SP600125

SP600125は、c-ジュンN末端キナーゼ(JNK)で最も有名な抑制によるセリン/トレオニン・キナーゼの幅広いスペクトル阻害剤で、 IC50 が 40 nM から、90 nMまで。

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SP600125 化学構造
分子量: 220.23

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製品説明

  • Compare JNK Inhibitors
    JNK製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法
  • SP600125のメカニズム

製品の説明

生物活性

製品説明 SP600125は、c-ジュンN末端キナーゼ(JNK)で最も有名な抑制によるセリン/トレオニン・キナーゼの幅広いスペクトル阻害剤で、 IC50 が 40 nM から、90 nMまで。
ターゲット JNK1 JNK2 JNK3 Aurora A Flt3 TRKA
IC50 40 nM 40 nM 90 nM [1] 60 nM 90 nM 70 nM [4]
In vitro試験 SP600125 is originally characterized as a selective ATP-competitive inhibitor of c-Jun N-terminal kinase JNK. In Jurkat T cells, SP600125 inhibits the phosphorylation of c-Jun with IC50 of 5 μM to 10 μM. In CD4+ cells, such as Th0 cells isolated from either human cord or peripheral blood, SP600125 blocks cell activation and differentiation and inhibits the expression of inflammatory genes COX-2, IL-2, IL-10, IFN-γ, and TNF-α, with IC50 of 5 μM to 12 μM. [1] However, later studies reveal that SP600125 also suppresses aryl hydrocarbon receptor (AhR) [2], Mps1 [3], and a panel of other serine/threonine kinases, including Aurora kinase A, FLT3, MELK, and TRKA [4]. In a mouse beta cells MIN6, SP600125 (20 μM) induces the phosphorylation of p38 MAPK and its downstream CREB-dependent promoter activation. [5] In HCT116 cells, SP600125 (20 μM) blocks the G2 phase to mitosis transition and induces endoreplication. This ability of SP600125 is independent of JNK inhibition, but due to its inhibition of CDK1-cyclin B activation upstream of Aurora A and Polo-like kinase 1. [6]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
Plasmodium falciparum HB3 M3\a[2FvfGmkYXP0[ZJq[WxiQYPzZZk> MkfWO|IhcA>? NUXVc4R3TE2VTx?= NHTR[GVCdnSrcHzhd41w\GmjbDDhZ5Rqfmm2eTD3bZRpKEmFNUCgc4YhPy57NEOyPEDPxE1? MoTaNVk4OzR7MUC=
Plasmodium falciparum W2 Mn22RY51cWKjY4TldolidCCDc4PhfS=> NX;MS3dFPzJiaB?= MmXOSG1UVw>? MlvJRY51cXCuYYPtc4Rq[WxiYXP0bZZqfHlid3n0bEBKSzVyIH;mJFcvQTR|Mkig{txO NIDIS|gyQTd|NEmxNC=>
Plasmodium falciparum 7G8 NY\FRm9rSW62aXLhZ5RmemmjbDDBd5NigQ>? M1vlR|czKGh? M4Dv[WROW09? NHjmR45CdnSrcHzhd41w\GmjbDDhZ5Rqfmm2eTD3bZRpKEmFNUCgc4YhOTBizszN NVrBOpduOTl5M{S5NVA>
