 孵育时间 | 72小时 | |||
| 方法 | 细胞接种在384孔板上。实验第一天,用SP600125处理细胞72小时，然后通过 CellTiter-Glo 实验处理实验板。测定与对照组相比，实验组的抑制活性，计算抑制增殖的IC50值。 |
|||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-JNK p-IGF1R / IGF1R / p-Akt / Akt / p-ERK / ERK p-Src / Src p-c-Jun / c-Jun / pJNK / JNK Survivin / Bcl-2 / PARP p-FADD / FADD / p-c-Jun / c-Jun |
|
25226534 | |
| Immunofluorescence | AIF / Endo G E-cadherin / β-catenin α-catenin / Actin |
|
21738692 | |
| Growth inhibition assay | Cell viability (U-87 MG) Cell viability (A549) |
|
27176481 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 |
SP600125按15 mg/kg或30 mg/kg剂量作用于小鼠，显著抑制脂多糖(LPS)诱导的TNF-α表达和CD3抗体诱导的CD4+ CD8+胸腺细胞凋亡。[1] |
|
|---|---|---|
| 动物实验 | Animal Models | 雌性 CD-1小鼠LPS/TNF模型 |
| Dosages | 15或30 mg/kg | |
| Administration | 静脉注射或口服处理 | |
化学信息&溶解度
| 分子量 | 220.23 | 分子式 | C14H8N2O |
| CAS号 | 129-56-6 | SDF | Download SP600125 SDF |
| Smiles | C1=CC=C2C(=C1)C3=NNC4=CC=CC(=C43)C2=O | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 44 mg/mL ( (199.79 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
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）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
技术支持
在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。
如果有其他问题，请给我们留言。
* 必填项
常见问题及建议解决方法
问题 1:
how to reconstitute the inhibitor for in vivo studies?
回答：
S1460 can be dissolved in 5% DMSO/corn oil at 5 mg/ml as a clear solution for injection. The inhibitor dissolved in vehicle 30% PEG400/0.5% Tween80/5%Propylene glycol, at 30mg/ml is a suspension and can be used for oral administration.
