SP600125

目录号:S1460 别名: Nsc75890

SP600125 Chemical Structure

Molecular Weight(MW): 220.23

SP600125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。

规格 价格 库存 购买数量  
RMB 1554.71 现货
RMB 633.17 现货
RMB 2011.01 现货
RMB 4814.33 现货
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客户购买Selleck的此次产品后发表的文献48篇:

客户使用该产品的4个实验数据:

  • Loss of DUSP4 function upregulates IL-6 and IL-8 and enhances mammosphere growth. Immunoblot analysis of MDA-231 cells after treatment of 24 hours with 1 umol/L selumetinib (MEKi) or 10 umol/L SP600125 (JNKi). I, MDA-231 mammosphere formation quantitated by GelCount software 7 days after siRNA transfection. Where indicated, selumetinib (MEKi) or SP600125 (JNK1) or the combination was added to the mammosphere cultures.

    Cancer Res 2013 73(20):6346-58. SP600125 purchased from Selleck.

    Comparative effects of inhibitors by immunofluorescence microscopy study. Confluent HC11 cells were grown on poly-L-lysine-coated glass coverslips (immunofluorescence) and on plastic plates (biochemical control) and then treated with inhibitors according to the standard procedure. Upper part: the biochemical action of the inhibitors was tested to validate the immunofluorescence results. Cellular proteins were analyzed by SDS-PAGE and the immunoblots were successively probed with anti-ADRP, anti-β-casein, and anti- β-actin antibodies and their respective HRP-conjugated secondary antibodies. Each experimental condition was performed in duplicate. Lower part: cells were fixed, permeabilized and subjected to immunofluorescence microscopy using antiserum against ADRP and TRITC-conjugated secondary antibody (red).

    Biochim Biophys Acta 2012 1823(5), 987-96. SP600125 purchased from Selleck.

  • Bone marrow derived macrophages were pre-treated with the indicated concentrations of SP600125 for 1h prior to LPS treatment (100 ng/ml).  TNF-a production was analyzed 24h later.

    Lee lay hoon from National University of Singapore. SP600125 purchased from Selleck.

    SP600125 purchased from Selleck.

产品安全说明书

JNK抑制剂选择性比较

生物活性

产品描述 SP600125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。
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
JNK1 [1]
(Cell-free assay)
JNK2 [1]
(Cell-free assay)
Aurora A [4]
(Cell-free assay)
TrkA [4]
(Cell-free assay)
JNK3 [1]
(Cell-free assay)
40 nM 40 nM 60 nM 70 nM 90 nM
体外研究

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Plasmodium falciparum HB3 NX\KOJZrSW62aXLhZ5RmemmjbDDBd5NigQ>? NWrXZm86PzJiaB?= MXzEUXNQ MnjhRY51cXCuYYPtc4Rq[WxiYXP0bZZqfHlid3n0bEBKSzVyIH;mJFcvQTR|Mkig{txO NWD3WHdiOTl5M{S5NVA>
Plasmodium falciparum W2 M{XYc2FvfGmkYXP0[ZJq[WxiQYPzZZk> M3;TbVczKGh? NUfUPWx7TE2VTx?= NGTMNoJCdnSrcHzhd41w\GmjbDDhZ5Rqfmm2eTD3bZRpKEmFNUCgc4YhPy57NEOyPEDPxE1? NHnyW2MyQTd|NEmxNC=>
Plasmodium falciparum 7G8 MlrhRY51cWKjY4TldolidCCDc4PhfS=> MWK3NkBp NGLzRZlFVVOR MYHBcpRqeGyjc33v[IlidCCjY4Tpeol1gSC5aYToJGlEPTBib3[gNVAh|ryP NHvHWnAyQTd|NEmxNC=>
Plasmodium falciparum 3D7 NYixcnl6SW62aXLhZ5RmemmjbDDBd5NigQ>? MVq3NkBp Mom5SG1UVw>? M3Xp[WFvfGmybHHzcY9lcWGuIHHjeIl3cXS7IIfpeIghUUN3MDDv[kAyOi53OEmzJO69VQ>? NWT4RnVbOTl5M{S5NVA>
Plasmodium falciparum GB4 NXSwfJZSSW62aXLhZ5RmemmjbDDBd5NigQ>? MnPsO|IhcA>? NV3CSmZZTE2VTx?= M4TnWWFvfGmybHHzcY9lcWGuIHHjeIl3cXS7IIfpeIghUUN3MDDv[kAyOi53OEmz{txO NUn0emx3OTl5M{S5NVA>
RAW264.7 NVnsVZZuTnWwY4Tpc44hSXO|YYm= NVvad2xYOTBizszN MoS2NVIhcA>? NIj6WlhCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gUHBUNWmwZIXj[YQhVk9icILv[JVkfGmxbjD3bZRpKEmFNUCgc4YhOTgQvF2= M4D6c|E6PDl5NEG4
SH-SY5Y NX7nbGVkTnWwY4Tpc44hSXO|YYm= MoXNNVAh|ryP MlTuNUBp NHva[VJFVVOR MV\O[ZVzd3C{b4TlZ5RqfmViYXP0bZZqfHliYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKGGwaYPvcZlkcW5vaX7keYNm\CClZXzsJIRm[XSq MmDaNlM1QTh7MUS=
SH-SY5Y Mof4T4lv[XOnIFHzd4F6 M3;vU|ExKM7:TR?= NV\n[IpzOSCq MXvEUXNQ Mn3xTY5pcWKrdHnvckBw\iCMTluzJIF{e2W|c3XkJIF{KGKub3PrZYRmKG:oIHHubZNwdXmlaX6tbY5lfWOnZDDjMYp2diCyaH;zdIhwenmuYYTpc44h[XRic3XyO|M> NF7FcXQzOzR7OEmxOC=>
RAW264.7 MXTGeY5kfGmxbjDBd5NigQ>? M4jPN|ExKM7:TR?= MViyOEBp MnvrRY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFnMMVFj\XSjIILlcIVie2V? MknVNlM4QTFyN{i=
RAW264.7 M3T6fGZ2dmO2aX;uJGF{e2G7 NXPtcYJtOTBizszN MYWyOEBp M3HOc2FvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDMVHMucW6mdXPl[EBqVk:VIHX4dJJme3Orb36= MnjtNlM4QTFyN{i=
RAW264.7 M{izc2Z2dmO2aX;uJGF{e2G7 MlztNVAh|ryP MVqyJIg> MV;BcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgUm8heHKxZIXjeIlwdg>? NHj2bXUzOzd7MUC3PC=>
B16-F10 NFHsU|VHfW6ldHnvckBCe3OjeR?= MnPjNUBp NHS4e|VKdmirYnn0bY9vKG:oIGTOSk1idHCqYT3pcoR2[2WmIHOtTnVPKHCqb4PwbI9zgWyjdHnvci=> MnToNlE5OTV4M{S=
PC12 NYHVZWQ2TnWwY4Tpc44hSXO|YYm= MkDGNVAh|ryP NGjzXmo2KGh? M{LnZmROW09? M3HqXWFkfGm4YYTpc44hd2ZiToLmNk9CWkViYYPz[ZN{\WRiYYOgTG8uOSCycn;0[YlvKGmwZIXjeIlwdiCycnX0doVifGWmIIfpeIghWER7OEC1PS=> MVKyNVM1PTZ6NR?=
PC12 MmPXSpVv[3Srb36gRZN{[Xl? MX:xNEDPxE1? MnTnOUBp Mn[4SG1UVw>? M{TNTmFkfGm4YYTpc44hd2ZiToLmNk9CWkViYYPz[ZN{\WRiYYOgTG8uOSCycn;0[YlvKGmwZIXjeIlwdiCycnX0doVifGWmIIfpeIghXTBzMk[= MkXaNlE{PDV4OEW=
PC12 NFq1[5JHfW6ldHnvckBCe3OjeR?= MmTSNVAh|ryP MofXOUBp NX;BZ2p5TE2VTx?= NYrYUI5jSWO2aY\heIlwdiCxZjDOdoYzN0GURTDhd5Nme3OnZDDhd{BJVy1zIIDyc5RmcW5iaX7keYN1cW:wIIDy[ZRz\WG2ZXSge4l1cCCVUE[wNFEzPQ>? MYqyNVM1PTZ6NR?=
PC12 NELMXXdHfW6ldHnvckBCe3OjeR?= M4DlR|ExKM7:TR?= NYLlToZ3PSCq M{LiT2ROW09? MoP6RYN1cX[jdHnvckBw\iCQcn[yM2FTTSCjc4Pld5Nm\CCjczDIU{0yKHC{b4TlbY4hcW6mdXP0bY9vKHC{ZYTy[YF1\WRid3n0bEBUSjJyM{W4NC=> NI[xXHIzOTN2NU[4OS=>
A549 Mo\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWeyNEDPxE1? MoDoO|IhcA>? NUTDeVhtTE2VTx?= NIjmZoNT[XCrZDDhcoQheG:2ZX70JIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:w M2nmVFI{QTF{OESw
PC3 NYrndZdpTnWwY4Tpc44hSXO|YYm= MVmyOUDPxE1? MmP5NlQhcA>? NGfkeI5KdmirYnn0bY9vKG:oIFHQMVEh[W6mIICyNUBtfWOrZnXyZZNmKGGldHn2bZR6KGmwZIXj[YQh[nliU{G3PWQhWFKO MW[yN|E3OjZ3Mh?=
THP-1 MWrGeY5kfGmxbjDBd5NigQ>? NXLLV3F5QTBibl2= NH:xeJg{OCCvaX6= MYnJcohq[mm2aX;uJI9nKHSrc4P1[UBn[WO2b4Kg[ZhxemW|c3nvci=> MXiyNlk1ODB3OR?=
LoVo M3m4WWZ2dmO2aX;uJGF{e2G7 NGXKWIIyKM7:TR?= MW[xJIg> NGL5N5NKdmirYnn0bY9vKG:oIGDHSVIucW6mdXPl[EBmgHC{ZYPzbY9vKG:oIIXQRUBidmRiTV3QMVkhe2mpbnnmbYNidnSueR?= MlPwNlE5PTl2N{m=
LoVo NHfW[I9HfW6ldHnvckBCe3OjeR?= MmHpNUDPxE1? MnXVNUBp NVfIR4UzSmyxY3vzVGdGOi2rbnT1Z4VlKGOnbHygcYloemG2aX;uJJNq\26rZnnjZY51dHl? MWmyNVg2QTR5OR?=
A549 NFXKfINHfW6ldHnvckBCe3OjeR?= NX\QeJhKOjBizszN MljBNUBp MWHJcohq[mm2aX;uJI9nKFSSQT3pcoR2[2WmIF3NVE0zKGGwZDD1MXBCKGW6cILld5Nqd25? NX;5bXBZOjB2OUKxO|U>
HaCaT Ml7aSpVv[3Srb36gRZN{[Xl? NIrCWIczOCEQvF2= MYC0JIg> MnjVSG1UVw>? MUnCcI9kc3NidHjlJHRPTi4QsT3pcoR2[2WmwrDDXXA1TjFzwrD0doFve2O{aYD0bY9v MoDmNVk5OTJ|NEm=
HaCaT NFPJc4dHfW6ldHnvckBCe3OjeR?= MWeyNEDPxE1? MnTlNlQhcA>? M3fTbmROW09? M3SxSWJtd2OtczD0bIUheGixc4Doc5J6dGG2aX;uJI9nKGNvSoXuJJBzd3SnaX6= NY\HcYkzOTl6MUKzOFk>
PC3 NX;jSHpkTnWwY4Tpc44hSXO|YYm= Ml3zNlAh|ryP NFfqSYwyKGh? MWPE[YNz\WG|ZYOgeIhmKE2PUEKgZY5lKE2PUEmg[ZhxemW|c3nvci=> Mn73NVk3OzN7N{W=
BV-2 NYfHZWhnTnWwY4Tpc44hSXO|YYm= MorzNkDPxE1? NWm2R|NiOSCq M4LIe2lvcGmkaYTzJJRp\SCrbnPy[YF{\SCxZjDzRmFHTiC{ZXzlZZNmKGmwIFftbZgufHKnYYTl[EBDXi1{IHPlcIx{ NWjtWXZNOTl2ME[4N|E>
Hep3B NH7BOo1HfW6ldHnvckBCe3OjeR?= NGOyU|AyOCEQvF2= NEnU[VUyKGh? M{HTb2Jtd2OtczDheZRweGijZ4mgZY5lKHWycnXneYxifGmxbjDv[kBD\WOuaX6gNUBmgHC{ZYPzbY9vKGmwZIXj[YQh[nliY3XyZY1q\GV? MknmNVkxPjB7MkC=

... Click to View More Cell Line Experimental Data

体内研究 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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[4]
+ 展开

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: [4]
+ 展开
  • Cell lines: HCT116, A2780, 和U2OS细胞
  • Concentrations: 0-5 μM, 溶于0.1% DMSO
  • Incubation Time: 72小时
  • Method: 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。
    (Only for Reference)
动物实验:[1]
+ 展开
  • Animal Models: 雌性 CD-1小鼠LPS/TNF模型
  • Formulation: 溶于PPCES (30% PEG-400/20% 聚丙二醇/15% Cremophor EL/5% 乙醇/30% 盐水)
  • Dosages: 15或30 mg/kg
  • Administration: 静脉注射或口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 44 mg/mL (199.79 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
3mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 220.23
化学式

C14H8N2O

CAS号 129-56-6
稳定性 powder
in solvent
别名 Nsc75890

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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。

操作手册

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.

JNK Signaling Pathway Map

相关JNK产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID