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SP600125
僅限科研使用
SP600125
別名: Nsc75890
SP600125 (Nsc75890)是一種廣譜JNK抑制劑，作用于JNK1、JNK2和JNK3，無細胞試驗中IC50分別為40 nM、40 nM和90 nM，比作用于MKK4選擇性高10倍，比作用于MKK3、MKK6、PKB和PKCα選擇性高25倍，比作用于ERK2、p38、Chk1、EGFR等選擇性高100倍。SP600125也是一種廣譜的serine/threonine kinases抑制劑，包括Aurora kinase A、FLT3和TRKA，對應的IC50值為60?nM、90?nM和70?nM。SP600125可抑制自噬而激活細胞凋亡。
SP600125 Chemical Structure
CAS: 129-56-6
產(chǎn)品質(zhì)控
批次：
純度：
99.94%
99.94
常與SP600125一起在實驗中被使用的化合物
SP600125和PD98059是兩種在TQ誘導的細胞死亡中具有促生存活性的激酶。
SP600125和SCH772984在體外顯著增加PMN-MDSC和M-MDSC的凋亡。
SP600125和LY294002抑制SNU-216和NCI-N87細胞的生長。
Choi Y, et al. World J Gastroenterol. 2016 Nov 7; 22(41): 9141–9153.
SP600125和Bentamapimod是泛JNK抑制劑，可導致GBM干細胞(GSC)培養(yǎng)物中的細胞活力大幅降低。
SP600125相關(guān)產(chǎn)品
| 相關(guān)靶點 | JNK1 JNK2 JNK3 | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | JNK-IN-8 Anisomycin JNK Inhibitor IX Tanzisertib HCl(CC-930) JNK Inhibitor VIII Bentamapimod (AS602801) BI-78D3 SP 600125, negative control DTP3 CC-401 Hydrochloride Polyphyllin I | 點擊展開 |
| 相關(guān)化合物庫 | 激酶抑制劑庫 MAPK抑制劑庫 細胞周期化合物庫 TGF-beta/Smad信號通路庫 抗阿爾茨海默病化合物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | SP600125 (Nsc75890)是一種廣譜JNK抑制劑，作用于JNK1、JNK2和JNK3，無細胞試驗中IC50分別為40 nM、40 nM和90 nM，比作用于MKK4選擇性高10倍，比作用于MKK3、MKK6、PKB和PKCα選擇性高25倍，比作用于ERK2、p38、Chk1、EGFR等選擇性高100倍。SP600125也是一種廣譜的serine/threonine kinases抑制劑，包括Aurora kinase A、FLT3和TRKA，對應的IC50值為60?nM、90?nM和70?nM。SP600125可抑制自噬而激活細胞凋亡。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | SP600125是絲/蘇氨酸激酶廣譜抑制劑，有效抑制c-Jun 氨基末端激酶(JNK)。 | |||||||||||
| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | SP600125是ATP競爭性的c-Jun氨基末端激酶(JNK)選擇性抑制劑，IC50為40 nM 到90 nM。SP600125作用于Jurkat T細胞，抑制c-Jun磷酸化，IC50為5 μM 到10 μM。SP600125作用于CD4+細胞, 如從人臍血或外周血分離的Th0細胞，抑制細胞活化和分化，且抑制炎癥基因 COX-2, IL-2, IL-10, IFN-γ,和TNF-α的表達, IC50為5 μM 到 12 μM。[1]然而,后期研究顯示 SP600125 也抑制香烴受體(AhR)[2] Mps1,[3] 和一系列其他絲/蘇氨酸激酶, 包括Aurora 激酶 A, FLT3, MELK,和 TRKA。[4] 20 μM SP600125作用于小鼠beta 細胞 MIN6, 誘導p38 MAPK 磷酸化，和其下游CREB依賴的 啟動子的激活。[5] 20 μM SP600125 作用于HCT116細胞, 使有絲分裂停在G2期，且誘導核內(nèi)復制。[6] |
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|---|---|---|---|---|
| 激酶實驗 | 體外激酶實驗 | |||
| 根據(jù)測量放射性磷酸轉(zhuǎn)移到底物中的量，而測定SP600125作用于激酶的效果，包括MPS1, JNK, 和 Aurora 激酶 A。使用5 nM MPS1 重組蛋白在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中測量MPS1活性。使用1:3 稀釋的(從30 μM 稀釋成 1.5 nM) SP600125進行實驗，然后測定IC50值。 | ||||
| 細胞實驗 | 細胞系 | HCT116, A2780, 和U2OS細胞 | ||
| 濃度 | 0-5 μM | |||
| 孵育時間 | 72小時 | |||
| 方法 | 細胞接種在384孔板上。實驗第一天,用SP600125處理細胞72小時，然后通過 CellTiter-Glo 實驗處理實驗板。測定與對照組相比，實驗組的抑制活性，計算抑制增殖的IC50值。 |
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| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | 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 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | SP600125按15 mg/kg或30 mg/kg劑量作用于小鼠，顯著抑制脂多糖(LPS)誘導的TNF-α表達和CD3抗體誘導的CD4+ CD8+胸腺細胞凋亡。[1] |
|
|---|---|---|
| 動物實驗 | Animal Models | 雌性 CD-1小鼠LPS/TNF模型 |
| Dosages | 15或30 mg/kg | |
| Administration | 靜脈注射或口服處理 | |
化學信息&溶解度
| 分子量 | 220.23 | 分子式 | C14H8N2O |
| CAS號 | 129-56-6 | SDF | Download SP600125 SDF |
| Smiles | C1=CC=C2C(=C1)C3=NNC4=CC=CC(=C43)C2=O | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 60 mg/mL ( (272.44 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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常見問題及建議解決方法
問題 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.
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