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.

Size Price Stock Quantity  
In DMSO USD 191 In stock
USD 77 In stock
USD 247 In stock
USD 587 In stock
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Cited by 48 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

Choose Selective JNK Inhibitors

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 NEL6TlFCdnSrYnHjeIVzcWGuIFHzd4F6 NWXZXYdxPzJiaB?= MkH0SG1UVw>? NVjsSXpvSW62aYDsZZNud2SrYXygZYN1cX[rdImge4l1cCCLQ{WwJI9nKDdwOUSzNlgh|ryP NEDEboUyQTd|NEmxNC=>
Plasmodium falciparum W2 M3S3UGFvfGmkYXP0[ZJq[WxiQYPzZZk> M{HiT|czKGh? NVO2OHN5TE2VTx?= MXLBcpRqeGyjc33v[IlidCCjY4Tpeol1gSC5aYToJGlEPTBib3[gO{46PDN{ODFOwG0> MnTONVk4OzR7MUC=
Plasmodium falciparum 7G8 M1nF[WFvfGmkYXP0[ZJq[WxiQYPzZZk> NH24To04OiCq MnjNSG1UVw>? M2fSSmFvfGmybHHzcY9lcWGuIHHjeIl3cXS7IIfpeIghUUN3MDDv[kAyOCEQvF2= NUfEN2NkOTl5M{S5NVA>
Plasmodium falciparum 3D7 M1H5eGFvfGmkYXP0[ZJq[WxiQYPzZZk> M4PQelczKGh? NXrmPJR7TE2VTx?= Mly5RY51cXCuYYPtc4Rq[WxiYXP0bZZqfHlid3n0bEBKSzVyIH;mJFEzNjV6OUOg{txO M3TMZ|E6PzN2OUGw
Plasmodium falciparum GB4 NHPi[lBCdnSrYnHjeIVzcWGuIFHzd4F6 M{XYcFczKGh? MVXEUXNQ MmPhRY51cXCuYYPtc4Rq[WxiYXP0bZZqfHlid3n0bEBKSzVyIH;mJFEzNjV6OUROwG0> NXPqXW5yOTl5M{S5NVA>
RAW264.7 MWrGeY5kfGmxbjDBd5NigQ>? MYixNEDPxE1? MYGxNkBp MXLBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgUm8heHKxZIXjeIlwdiC5aYToJGlEPTBib3[gNVfPxE1? NV;NdVI3OTl2OUe0NVg>
SH-SY5Y MX3GeY5kfGmxbjDBd5NigQ>? MWexNEDPxE1? NGnFXVYyKGh? MXnEUXNQ M2r5d25mfXKxcILveIVkfGm4ZTDhZ5Rqfmm2eTDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZiYX7pd49ugWOrbj3pcoR2[2WmIHPlcIwh\GWjdHi= MkPBNlM1QTh7MUS=
SH-SY5Y M1nje2tqdmG|ZTDBd5NigQ>? MV[xNEDPxE1? MmHMNUBp M3jINWROW09? NY\FR2tQUW6qaXLpeIlwdiCxZjDKUms{KGG|c3Xzd4VlKGG|IHLsc4Ns[WSnIH;mJIFvcXOxbYnjbY4ucW6mdXPl[EBkNWq3bjDwbI9{eGixconsZZRqd25iYYSgd4VzPzN? M4XyN|I{PDl6OUG0
RAW264.7 NUOweIdjTnWwY4Tpc44hSXO|YYm= M3;VUFExKM7:TR?= M2rzdVI1KGh? MV\BcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiSVytNYJmfGFicnXs[YF{\Q>? NXj0b|lCOjN5OUGwO|g>
RAW264.7 MmTRSpVv[3Srb36gRZN{[Xl? M1vZNFExKM7:TR?= NYex[Y9HOjRiaB?= Ml3xRY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFzQV{1qdmS3Y3XkJIlPV1NiZYjwdoV{e2mxbh?= NGr4VGozOzd7MUC3PC=>
RAW264.7 M1jXRWZ2dmO2aX;uJGF{e2G7 NUK4ZXdUOTBizszN MkPPNkBp NYDIN41RSW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKE6RIIDyc4R2[3Srb36= MWKyN|c6OTB5OB?=
B16-F10 MYfGeY5kfGmxbjDBd5NigQ>? Ml\ZNUBp NU\CUIt7UW6qaXLpeIlwdiCxZjDUUmYu[WyyaHGtbY5lfWOnZDDjMWpWViCyaH;zdIhwenmuYYTpc44> MlzKNlE5OTV4M{S=
PC12 NETKOHhHfW6ldHnvckBCe3OjeR?= Ml;FNVAh|ryP Mke1OUBp MnrKSG1UVw>? MY\BZ5RqfmG2aX;uJI9nKE6{ZkKvRXJGKGG|c3Xzd4VlKGG|IFjPMVEheHKxdHXpckBqdmS3Y4Tpc44heHKndILlZZRm\CC5aYToJHBFQThyNUm= MWGyNVM1PTZ6NR?=
PC12 M13ZdmZ2dmO2aX;uJGF{e2G7 M1nRSlExKM7:TR?= M1r3dVUhcA>? MnPLSG1UVw>? MV7BZ5RqfmG2aX;uJI9nKE6{ZkKvRXJGKGG|c3Xzd4VlKGG|IFjPMVEheHKxdHXpckBqdmS3Y4Tpc44heHKndILlZZRm\CC5aYToJHUxOTJ4 MoTkNlE{PDV4OEW=
PC12 MULGeY5kfGmxbjDBd5NigQ>? NHy1WJgyOCEQvF2= Ml;xOUBp MXrEUXNQ M4rST2FkfGm4YYTpc44hd2ZiToLmNk9CWkViYYPz[ZN{\WRiYYOgTG8uOSCycn;0[YlvKGmwZIXjeIlwdiCycnX0doVifGWmIIfpeIghW1B4MECxNlU> MXGyNVM1PTZ6NR?=
PC12 NUfneJVOTnWwY4Tpc44hSXO|YYm= MVWxNEDPxE1? NWmydoxyPSCq MWTEUXNQ NHnRVIhC[3SrdnH0bY9vKG:oIF7y[lIwSVKHIHHzd4V{e2WmIHHzJGhQNTFicILveIVqdiCrbnT1Z5Rqd25icILleJJm[XSnZDD3bZRpKFOEMkCzOVgx NWn1ZldpOjF|NEW2PFU>
A549 M3vGWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUCyNEDPxE1? NH;KUm04OiCq MXrEUXNQ NGPjWpRT[XCrZDDhcoQheG:2ZX70JIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:w NVTrUIVUOjN7MUK4OFA>
PC3 M3HYcmZ2dmO2aX;uJGF{e2G7 NEnF[IkzPSEQvF2= Mn:3NlQhcA>? MVLJcohq[mm2aX;uJI9nKEGSLUGgZY5lKHB{MTDseYNq\mW{YYPlJIFkfGm4aYT5JIlv\HWlZXSgZpkhWzF5OVSgVHJN MlLKNlMyPjJ4NUK=
THP-1 MmfFSpVv[3Srb36gRZN{[Xl? Mmi4PVAhdk1? Mn3KN|AhdWmw NWPKXJQxUW6qaXLpeIlwdiCxZjD0bZN{fWViZnHjeI9zKGW6cILld5Nqd25? NWntVXF7OjJ7NECwOVk>
LoVo MWHGeY5kfGmxbjDBd5NigQ>? MlW0NUDPxE1? MXuxJIg> NEHNelRKdmirYnn0bY9vKG:oIGDHSVIucW6mdXPl[EBmgHC{ZYPzbY9vKG:oIIXQRUBidmRiTV3QMVkhe2mpbnnmbYNidnSueR?= M3XafFIyQDV7NEe5
LoVo M37mZmZ2dmO2aX;uJGF{e2G7 MkXmNUDPxE1? MnvPNUBp NGm2XJZDdG:la4PQS2UzNWmwZIXj[YQh[2WubDDtbYdz[XSrb36gd4lodmmoaXPhcpRtgQ>? NYDuT3dSOjF6NUm0O|k>
A549 MXLGeY5kfGmxbjDBd5NigQ>? NE\yNGEzOCEQvF2= M4PFc|EhcA>? NUTEXFJrUW6qaXLpeIlwdiCxZjDUVGEucW6mdXPl[EBOVVBvMjDhcoQhfS2SQTDlfJBz\XO|aX;u MXSyNFQ6OjF5NR?=
HaCaT NXXMPFZNTnWwY4Tpc44hSXO|YYm= MXGyNEDPxE1? MYm0JIg> MV7EUXNQ NXTDZ3N4SmyxY3vzJJRp\SCWTl[t{tEucW6mdXPl[OKhS1mSNF[xNeKhfHKjboPjdolxfGmxbh?= NEDWV20yQThzMkO0PS=>
HaCaT MkXpSpVv[3Srb36gRZN{[Xl? NGPzfmwzOCEQvF2= MkjsNlQhcA>? NHT1TldFVVOR MUTCcI9kc3NidHjlJJBpd3OyaH;yfYxifGmxbjDv[kBkNUq3bjDwdo91\Wmw NXPGNJA1OTl6MUKzOFk>
PC3 MVjGeY5kfGmxbjDBd5NigQ>? MoXPNlAh|ryP M2ToR|EhcA>? MYLE[YNz\WG|ZYOgeIhmKE2PUEKgZY5lKE2PUEmg[ZhxemW|c3nvci=> NEP3WXMyQTZ|M{m3OS=>
BV-2 MWPGeY5kfGmxbjDBd5NigQ>? M1THN|Ih|ryP M4[4W|EhcA>? M2myUmlvcGmkaYTzJJRp\SCrbnPy[YF{\SCxZjDzRmFHTiC{ZXzlZZNmKGmwIFftbZgufHKnYYTl[EBDXi1{IHPlcIx{ MlXNNVk1ODZ6M{G=
Hep3B NHnXdFBHfW6ldHnvckBCe3OjeR?= MVGxNEDPxE1? MYCxJIg> M3ixdGJtd2OtczDheZRweGijZ4mgZY5lKHWycnXneYxifGmxbjDv[kBD\WOuaX6gNUBmgHC{ZYPzbY9vKGmwZIXj[YQh[nliY3XyZY1q\GV? NXjDflBWOTlyNkC5NlA>

... 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 Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
3mg/mL

* 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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Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID