SP600125

製品コード:S1460 別名:Nsc75890

For research use only.

SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.

SP600125化学構造

CAS No. 129-56-6

サイズ 価格(税別)
10mM (1mL in DMSO) JPY 16300
JPY 12000
JPY 23100

代表番号: 03-5615-9297|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(913)

製品安全説明書

JNK阻害剤の選択性比較

相関JNK製品

生物活性

製品説明 SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
ターゲット
serine/threonine kinase [1] JNK1 [1]
(Cell-free assay)
JNK2 [1]
(Cell-free assay)
Aurora A [4]
(Cell-free assay)
TrkA [4]
(Cell-free assay)
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40 nM 40 nM 60 nM 70 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Hep3B NXL4U2o1TnWwY4Tpc44hSXO|YYm= M3TpOVExKM7:TR?= NH;lV2UyKGh? Mn;4Roxw[2u|IHH1eI9xcGGpeTDhcoQhfXC{ZXf1cIF1cW:wIH;mJGJm[2yrbjCxJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSClZYLhcYll\Q>? MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTB4MEmyNEc,OTlyNkC5NlA9N2F-
BV-2 MYrGeY5kfGmxbjDBd5NigQ>? MWiyJO69VQ>? MnjJNUBp MWrJcohq[mm2czD0bIUhcW6lcnXhd4Uhd2Zic1LBSmYhemWuZXHz[UBqdiCJbXn4MZRz\WG2ZXSgRnYuOiClZXzsdy=> MlfrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl2ME[4N|EoRjF7NEC2PFMyRC:jPh?=
RAW264.7 M{PIbmZ2dmO2aX;uJGF{e2G7 NYnaXoRkOTBizszN NG[5PYgyOiCq MUfBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgUm8heHKxZIXjeIlwdiC5aYToJGlEPTBib3[gNVfPxE1? NFjKfow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUS5O|QyQCd-MUm0PVc1OTh:L3G+
PC3 M1nD[2Z2dmO2aX;uJGF{e2G7 NH36WmozOCEQvF2= NHLCe4oyKGh? MUHE[YNz\WG|ZYOgeIhmKE2PUEKgZY5lKE2PUEmg[ZhxemW|c3nvci=> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTZ|M{m3OUc,OTl4M{O5O|U9N2F-
Plasmodium falciparum HB3 MYDBcpRq[mGldHXybYFtKEG|c3H5 MVS3NkBp MX7EUXNQ Ml;NRY51cXCuYYPtc4Rq[WxiYXP0bZZqfHlid3n0bEBKSzVyIH;mJFcvQTR|Mkig{txO MkfGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5M{S5NVAoRjF7N{O0PVExRC:jPh?=
Plasmodium falciparum W2 MXjBcpRq[mGldHXybYFtKEG|c3H5 MXO3NkBp M4DoN2ROW09? MXnBcpRqeGyjc33v[IlidCCjY4Tpeol1gSC5aYToJGlEPTBib3[gO{46PDN{ODFOwG0> NWW3UHg{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3N|Q6OTBpPkG5O|M1QTFyPD;hQi=>
Plasmodium falciparum 7G8 M4PubmFvfGmkYXP0[ZJq[WxiQYPzZZk> Mmq4O|IhcA>? MkPaSG1UVw>? NWPxWHRFSW62aYDsZZNud2SrYXygZYN1cX[rdImge4l1cCCLQ{WwJI9nKDFyIN88US=> MlfpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5M{S5NVAoRjF7N{O0PVExRC:jPh?=
Plasmodium falciparum 3D7 MkXpRY51cWKjY4TldolidCCDc4PhfS=> MYe3NkBp MnS1SG1UVw>? MkDXRY51cXCuYYPtc4Rq[WxiYXP0bZZqfHlid3n0bEBKSzVyIH;mJFEzNjV6OUOg{txO NUnhPZlzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3N|Q6OTBpPkG5O|M1QTFyPD;hQi=>
Plasmodium falciparum GB4 NYrIdGVTSW62aXLhZ5RmemmjbDDBd5NigQ>? MUm3NkBp MnvnSG1UVw>? MYXBcpRqeGyjc33v[IlidCCjY4Tpeol1gSC5aYToJGlEPTBib3[gNVIvPTh7M988US=> MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTd|NEmxNEc,OTl5M{S5NVA9N2F-
HaCaT MYDGeY5kfGmxbjDBd5NigQ>? MVqyNEDPxE1? NVuwWpRUPCCq M3nKOWROW09? NUHZ[|lQSmyxY3vzJJRp\SCWTl[t{tEucW6mdXPl[OKhS1mSNF[xNeKhfHKjboPjdolxfGmxbh?= M4S5W|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEGyN|Q6Lz5zOUixNlM1QTxxYU6=
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A549 MkXqSpVv[3Srb36gRZN{[Xl? NHzYdGwzOCEQvF2= NGnoPIkyKGh? MmHFTY5pcWKrdHnvckBw\iCWUFGtbY5lfWOnZDDNUXAuOiCjbnSgeU1RSSCneIDy[ZN{cW:w NYTrSItFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC0PVIyPzVpPkKwOFkzOTd3PD;hQi=>
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PC12 NX\aXmpVTnWwY4Tpc44hSXO|YYm= NFvNW|IyOCEQvF2= MWe1JIg> MlGySG1UVw>? MUnBZ5RqfmG2aX;uJI9nKE6{ZkKvRXJGKGG|c3Xzd4VlKGG|IFjPMVEheHKxdHXpckBqdmS3Y4Tpc44heHKndILlZZRm\CC5aYToJHUxOTJ4 NIX0Znk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO0OVY5PSd-MkGzOFU3QDV:L3G+
PC12 MXTGeY5kfGmxbjDBd5NigQ>? NEfscIcyOCEQvF2= NWjmbY9lPSCq NUPDfGxWTE2VTx?= MVLBZ5RqfmG2aX;uJI9nKE6{ZkKvRXJGKGG|c3Xzd4VlKGG|IFjPMVEheHKxdHXpckBqdmS3Y4Tpc44heHKndILlZZRm\CC5aYToJHNRPjByMUK1 NWjobpluRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzOFU3QDVpPkKxN|Q2Pjh3PD;hQi=>
PC12 NUf5OplnTnWwY4Tpc44hSXO|YYm= MnLZNVAh|ryP NXLMXFA4PSCq NHL0dY1FVVOR MWfBZ5RqfmG2aX;uJI9nKE6{ZkKvRXJGKGG|c3Xzd4VlKGG|IFjPMVEheHKxdHXpckBqdmS3Y4Tpc44heHKndILlZZRm\CC5aYToJHNDOjB|NUiw NFT5[VI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO0OVY5PSd-MkGzOFU3QDV:L3G+
B16-F10 MUHGeY5kfGmxbjDBd5NigQ>? NEPY[5oyKGh? NIDYbmhKdmirYnn0bY9vKG:oIGTOSk1idHCqYT3pcoR2[2WmIHOtTnVPKHCqb4PwbI9zgWyjdHnvci=> NHn6V|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUixOVY{PCd-MkG4NVU3OzR:L3G+
LoVo MonaSpVv[3Srb36gRZN{[Xl? MX:xJO69VQ>? M4XV[FEhcA>? MknoTY5pcWKrdHnvckBw\iCSR1WyMYlv\HWlZXSg[ZhxemW|c3nvckBw\iC3UFGgZY5lKE2PUD25JJNq\26rZnnjZY51dHl? NIf5eVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUi1PVQ4QSd-MkG4OVk1Pzl:L3G+
LoVo NXTsUpdETnWwY4Tpc44hSXO|YYm= M1HnRlEh|ryP M{i0bVEhcA>? M{DkRWJtd2Otc2DHSVIucW6mdXPl[EBk\WyuIH3p[5JifGmxbjDzbYdvcW[rY3HueIx6 NHnI[4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUi1PVQ4QSd-MkG4OVk1Pzl:L3G+
THP-1 NHv6W5NHfW6ldHnvckBCe3OjeR?= MY[5NEBvVQ>? NIW1NHU{OCCvaX6= NFHle29KdmirYnn0bY9vKG:oIITpd5N2\SCoYXP0c5Ih\XiycnXzd4lwdg>? M1fXOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUSwNFU6Lz5{Mkm0NFA2QTxxYU6=
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SH-SY5Y NVrGb5ZxTnWwY4Tpc44hSXO|YYm= MkDDNVAh|ryP MX6xJIg> MXTEUXNQ NHvjO3dP\XW{b4Dyc5Rm[3SrdnWgZYN1cX[rdImgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIHHubZNwdXmlaX6tbY5lfWOnZDDj[YxtKGSnYYTo NFHRPZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S5PFkyPCd-MkO0PVg6OTR:L3G+
SH-SY5Y MUHLbY5ie2ViQYPzZZk> NYjuc4FuOTBizszN MlT0NUBp NVzMRnRKTE2VTx?= NYT6ZpNuUW6qaXLpeIlwdiCxZjDKUms{KGG|c3Xzd4VlKGG|IHLsc4Ns[WSnIH;mJIFvcXOxbYnjbY4ucW6mdXPl[EBkNWq3bjDwbI9{eGixconsZZRqd25iYYSgd4VzPzN? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR7OEmxOEc,OjN2OUi5NVQ9N2F-
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RAW264.7 M4\uU2FvfGmrbn\sZY1u[XSxcomgZZN{[Xl? NGHZWlJCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKG2xdYPlJHJCXzJ4ND63JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgUm8heHKxZIXjeIlwdiC{ZXzheIl3\SC2bzDjc451em:uLDDJR|UxKD1iMUeg{txONg>? NWnwb3BORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4N|E4QThpPkKyPFMyPzl6PD;hQi=>
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LAN-5 NXXW[FVNeUiWUzDhd5NigQ>? MXfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN? M2XFbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
アッセイ
Methods Test Index 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 27176481 22870247 21859840
Immunofluorescence AIF / Endo G ; E-cadherin / β-catenin ; α-catenin / Actin 21738692 21030692
Growth inhibition assay Cell viability (U-87 MG) ; Cell viability (A549) 27176481 24944614
体内試験

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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[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.

細胞試験:

[4]

  • 細胞株:HCT116, A2780, and U2OS cells
  • 濃度: 0–5 μM
  • 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.

動物試験:

[1]

  • 動物モデル:Mouse LPS/TNF model (female CD-1)
  • 投薬量:15 or 30 mg/kg
  • 投与方法:Administered via intravenous injection or orally

溶解度 (25°C)

体外

体内

左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
混合させたのち直ちに使用することを推奨します。

2mg/mL

化学情報

分子量 220.23
化学式

C14H8N2O

CAS No. 129-56-6
Storage 3年 -20°C
2年 -80°C in solvent
Smiles C1=CC=C2C(=C1)C3=NNC4=CC=CC(=C43)C2=O

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

便利ツール

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

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よくある質問(FAQ)

質問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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