Plasmodium falciparum 3D7 NYX3XW5qSW62aXLhZ5RmemmjbDDBd5NigQ>? M2\DVVczKGh? M17rc2ROW09? NH\SUo9CdnSrcHzhd41w\GmjbDDhZ5Rqfmm2eTD3bZRpKEmFNUCgc4YhOTJwNUi5N{DPxE1? NV3KO5BNOTl5M{S5NVA>
Plasmodium falciparum GB4 NFXnWXNCdnSrYnHjeIVzcWGuIFHzd4F6 M1vTV|czKGh? M3fHVGROW09? Mn7URY51cXCuYYPtc4Rq[WxiYXP0bZZqfHlid3n0bEBKSzVyIH;mJFEzNjV6OUROwG0> NYHyd|RIOTl5M{S5NVA>
RAW264.7 NXzDO|N[TnWwY4Tpc44hSXO|YYm= NXvnSItPOTBizszN NIr5fZkyOiCq NYfLT4tbSW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKE6RIIDyc4R2[3Srb36ge4l1cCCLQ{WwJI9nKDF5zszN MX:xPVQ6PzRzOB?=
SH-SY5Y MlHmSpVv[3Srb36gRZN{[Xl? NYHaWYVlOTBizszN M{n1U|EhcA>? NXHxWI9NTE2VTx?= M1XqUW5mfXKxcILveIVkfGm4ZTDhZ5Rqfmm2eTDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZiYX7pd49ugWOrbj3pcoR2[2WmIHPlcIwh\GWjdHi= MVKyN|Q6QDlzNB?=
SH-SY5Y Mn;0T4lv[XOnIFHzd4F6 NXPGd41NOTBizszN MoX1NUBp MnTFSG1UVw>? MVrJcohq[mm2aX;uJI9nKEqQS{OgZZN{\XO|ZXSgZZMh[myxY3vh[IUhd2ZiYX7pd49ugWOrbj3pcoR2[2WmIHOtbpVvKHCqb4PwbI9zgWyjdHnvckBifCC|ZYK3Ny=> NWLJS5FTOjN2OUi5NVQ>
RAW264.7 Ml7MSpVv[3Srb36gRZN{[Xl? NH7t[ZEyOCEQvF2= MYCyOEBp M3X2VmFvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDJUE0y[mW2YTDy[Yxm[XOn MVKyN|c6OTB5OB?=
RAW264.7 NILGSFVHfW6ldHnvckBCe3OjeR?= NWTudnpJOTBizszN NV;tdVZHOjRiaB?= M4LieGFvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDMVHMucW6mdXPl[EBqVk:VIHX4dJJme3Orb36= M4DaTlI{PzlzMEe4
RAW264.7 NVL5XldlTnWwY4Tpc44hSXO|YYm= MlTXNVAh|ryP NWLzZWlFOiCq M37vR2FvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDMVHMucW6mdXPl[EBPVyCycn;keYN1cW:w MVWyN|c6OTB5OB?=
B16-F10 NUm3TZBZTnWwY4Tpc44hSXO|YYm= NGDYNIgyKGh? M4\tXWlvcGmkaYTpc44hd2ZiVF7GMYFteGijLXnu[JVk\WRiYz3KWW4heGixc4Doc5J6dGG2aX;u M2GzXFIyQDF3NkO0
PC12 MoqySpVv[3Srb36gRZN{[Xl? M4T1NFExKM7:TR?= NIrM[HM2KGh? NXKycXhzTE2VTx?= NInZdoZC[3SrdnH0bY9vKG:oIF7y[lIwSVKHIHHzd4V{e2WmIHHzJGhQNTFicILveIVqdiCrbnT1Z5Rqd25icILleJJm[XSnZDD3bZRpKFCGOUiwOVk> Mn;MNlE{PDV4OEW=
PC12 NYTsbJNvTnWwY4Tpc44hSXO|YYm= M4nLXVExKM7:TR?= MkTpOUBp MVLEUXNQ MlfvRYN1cX[jdHnvckBw\iCQcn[yM2FTTSCjc4Pld5Nm\CCjczDIU{0yKHC{b4TlbY4hcW6mdXP0bY9vKHC{ZYTy[YF1\WRid3n0bEBWODF{Nh?= MofINlE{PDV4OEW=
PC12 MUfGeY5kfGmxbjDBd5NigQ>? M3nLNlExKM7:TR?= NIW2TXQ2KGh? MUDEUXNQ M1TPfmFkfGm4YYTpc44hd2ZiToLmNk9CWkViYYPz[ZN{\WRiYYOgTG8uOSCycn;0[YlvKGmwZIXjeIlwdiCycnX0doVifGWmIIfpeIghW1B4MECxNlU> MkHQNlE{PDV4OEW=
PC12 M{nvU2Z2dmO2aX;uJGF{e2G7 NV;6N|U3OTBizszN MkLIOUBp MWXEUXNQ MlLBRYN1cX[jdHnvckBw\iCQcn[yM2FTTSCjc4Pld5Nm\CCjczDIU{0yKHC{b4TlbY4hcW6mdXP0bY9vKHC{ZYTy[YF1\WRid3n0bEBUSjJyM{W4NC=> NX:5RldoOjF|NEW2PFU>
A549 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\a[nczOCEQvF2= MWm3NkBp MYPEUXNQ M2fpfHJieGmmIHHu[EBxd3SnboSgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25? M1LLUVI{QTF{OESw
PC3 M4n3R2Z2dmO2aX;uJGF{e2G7 NH\mWo0zPSEQvF2= MYiyOEBp NHr4e3ZKdmirYnn0bY9vKG:oIFHQMVEh[W6mIICyNUBtfWOrZnXyZZNmKGGldHn2bZR6KGmwZIXj[YQh[nliU{G3PWQhWFKO NHPmfHEzOzF4Mk[1Ni=>
THP-1 NEixXVFHfW6ldHnvckBCe3OjeR?= MkXQPVAhdk1? NFLy[HA{OCCvaX6= NITEXFhKdmirYnn0bY9vKG:oIITpd5N2\SCoYXP0c5Ih\XiycnXzd4lwdg>? NWruZYtSOjJ7NECwOVk>
LoVo Mn7ISpVv[3Srb36gRZN{[Xl? NIO0fZMyKM7:TR?= Mlj5NUBp MojCTY5pcWKrdHnvckBw\iCSR1WyMYlv\HWlZXSg[ZhxemW|c3nvckBw\iC3UFGgZY5lKE2PUD25JJNq\26rZnnjZY51dHl? MV:yNVg2QTR5OR?=
LoVo NVPFUoVvTnWwY4Tpc44hSXO|YYm= Mmi2NUDPxE1? MVOxJIg> M1zrS2Jtd2Otc2DHSVIucW6mdXPl[EBk\WyuIH3p[5JifGmxbjDzbYdvcW[rY3HueIx6 M3\j[lIyQDV7NEe5
A549 MVvGeY5kfGmxbjDBd5NigQ>? NFKxTVEzOCEQvF2= NWPte5dkOSCq MVXJcohq[mm2aX;uJI9nKFSSQT3pcoR2[2WmIF3NVE0zKGGwZDD1MXBCKGW6cILld5Nqd25? MVqyNFQ6OjF5NR?=
HaCaT M3ux[WZ2dmO2aX;uJGF{e2G7 NXfRdpEzOjBizszN NE\H[Wk1KGh? NF\0UGtFVVOR NV2yWYRTSmyxY3vzJJRp\SCWTl[t{tEucW6mdXPl[OKhS1mSNF[xNeKhfHKjboPjdolxfGmxbh?= NVPJZlh6OTl6MUKzOFk>
HaCaT MVvGeY5kfGmxbjDBd5NigQ>? NUnqToFrOjBizszN NILpSnczPCCq M3fVTGROW09? MkjDRoxw[2u|IITo[UBxcG:|cHjvdplt[XSrb36gc4Yh[y2MdX6gdJJwfGWrbh?= NF3CSFIyQThzMkO0PS=>
PC3 NHvNSo9HfW6ldHnvckBCe3OjeR?= M3zYUFIxKM7:TR?= MVexJIg> NFnXZ2lF\WO{ZXHz[ZMhfGinIF3NVFIh[W6mIF3NVFkh\XiycnXzd4lwdg>? NHKyRYIyQTZ|M{m3OS=>
BV-2 NYnNNo1ZTnWwY4Tpc44hSXO|YYm= MXSyJO69VQ>? MXKxJIg> MWTJcohq[mm2czD0bIUhcW6lcnXhd4Uhd2Zic1LBSmYhemWuZXHz[UBqdiCJbXn4MZRz\WG2ZXSgRnYuOiClZXzsdy=> MVixPVQxPjh|MR?=
Hep3B MX7GeY5kfGmxbjDBd5NigQ>? M{PBflExKM7:TR?= NVX2U4tFOSCq NIfXcppDdG:la4OgZZV1d3CqYXf5JIFv\CC3cILl[5Vt[XSrb36gc4YhSmWlbHnuJFEh\XiycnXzd4lwdiCrbnT1Z4VlKGK7IHPldoFucWSn NIHHTIsyQTB4MEmyNC=>

... Click to View More Cell Line Experimental Data

In vivo試験 In mice, SP600125 (15 mg/kg or 30 mg/kg) significantly inhibits lipopolysaccharide (LPS)-induced TNF-α expression and anti-CD3-induced apoptosis of CD4+ CD8+ thymocytes. [1]
臨床試験
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [4]

In Vitro Kinase Assays The potency of SP600125 towards kinases, including MPS1, JNK, and Aurora kinase A, is determined based on the specific measurement of radioactive phosphotransfer to the substrate. For each enzyme, the absolute Km values for ATP and the specific substrate are initially determined and each assay is then run at optimized [ATP] (2·αKm) and [substrate] (5·Km) concentrations. MPS1 activity is measured using 5 nM of MPS1 recombinant protein in 50 mM HEPES pH 7.5, 2.5 mM MgCl2, 1 mM MnCl2, 1 mM DTT, 3 μM NaVO3, 2 mM β-glycerophosphate, 0.2 mg/mL BSA, 200 μM P38-βtide substrate-peptide (KRQADEEMTGYVATRWYRAE), and 8 μM ATP with 1.5 nM 33P-γ-ATP. Ten serial 1:3 dilutions (from 30 μM to 1.5 nM) of SP600125 are tested and IC50 determined.

細胞アッセイ: [4]

細胞株 HCT116, A2780, and U2OS cells
濃度 0–5 μM, dissolved in 0.1% DMSO
反応時間 72 hours
実験の流れ Cells are seeded in 384 well-plates. One day after seeding, the cells are treated with SP600125 for 72 hours and the plates are then processed using a CellTiter-Glo assay. Inhibitory activity is evaluated comparing treated versus control data and IC50 value of proliferation is calculated.

動物実験: [1]

動物モデル Mouse LPS/TNF model (female CD-1)
製剤 Dissolved in PPCES (30% PEG-400/20% polypropylene glycol/15% Cremophor EL/5% ethanol/30% saline)
投薬量 15 or 30 mg/kg
投与方法 Administered via intravenous injection or orally

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download SP600125 SDF
分子量 220.23
化学式

C14H8N2O

CAS No. 129-56-6
保管 2年-20℃
6月-80℃in solvent
別名 Nsc75890
溶解度 (25°C) * In vitro DMSO 44 mg/mL (199.79 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 5% DMSO+corn oil 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 2H-Dibenzo[cd,g]indazol-6-one

カスタマーフィードバック (4)


Click to enlarge
Rating
Source Cancer Res, 2013, 73(20):6346-58. SP600125 purchased from Selleck
Method Immunoblot analysis
Cell Lines MDA-231 cells
Concentrations 10 uM
Incubation Time 24 h
Results cJUN phosphorylation and expression were downregulated by both the SP600125 and selumetinib, with maximal inhibition by the combination.

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Rating
Source Lee lay hoon from National University of Singapore. SP600125 purchased from Selleck
Method ELISA
Cell Lines Bone marrow derived macrophages
Concentrations 10-20 μM
Incubation Time 24 h
Results SP600125 treatment resulted in a reduction of TNF-a production.

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Rating
Source SP600125 purchased from Selleck
Method Sectional Immunohistochemistry
Cell Lines E14.5 male UGSs
Concentrations 10 μM
Incubation Time 4 d
Results Cell elongation index measured from spindle-like morphology was used to d etermine the effect of individual inhibitors. Prevention of MSP-induced spindle-like morphology was not observed in M-RON cells treated with w ortmannin, SB203580, SP600125, Cay10512, and S 31-201, suggesting that signaling from these pathways was not involved in MSP-induced EMT. A moderate effect, based on changes in elongation index, was s een w hen rapa mycin, vismode-gi b, and XAV- 939 were ap plied, suggesti ng that s ignal-ing f rom H edgeho g, Wnt / b -catenin, a nd FRAP /mTOR pathwa ys played a role i n MSP-induced EMT.

Click to enlarge
Rating
Source Biochim Biophys Acta, 2012, 1823(5), 987-96. SP600125 purchased from Selleck
Method Immunofluorescence
Cell Lines HC11 cells
Concentrations 50 µM
Incubation Time 1 h
Results whole ADRP levels, estimated by Western blot , decreased only in the presence of MK -2206 and LY294002. In most cases, ADRP decorated the surface of small lipid droplets and appeared as little patches on large cytoplasmic lipid droplets. With the exception of SP600125, which induced a strong ADRP coating of almost all cytoplasmic lipid droplets (although this inhibitor did not increase ADRP synthesis), variation in the distribution of ADRP at the surface of lipid droplet was difficult to estimate, notably because the signal was faint and uneven.

文献中の引用 (46)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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