SP600125

Catalog No.S1460 Synonyms: Nsc75890

SP600125 Chemical Structure

Molecular Weight(MW): 220.23

SP600125 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.

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In DMSO USD 191 In stock
USD 77 In stock
USD 247 In stock
USD 587 In stock

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Cited by 46 Publications

4 Customer Reviews

  • 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.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description SP600125 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.
Targets
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

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 MWXBcpRq[mGldHXybYFtKEG|c3H5 NHXJb5I4OiCq MnjVSG1UVw>? NWHmd|FpSW62aYDsZZNud2SrYXygZYN1cX[rdImge4l1cCCLQ{WwJI9nKDdwOUSzNlgh|ryP MnzENVk4OzR7MUC=
Plasmodium falciparum W2 NVLCVmM1SW62aXLhZ5RmemmjbDDBd5NigQ>? NELiPZQ4OiCq MnrPSG1UVw>? M4PDe2FvfGmybHHzcY9lcWGuIHHjeIl3cXS7IIfpeIghUUN3MDDv[kA4Njl2M{K4JO69VQ>? MVuxPVc{PDlzMB?=
Plasmodium falciparum 7G8 M1Pu[mFvfGmkYXP0[ZJq[WxiQYPzZZk> MlHYO|IhcA>? NWHYVFBPTE2VTx?= M3vLe2FvfGmybHHzcY9lcWGuIHHjeIl3cXS7IIfpeIghUUN3MDDv[kAyOCEQvF2= MnrlNVk4OzR7MUC=
Plasmodium falciparum 3D7 NIX2WpNCdnSrYnHjeIVzcWGuIFHzd4F6 M{TFcVczKGh? NYLzWmtFTE2VTx?= MofiRY51cXCuYYPtc4Rq[WxiYXP0bZZqfHlid3n0bEBKSzVyIH;mJFEzNjV6OUOg{txO M1n5XlE6PzN2OUGw
Plasmodium falciparum GB4 NIHieGlCdnSrYnHjeIVzcWGuIFHzd4F6 NF7r[o04OiCq MXvEUXNQ NGjE[YdCdnSrcHzhd41w\GmjbDDhZ5Rqfmm2eTD3bZRpKEmFNUCgc4YhOTJwNUi5N:69VQ>? M{TadlE6PzN2OUGw
RAW264.7 NH\PdFBHfW6ldHnvckBCe3OjeR?= MX:xNEDPxE1? M3joUlEzKGh? NXX4enR7SW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKE6RIIDyc4R2[3Srb36ge4l1cCCLQ{WwJI9nKDF5zszN MlnuNVk1QTd2MUi=
SH-SY5Y MWfGeY5kfGmxbjDBd5NigQ>? NYLNW3VLOTBizszN MnPXNUBp NUP0Olg1TE2VTx?= M1z1WW5mfXKxcILveIVkfGm4ZTDhZ5Rqfmm2eTDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZiYX7pd49ugWOrbj3pcoR2[2WmIHPlcIwh\GWjdHi= M2H6OVI{PDl6OUG0
SH-SY5Y MmroT4lv[XOnIFHzd4F6 NWjaT2RiOTBizszN MlK5NUBp NH;NS2xFVVOR NWLMdWRiUW6qaXLpeIlwdiCxZjDKUms{KGG|c3Xzd4VlKGG|IHLsc4Ns[WSnIH;mJIFvcXOxbYnjbY4ucW6mdXPl[EBkNWq3bjDwbI9{eGixconsZZRqd25iYYSgd4VzPzN? M13vSlI{PDl6OUG0
RAW264.7 MkjJSpVv[3Srb36gRZN{[Xl? NV\ldFFzOTBizszN MoTFNlQhcA>? NGfFfJpCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWwuOWKndHGgdoVt\WG|ZR?= M1j1VVI{PzlzMEe4
RAW264.7 NIOwdHFHfW6ldHnvckBCe3OjeR?= MWqxNEDPxE1? NULZT4hLOjRiaB?= NH\oW2pCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gUHBUNWmwZIXj[YQhcU6RUzDlfJBz\XO|aX;u MUCyN|c6OTB5OB?=
RAW264.7 M{\OSGZ2dmO2aX;uJGF{e2G7 NX6zW|JNOTBizszN NFr4XGczKGh? M3nY[2FvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDMVHMucW6mdXPl[EBPVyCycn;keYN1cW:w NVjlSpUxOjN5OUGwO|g>
B16-F10 MlrLSpVv[3Srb36gRZN{[Xl? MmjqNUBp M{LETWlvcGmkaYTpc44hd2ZiVF7GMYFteGijLXnu[JVk\WRiYz3KWW4heGixc4Doc5J6dGG2aX;u Mn\INlE5OTV4M{S=
PC12 Ml3USpVv[3Srb36gRZN{[Xl? M3LENFExKM7:TR?= MVy1JIg> NXrjSo5GTE2VTx?= NIPEdVZC[3SrdnH0bY9vKG:oIF7y[lIwSVKHIHHzd4V{e2WmIHHzJGhQNTFicILveIVqdiCrbnT1Z5Rqd25icILleJJm[XSnZDD3bZRpKFCGOUiwOVk> M2[zWlIyOzR3Nki1
PC12 MlfpSpVv[3Srb36gRZN{[Xl? M2TZPFExKM7:TR?= NYT0UIFYPSCq Mo\2SG1UVw>? NFToflJC[3SrdnH0bY9vKG:oIF7y[lIwSVKHIHHzd4V{e2WmIHHzJGhQNTFicILveIVqdiCrbnT1Z5Rqd25icILleJJm[XSnZDD3bZRpKFVyMUK2 MYiyNVM1PTZ6NR?=
PC12 M33NXmZ2dmO2aX;uJGF{e2G7 NW\ofphmOTBizszN MnjyOUBp Mni3SG1UVw>? NEXkbGhC[3SrdnH0bY9vKG:oIF7y[lIwSVKHIHHzd4V{e2WmIHHzJGhQNTFicILveIVqdiCrbnT1Z5Rqd25icILleJJm[XSnZDD3bZRpKFOSNkCwNVI2 Mm\kNlE{PDV4OEW=
PC12 MonxSpVv[3Srb36gRZN{[Xl? NILkXoQyOCEQvF2= NXzrUJVvPSCq NH3BXnpFVVOR M2PHW2FkfGm4YYTpc44hd2ZiToLmNk9CWkViYYPz[ZN{\WRiYYOgTG8uOSCycn;0[YlvKGmwZIXjeIlwdiCycnX0doVifGWmIIfpeIghW0J{MEO1PFA> NUn6[JJ1OjF|NEW2PFU>
A549 NVXJWHpIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTpNlAh|ryP NEjWdZI4OiCq MWfEUXNQ M1H4c3JieGmmIHHu[EBxd3SnboSgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25? MW[yN|kyOjh2MB?=
PC3 M4nKS2Z2dmO2aX;uJGF{e2G7 MmTUNlUh|ryP Mm\TNlQhcA>? NYDscmhZUW6qaXLpeIlwdiCxZjDBVE0yKGGwZDDwNlEhdHWlaX\ldoF{\SCjY4Tpeol1gSCrbnT1Z4VlKGK7IGOxO|lFKFCUTB?= Ml\6NlMyPjJ4NUK=
THP-1 NWT0NZRRTnWwY4Tpc44hSXO|YYm= MX65NEBvVQ>? M1T6RVMxKG2rbh?= MUPJcohq[mm2aX;uJI9nKHSrc4P1[UBn[WO2b4Kg[ZhxemW|c3nvci=> NV\ZfFVFOjJ7NECwOVk>
LoVo M1rBS2Z2dmO2aX;uJGF{e2G7 M1XEOFEh|ryP MkPmNUBp NWjQZVB7UW6qaXLpeIlwdiCxZjDQS2UzNWmwZIXj[YQh\XiycnXzd4lwdiCxZjD1VGEh[W6mIF3NVE06KHOrZ37p[olk[W62bIm= NXrjSZdDOjF6NUm0O|k>
LoVo M12wc2Z2dmO2aX;uJGF{e2G7 M2mzfVEh|ryP MXGxJIg> M170PGJtd2Otc2DHSVIucW6mdXPl[EBk\WyuIH3p[5JifGmxbjDzbYdvcW[rY3HueIx6 MYiyNVg2QTR5OR?=
A549 NWm4eJRMTnWwY4Tpc44hSXO|YYm= MVGyNEDPxE1? NITaeJUyKGh? M4\zWWlvcGmkaYTpc44hd2ZiVGDBMYlv\HWlZXSgUW1RNTJiYX7kJJUuWEFiZYjwdoV{e2mxbh?= NH7lO3AzODR7MkG3OS=>
HaCaT MUHGeY5kfGmxbjDBd5NigQ>? MnPwNlAh|ryP MV:0JIg> MX;EUXNQ NUL5SWFYSmyxY3vzJJRp\SCWTl[t{tEucW6mdXPl[OKhS1mSNF[xNeKhfHKjboPjdolxfGmxbh?= MlTLNVk5OTJ|NEm=
HaCaT MVPGeY5kfGmxbjDBd5NigQ>? M4TvTlIxKM7:TR?= NFfOSnMzPCCq MYjEUXNQ NHXOVnpDdG:la4OgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iClLVr1ckBxem:2ZXnu NImwWo4yQThzMkO0PS=>
PC3 NG\iRmNHfW6ldHnvckBCe3OjeR?= NVG4[JVZOjBizszN NFnhW24yKGh? MkXWSIVkemWjc3XzJJRp\SCPTWCyJIFv\CCPTWC5JIV5eHKnc4Ppc44> NXnXV2FGOTl4M{O5O|U>
BV-2 NGH4b4NHfW6ldHnvckBCe3OjeR?= NIPVbmgzKM7:TR?= NWjY[m1mOSCq NW\aN3J[UW6qaXLpeJMhfGinIHnuZ5Jm[XOnIH;mJJNDSU[IIILlcIVie2ViaX6gS41qgC22cnXheIVlKEKYLUKgZ4VtdHN? M{mzTVE6PDB4OEOx
Hep3B Ml\sSpVv[3Srb36gRZN{[Xl? NH[x[o0yOCEQvF2= NEnieGkyKGh? NUTpW|B[SmyxY3vzJIF2fG:yaHHnfUBidmRidYDy[Yd2dGG2aX;uJI9nKEKnY3zpckAyKGW6cILld5Nqd25iaX7keYNm\CCkeTDj[ZJidWmmZR?= MWexPVA3ODl{MB?=

... Click to View More Cell Line Experimental Data

In vivo 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]

Protocol

Kinase Assay:[4]
+ Expand

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.
Cell Research:[4]
+ Expand
  • Cell lines: HCT116, A2780, and U2OS cells
  • Concentrations: 0–5 μM, dissolved in 0.1% DMSO
  • Incubation Time: 72 hours
  • Method: 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Mouse LPS/TNF model (female CD-1)
  • Formulation: Dissolved in PPCES (30% PEG-400/20% polypropylene glycol/15% Cremophor EL/5% ethanol/30% saline)
  • Dosages: 15 or 30 mg/kg
  • Administration: Administered via intravenous injection or orally
    (Only for Reference)

Solubility (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.

Chemical Information

Molecular Weight 220.23
Formula

C14H8N2O

CAS No. 129-56-6
Storage powder
in solvent
Synonyms Nsc75890

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID