SP600125

製品コードS1460 別名:Nsc75890

SP600125化学構造

分子量(MW):220.23

SP600125は一種の広範囲に使用されるJNK阻害剤で、無細胞試験でJNK1、JNK2とJNK3に作用する時のIC50値が40 nM、40 nMと90 nMにそれぞれ分かれることですが、JNKに作用する選択性はMKK4に作用する選択性より10倍が高くなって、MKK3、MKK6、PKBとPKCαに作用する選択性より25倍が高くなって、ERK2、p38、Chk1とEGFR等に作用する選択性より100倍が高くなります。

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文献中の引用(46)

カスタマーフィードバック(4)

  • 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.

    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.

    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.

製品安全説明書

JNK阻害剤の選択性比較

生物活性

製品説明 SP600125は一種の広範囲に使用されるJNK阻害剤で、無細胞試験でJNK1、JNK2とJNK3に作用する時のIC50値が40 nM、40 nMと90 nMにそれぞれ分かれることですが、JNKに作用する選択性はMKK4に作用する選択性より10倍が高くなって、MKK3、MKK6、PKBとPKCαに作用する選択性より25倍が高くなって、ERK2、p38、Chk1とEGFR等に作用する選択性より100倍が高くなります。
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
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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Plasmodium falciparum HB3 NHLUenhCdnSrYnHjeIVzcWGuIFHzd4F6 NFv0[mo4OiCq M{jSeGROW09? NIfrOmxCdnSrcHzhd41w\GmjbDDhZ5Rqfmm2eTD3bZRpKEmFNUCgc4YhPy57NEOyPEDPxE1? MkPPNVk4OzR7MUC=
Plasmodium falciparum W2 NW\3PWdXSW62aXLhZ5RmemmjbDDBd5NigQ>? NVv6PI1PPzJiaB?= Mmj3SG1UVw>? MnnIRY51cXCuYYPtc4Rq[WxiYXP0bZZqfHlid3n0bEBKSzVyIH;mJFcvQTR|Mkig{txO MkjiNVk4OzR7MUC=
Plasmodium falciparum 7G8 NUnwVo05SW62aXLhZ5RmemmjbDDBd5NigQ>? MYC3NkBp Mmr6SG1UVw>? M1rkW2FvfGmybHHzcY9lcWGuIHHjeIl3cXS7IIfpeIghUUN3MDDv[kAyOCEQvF2= MW[xPVc{PDlzMB?=
Plasmodium falciparum 3D7 MXnBcpRq[mGldHXybYFtKEG|c3H5 NIDBWVc4OiCq NGfiO5VFVVOR NFrTOHBCdnSrcHzhd41w\GmjbDDhZ5Rqfmm2eTD3bZRpKEmFNUCgc4YhOTJwNUi5N{DPxE1? NHP1ZmMyQTd|NEmxNC=>
Plasmodium falciparum GB4 M3\RSWFvfGmkYXP0[ZJq[WxiQYPzZZk> NFzzUmI4OiCq NGO2NYFFVVOR M1PJcGFvfGmybHHzcY9lcWGuIHHjeIl3cXS7IIfpeIghUUN3MDDv[kAyOi53OEmz{txO MV:xPVc{PDlzMB?=
RAW264.7 M17oVWZ2dmO2aX;uJGF{e2G7 NGq1d48yOCEQvF2= MV[xNkBp NVvCWVBPSW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKE6RIIDyc4R2[3Srb36ge4l1cCCLQ{WwJI9nKDF5zszN MX2xPVQ6PzRzOB?=
SH-SY5Y NFLT[opHfW6ldHnvckBCe3OjeR?= MWOxNEDPxE1? Mn;YNUBp MonvSG1UVw>? NXL3fVdCVmW3cn;wdo91\WO2aY\lJIFkfGm4aYT5JIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCxZjDhcol{d227Y3nuMYlv\HWlZXSgZ4VtdCCmZXH0bC=> Ml3vNlM1QTh7MUS=
SH-SY5Y MV\LbY5ie2ViQYPzZZk> NGrWVYMyOCEQvF2= M{KzTVEhcA>? M4\ycmROW09? Mn;6TY5pcWKrdHnvckBw\iCMTluzJIF{e2W|c3XkJIF{KGKub3PrZYRmKG:oIHHubZNwdXmlaX6tbY5lfWOnZDDjMYp2diCyaH;zdIhwenmuYYTpc44h[XRic3XyO|M> NXvoe41bOjN2OUi5NVQ>
RAW264.7 M1rP[mZ2dmO2aX;uJGF{e2G7 NELMb5QyOCEQvF2= NVXaU2V6OjRiaB?= NIHzeZRCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWwuOWKndHGgdoVt\WG|ZR?= NWmxNVl3OjN5OUGwO|g>
RAW264.7 M4PpXWZ2dmO2aX;uJGF{e2G7 M2jTfFExKM7:TR?= M3jR[lI1KGh? M1HzfWFvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDMVHMucW6mdXPl[EBqVk:VIHX4dJJme3Orb36= NVz0WppzOjN5OUGwO|g>
RAW264.7 NGfHVnFHfW6ldHnvckBCe3OjeR?= Ml;sNVAh|ryP NU\NXHJzOiCq NIq5TFNCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gUHBUNWmwZIXj[YQhVk9icILv[JVkfGmxbh?= NFL2OoQzOzd7MUC3PC=>
B16-F10 NFexRVZHfW6ldHnvckBCe3OjeR?= M17tb|EhcA>? M2C1fGlvcGmkaYTpc44hd2ZiVF7GMYFteGijLXnu[JVk\WRiYz3KWW4heGixc4Doc5J6dGG2aX;u NXnmUVUzOjF6MUW2N|Q>
PC12 M3m5N2Z2dmO2aX;uJGF{e2G7 Mn\INVAh|ryP M2frUVUhcA>? M3r5cGROW09? M{nBdGFkfGm4YYTpc44hd2ZiToLmNk9CWkViYYPz[ZN{\WRiYYOgTG8uOSCycn;0[YlvKGmwZIXjeIlwdiCycnX0doVifGWmIIfpeIghWER7OEC1PS=> MXSyNVM1PTZ6NR?=
PC12 MlX6SpVv[3Srb36gRZN{[Xl? MVuxNEDPxE1? NVXEeIRSPSCq M2XqW2ROW09? M4C4bWFkfGm4YYTpc44hd2ZiToLmNk9CWkViYYPz[ZN{\WRiYYOgTG8uOSCycn;0[YlvKGmwZIXjeIlwdiCycnX0doVifGWmIIfpeIghXTBzMk[= NEP2dpgzOTN2NU[4OS=>
PC12 M3ztemZ2dmO2aX;uJGF{e2G7 Ml7QNVAh|ryP MX:1JIg> NG\a[JBFVVOR MVTBZ5RqfmG2aX;uJI9nKE6{ZkKvRXJGKGG|c3Xzd4VlKGG|IFjPMVEheHKxdHXpckBqdmS3Y4Tpc44heHKndILlZZRm\CC5aYToJHNRPjByMUK1 MYKyNVM1PTZ6NR?=
PC12 MUnGeY5kfGmxbjDBd5NigQ>? MljvNVAh|ryP MVi1JIg> NIK2V4pFVVOR NWfET2VrSWO2aY\heIlwdiCxZjDOdoYzN0GURTDhd5Nme3OnZDDhd{BJVy1zIIDyc5RmcW5iaX7keYN1cW:wIIDy[ZRz\WG2ZXSge4l1cCCVQkKwN|U5OA>? MUKyNVM1PTZ6NR?=
A549 NUHpVYtoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI[3dlIzOCEQvF2= NYH1NmNxPzJiaB?= NFy1V5NFVVOR MkK3VoFxcWRiYX7kJJBwfGWwdDDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdg>? NFfD[Y8zOzlzMki0NC=>
PC3 NGPxW2FHfW6ldHnvckBCe3OjeR?= NFrubmIzPSEQvF2= MYKyOEBp M3XqWWlvcGmkaYTpc44hd2ZiQWCtNUBidmRicEKxJIx2[2moZYLhd4Uh[WO2aY\peJkhcW6mdXPl[EBjgSCVMUe5SEBRWkx? NF7pRXQzOzF4Mk[1Ni=>
THP-1 NXL1TWRITnWwY4Tpc44hSXO|YYm= MUm5NEBvVQ>? M{\DUVMxKG2rbh?= NFjLc|VKdmirYnn0bY9vKG:oIITpd5N2\SCoYXP0c5Ih\XiycnXzd4lwdg>? MXGyNlk1ODB3OR?=
LoVo Ml7jSpVv[3Srb36gRZN{[Xl? MYCxJO69VQ>? MYWxJIg> MYLJcohq[mm2aX;uJI9nKFCJRUKtbY5lfWOnZDDlfJBz\XO|aX;uJI9nKHWSQTDhcoQhVU2SLUmgd4lodmmoaXPhcpRtgQ>? MWeyNVg2QTR5OR?=
LoVo NX7tN25{TnWwY4Tpc44hSXO|YYm= NEjDd4gyKM7:TR?= NV;UTmdvOSCq MmTjRoxw[2u|UFfFNk1qdmS3Y3XkJINmdGxibXnndoF1cW:wIIPp[45q\mmlYX70cJk> NWjjeJhMOjF6NUm0O|k>
A549 NVH3c4ROTnWwY4Tpc44hSXO|YYm= NF[5flYzOCEQvF2= NF\YcGgyKGh? M{m3bmlvcGmkaYTpc44hd2ZiVGDBMYlv\HWlZXSgUW1RNTJiYX7kJJUuWEFiZYjwdoV{e2mxbh?= NGnIeHYzODR7MkG3OS=>
HaCaT MnHySpVv[3Srb36gRZN{[Xl? NF;xd4wzOCEQvF2= Ml;5OEBp M1fLTmROW09? NWflS4R[SmyxY3vzJJRp\SCWTl[t{tEucW6mdXPl[OKhS1mSNF[xNeKhfHKjboPjdolxfGmxbh?= NX3RNlBWOTl6MUKzOFk>
HaCaT MYjGeY5kfGmxbjDBd5NigQ>? NF:xOGMzOCEQvF2= NGPDfGgzPCCq M{DkRmROW09? MWjCcI9kc3NidHjlJJBpd3OyaH;yfYxifGmxbjDv[kBkNUq3bjDwdo91\Wmw NULpXItVOTl6MUKzOFk>
PC3 Mmr1SpVv[3Srb36gRZN{[Xl? NF;URYozOCEQvF2= NVO0RpQ1OSCq M2DyUGRm[3KnYYPld{B1cGViTV3QNkBidmRiTV3QPUBmgHC{ZYPzbY9v MnjZNVk3OzN7N{W=
BV-2 MoTrSpVv[3Srb36gRZN{[Xl? NIH1ZWozKM7:TR?= M1XXRVEhcA>? Ml\OTY5pcWKrdIOgeIhmKGmwY4LlZZNmKG:oIIPCRWZHKHKnbHXhd4UhcW5iR33pfE11emWjdHXkJGJXNTJiY3XscJM> NEi1fYoyQTRyNkizNS=>
Hep3B MnfpSpVv[3Srb36gRZN{[Xl? MVqxNEDPxE1? NIH1bpkyKGh? M3THWWJtd2OtczDheZRweGijZ4mgZY5lKHWycnXneYxifGmxbjDv[kBD\WOuaX6gNUBmgHC{ZYPzbY9vKGmwZIXj[YQh[nliY3XyZY1q\GV? M3Hs[lE6ODZyOUKw

... 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]

プロトコル(参考用のみ)

キナーゼアッセイ:[4]
+ 展開

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]
+ 展開
  • 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.
    (参考用のみ)
動物実験:[1]
+ 展開
  • 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
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 44 mg/mL (199.79 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
体内 5% DMSO+corn oil 5mg/mL

* <1 mg/mlは製品が微弱に溶解する或いは溶解しないことを示します。
* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 220.23
化学式

C14H8N2O

CAS No. 129-56-6
保管
in solvent
別名 Nsc75890

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 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.

JNK信号経路図

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID