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 MYrBcpRq[mGldHXybYFtKEG|c3H5 MXO3NkBp M2q1fWROW09? NIj1WYZCdnSrcHzhd41w\GmjbDDhZ5Rqfmm2eTD3bZRpKEmFNUCgc4YhPy57NEOyPEDPxE1? M1PmTVE6PzN2OUGw
Plasmodium falciparum W2 M{HDNWFvfGmkYXP0[ZJq[WxiQYPzZZk> MXi3NkBp NUL5TXRoTE2VTx?= MWTBcpRqeGyjc33v[IlidCCjY4Tpeol1gSC5aYToJGlEPTBib3[gO{46PDN{ODFOwG0> NEjYdWkyQTd|NEmxNC=>
Plasmodium falciparum 7G8 NW\DSZBuSW62aXLhZ5RmemmjbDDBd5NigQ>? M2KxbFczKGh? M3PnfmROW09? MkfhRY51cXCuYYPtc4Rq[WxiYXP0bZZqfHlid3n0bEBKSzVyIH;mJFExKM7:TR?= M2\wbVE6PzN2OUGw
Plasmodium falciparum 3D7 NEPqVY1CdnSrYnHjeIVzcWGuIFHzd4F6 MVu3NkBp MmftSG1UVw>? M2rvPGFvfGmybHHzcY9lcWGuIHHjeIl3cXS7IIfpeIghUUN3MDDv[kAyOi53OEmzJO69VQ>? M4K5NlE6PzN2OUGw
Plasmodium falciparum GB4 MYPBcpRq[mGldHXybYFtKEG|c3H5 Mn7VO|IhcA>? MX;EUXNQ NYrnNWI6SW62aYDsZZNud2SrYXygZYN1cX[rdImge4l1cCCLQ{WwJI9nKDF{LkW4PVPPxE1? Mk\HNVk4OzR7MUC=
RAW264.7 NE\qOHFHfW6ldHnvckBCe3OjeR?= NV3hd4dUOTBizszN MVyxNkBp MXfBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgUm8heHKxZIXjeIlwdiC5aYToJGlEPTBib3[gNVfPxE1? NGfqSI8yQTR7N{SxPC=>
SH-SY5Y MmTnSpVv[3Srb36gRZN{[Xl? NF3hXlIyOCEQvF2= M1\LVVEhcA>? NWfCOll1TE2VTx?= Mkf6UoV2em:ycn;0[YN1cX[nIHHjeIl3cXS7IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iCjbnnzc416[2mwLXnu[JVk\WRiY3XscEBl\WG2aB?= MVWyN|Q6QDlzNB?=
SH-SY5Y MXrLbY5ie2ViQYPzZZk> NUjic3d3OTBizszN M2W5dVEhcA>? MV;EUXNQ NILoXlhKdmirYnn0bY9vKG:oIFrOT|Mh[XO|ZYPz[YQh[XNiYnzvZ4ti\GVib3[gZY5qe2:veXPpck1qdmS3Y3XkJIMucnWwIIDoc5NxcG:{eXzheIlwdiCjdDDz[ZI4Ow>? NVX3bXFDOjN2OUi5NVQ>
RAW264.7 MVTGeY5kfGmxbjDBd5NigQ>? M1:xRlExKM7:TR?= MV[yOEBp MY\BcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiSVytNYJmfGFicnXs[YF{\Q>? M4PBPVI{PzlzMEe4
RAW264.7 NFjCOIxHfW6ldHnvckBCe3OjeR?= NVPLd5N[OTBizszN M1HmflI1KGh? M3rkW2FvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDMVHMucW6mdXPl[EBqVk:VIHX4dJJme3Orb36= MoHZNlM4QTFyN{i=
RAW264.7 NVP3RnZTTnWwY4Tpc44hSXO|YYm= MVuxNEDPxE1? M4G5blIhcA>? MoPJRY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFzQV{1qdmS3Y3XkJG5QKHC{b3T1Z5Rqd25? NGjpR2kzOzd7MUC3PC=>
B16-F10 Ml3jSpVv[3Srb36gRZN{[Xl? MVuxJIg> M3m3bWlvcGmkaYTpc44hd2ZiVF7GMYFteGijLXnu[JVk\WRiYz3KWW4heGixc4Doc5J6dGG2aX;u M1fpcFIyQDF3NkO0
PC12 MmHaSpVv[3Srb36gRZN{[Xl? MX:xNEDPxE1? MUG1JIg> MYPEUXNQ NEDDO2JC[3SrdnH0bY9vKG:oIF7y[lIwSVKHIHHzd4V{e2WmIHHzJGhQNTFicILveIVqdiCrbnT1Z5Rqd25icILleJJm[XSnZDD3bZRpKFCGOUiwOVk> Ml\pNlE{PDV4OEW=
PC12 MVfGeY5kfGmxbjDBd5NigQ>? MlrzNVAh|ryP MW[1JIg> M{PoNGROW09? NWHzZ|ZNSWO2aY\heIlwdiCxZjDOdoYzN0GURTDhd5Nme3OnZDDhd{BJVy1zIIDyc5RmcW5iaX7keYN1cW:wIIDy[ZRz\WG2ZXSge4l1cCCXMEGyOi=> MXeyNVM1PTZ6NR?=
PC12 MlruSpVv[3Srb36gRZN{[Xl? NH7NdlIyOCEQvF2= NUnHNoVSPSCq MVTEUXNQ NUX0[Vl5SWO2aY\heIlwdiCxZjDOdoYzN0GURTDhd5Nme3OnZDDhd{BJVy1zIIDyc5RmcW5iaX7keYN1cW:wIIDy[ZRz\WG2ZXSge4l1cCCVUE[wNFEzPQ>? M2XXPFIyOzR3Nki1
PC12 MWDGeY5kfGmxbjDBd5NigQ>? M{\yelExKM7:TR?= MX[1JIg> M3\R[WROW09? M4CzOGFkfGm4YYTpc44hd2ZiToLmNk9CWkViYYPz[ZN{\WRiYYOgTG8uOSCycn;0[YlvKGmwZIXjeIlwdiCycnX0doVifGWmIIfpeIghW0J{MEO1PFA> MXSyNVM1PTZ6NR?=
A549 MlW3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M124SVIxKM7:TR?= Mlq0O|IhcA>? M1iwemROW09? MUfSZZBq\CCjbnSgdI91\W62IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9v MUKyN|kyOjh2MB?=
PC3 M{\qRWZ2dmO2aX;uJGF{e2G7 Mn7QNlUh|ryP M4nXXVI1KGh? MV7Jcohq[mm2aX;uJI9nKEGSLUGgZY5lKHB{MTDseYNq\mW{YYPlJIFkfGm4aYT5JIlv\HWlZXSgZpkhWzF5OVSgVHJN M3rJdVI{OTZ{NkWy
THP-1 MUDGeY5kfGmxbjDBd5NigQ>? M3jXelkxKG6P NXrENHk3OzBibXnu MkHITY5pcWKrdHnvckBw\iC2aYPzeYUh\mGldH;yJIV5eHKnc4Ppc44> NH;tZmQzOjl2MEC1PS=>
LoVo MmTaSpVv[3Srb36gRZN{[Xl? NWLvXlVHOSEQvF2= MoCyNUBp MmftTY5pcWKrdHnvckBw\iCSR1WyMYlv\HWlZXSg[ZhxemW|c3nvckBw\iC3UFGgZY5lKE2PUD25JJNq\26rZnnjZY51dHl? MXuyNVg2QTR5OR?=
LoVo M13j[mZ2dmO2aX;uJGF{e2G7 NV:0epFkOSEQvF2= MVyxJIg> NIfNRphDdG:la4PQS2UzNWmwZIXj[YQh[2WubDDtbYdz[XSrb36gd4lodmmoaXPhcpRtgQ>? NVXRXXlGOjF6NUm0O|k>
A549 MkftSpVv[3Srb36gRZN{[Xl? MWeyNEDPxE1? NFW4[HEyKGh? MUXJcohq[mm2aX;uJI9nKFSSQT3pcoR2[2WmIF3NVE0zKGGwZDD1MXBCKGW6cILld5Nqd25? M2PaWFIxPDl{MUe1
HaCaT M{nTSmZ2dmO2aX;uJGF{e2G7 M3zWflIxKM7:TR?= NH:3PXQ1KGh? MYHEUXNQ MonxRoxw[2u|IITo[UBVVkZvzsGtbY5lfWOnZNMgR3lRPEZzMdMgeJJidnOlcnnweIlwdg>? M1iyeVE6QDF{M{S5
HaCaT NFHvVoZHfW6ldHnvckBCe3OjeR?= MnPiNlAh|ryP MViyOEBp NV;6VFNvTE2VTx?= NH7TTXlDdG:la4OgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iClLVr1ckBxem:2ZXnu NYfJOpRIOTl6MUKzOFk>
PC3 NYfZVlhXTnWwY4Tpc44hSXO|YYm= M{X0O|IxKM7:TR?= M2G0W|EhcA>? Mn7GSIVkemWjc3XzJJRp\SCPTWCyJIFv\CCPTWC5JIV5eHKnc4Ppc44> NGTyXpIyQTZ|M{m3OS=>
BV-2 MWrGeY5kfGmxbjDBd5NigQ>? MWCyJO69VQ>? NXn3Z|N1OSCq Moe4TY5pcWKrdIOgeIhmKGmwY4LlZZNmKG:oIIPCRWZHKHKnbHXhd4UhcW5iR33pfE11emWjdHXkJGJXNTJiY3XscJM> NHzp[mIyQTRyNkizNS=>
Hep3B MlWwSpVv[3Srb36gRZN{[Xl? MoDuNVAh|ryP M{i3WlEhcA>? M4LybGJtd2OtczDheZRweGijZ4mgZY5lKHWycnXneYxifGmxbjDv[kBD\WOuaX6gNUBmgHC{ZYPzbY9vKGmwZIXj[YQh[nliY3XyZY1q\GV? NUTXUnByOTlyNkC5NlA>

... 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 3年-20℃
2年-80℃in solvent
別名 Nsc75890
溶解度 (25°C) * In vitro DMSO 44 mg/mL (199.79 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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

文献中の引用 (46)

Frequently Asked Questions

  • Question 1
    how to reconstitute the inhibitor for in vivo studies?

    Answer: 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.

技術サポート&よくある質問(FAQ)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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