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 47 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 MVzBcpRq[mGldHXybYFtKEG|c3H5 MkXxO|IhcA>? M4\YfWROW09? NG\ZN5NCdnSrcHzhd41w\GmjbDDhZ5Rqfmm2eTD3bZRpKEmFNUCgc4YhPy57NEOyPEDPxE1? NE\oTnQyQTd|NEmxNC=>
Plasmodium falciparum W2 M1HNdmFvfGmkYXP0[ZJq[WxiQYPzZZk> NW\YU25pPzJiaB?= MnHtSG1UVw>? M1TFSWFvfGmybHHzcY9lcWGuIHHjeIl3cXS7IIfpeIghUUN3MDDv[kA4Njl2M{K4JO69VQ>? MX6xPVc{PDlzMB?=
Plasmodium falciparum 7G8 NF7kbVRCdnSrYnHjeIVzcWGuIFHzd4F6 MlXMO|IhcA>? MYrEUXNQ Ml\nRY51cXCuYYPtc4Rq[WxiYXP0bZZqfHlid3n0bEBKSzVyIH;mJFExKM7:TR?= NYP5WGkxOTl5M{S5NVA>
Plasmodium falciparum 3D7 NWfNeGJtSW62aXLhZ5RmemmjbDDBd5NigQ>? NFvJbVI4OiCq NYTVenRkTE2VTx?= MYnBcpRqeGyjc33v[IlidCCjY4Tpeol1gSC5aYToJGlEPTBib3[gNVIvPTh7MzFOwG0> NETMO|YyQTd|NEmxNC=>
Plasmodium falciparum GB4 NVzncmFQSW62aXLhZ5RmemmjbDDBd5NigQ>? NXPGNmV6PzJiaB?= MlXlSG1UVw>? M17jcWFvfGmybHHzcY9lcWGuIHHjeIl3cXS7IIfpeIghUUN3MDDv[kAyOi53OEmz{txO MnjqNVk4OzR7MUC=
RAW264.7 M3vI[2Z2dmO2aX;uJGF{e2G7 NF3u[4YyOCEQvF2= NVPjU5E2OTJiaB?= MYPBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgUm8heHKxZIXjeIlwdiC5aYToJGlEPTBib3[gNVfPxE1? MkjLNVk1QTd2MUi=
SH-SY5Y NISxfGtHfW6ldHnvckBCe3OjeR?= MkT6NVAh|ryP M1riS|EhcA>? NV\QbIgzTE2VTx?= NELNUVJP\XW{b4Dyc5Rm[3SrdnWgZYN1cX[rdImgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIHHubZNwdXmlaX6tbY5lfWOnZDDj[YxtKGSnYYTo Ml;DNlM1QTh7MUS=
SH-SY5Y NWfieXk3U2mwYYPlJGF{e2G7 M1LDUlExKM7:TR?= MWixJIg> M1vTZmROW09? MmTLTY5pcWKrdHnvckBw\iCMTluzJIF{e2W|c3XkJIF{KGKub3PrZYRmKG:oIHHubZNwdXmlaX6tbY5lfWOnZDDjMYp2diCyaH;zdIhwenmuYYTpc44h[XRic3XyO|M> NH[w[IYzOzR7OEmxOC=>
RAW264.7 MWXGeY5kfGmxbjDBd5NigQ>? MortNVAh|ryP NVjQbXhJOjRiaB?= NYnBOHV[SW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGlNNTGkZYThJJJmdGWjc3W= NGfsOIQzOzd7MUC3PC=>
RAW264.7 MojmSpVv[3Srb36gRZN{[Xl? MV6xNEDPxE1? MWSyOEBp Ml63RY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFzQV{1qdmS3Y3XkJIlPV1NiZYjwdoV{e2mxbh?= NGXjdJQzOzd7MUC3PC=>
RAW264.7 NWPUUWU6TnWwY4Tpc44hSXO|YYm= NWjGZ4c{OTBizszN NU\SUFVoOiCq NV\QRlVkSW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKE6RIIDyc4R2[3Srb36= NFPONVkzOzd7MUC3PC=>
B16-F10 M2T0WWZ2dmO2aX;uJGF{e2G7 NX\wdpZ1OSCq MkjQTY5pcWKrdHnvckBw\iCWTl[tZYxxcGFvaX7keYNm\CClLVrVUkBxcG:|cHjvdplt[XSrb36= NVfueXA5OjF6MUW2N|Q>
PC12 MkTzSpVv[3Srb36gRZN{[Xl? NXr0WXlMOTBizszN NYqxdlRZPSCq NFzneI9FVVOR MX\BZ5RqfmG2aX;uJI9nKE6{ZkKvRXJGKGG|c3Xzd4VlKGG|IFjPMVEheHKxdHXpckBqdmS3Y4Tpc44heHKndILlZZRm\CC5aYToJHBFQThyNUm= MnvMNlE{PDV4OEW=
PC12 NU\sb2NQTnWwY4Tpc44hSXO|YYm= MV6xNEDPxE1? NVv4WZRuPSCq NEDKOWNFVVOR MmT6RYN1cX[jdHnvckBw\iCQcn[yM2FTTSCjc4Pld5Nm\CCjczDIU{0yKHC{b4TlbY4hcW6mdXP0bY9vKHC{ZYTy[YF1\WRid3n0bEBWODF{Nh?= M4TWNVIyOzR3Nki1
PC12 MlHZSpVv[3Srb36gRZN{[Xl? M1uyelExKM7:TR?= M3\wSlUhcA>? M2ixbWROW09? NH7ZVZFC[3SrdnH0bY9vKG:oIF7y[lIwSVKHIHHzd4V{e2WmIHHzJGhQNTFicILveIVqdiCrbnT1Z5Rqd25icILleJJm[XSnZDD3bZRpKFOSNkCwNVI2 M13tXVIyOzR3Nki1
PC12 M4TtbmZ2dmO2aX;uJGF{e2G7 MVKxNEDPxE1? MkfoOUBp NYLVb246TE2VTx?= MYPBZ5RqfmG2aX;uJI9nKE6{ZkKvRXJGKGG|c3Xzd4VlKGG|IFjPMVEheHKxdHXpckBqdmS3Y4Tpc44heHKndILlZZRm\CC5aYToJHNDOjB|NUiw MkOwNlE{PDV4OEW=
A549 MnvKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHtZoMzOCEQvF2= NYTxVYd1PzJiaB?= Mme0SG1UVw>? NWrPfHU2WmGyaXSgZY5lKHCxdHXueEBqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbh?= NWnVW3V4OjN7MUK4OFA>
PC3 NGTSTlhHfW6ldHnvckBCe3OjeR?= M3XlS|I2KM7:TR?= Ml6xNlQhcA>? NG\CbnpKdmirYnn0bY9vKG:oIFHQMVEh[W6mIICyNUBtfWOrZnXyZZNmKGGldHn2bZR6KGmwZIXj[YQh[nliU{G3PWQhWFKO NGf0VoozOzF4Mk[1Ni=>
THP-1 NWL0W|JyTnWwY4Tpc44hSXO|YYm= NV3SeYRHQTBibl2= MWqzNEBucW5? MYTJcohq[mm2aX;uJI9nKHSrc4P1[UBn[WO2b4Kg[ZhxemW|c3nvci=> NXTvZlBmOjJ7NECwOVk>
LoVo NWD5PGdyTnWwY4Tpc44hSXO|YYm= MVSxJO69VQ>? NWHCfIZtOSCq NGL4TXlKdmirYnn0bY9vKG:oIGDHSVIucW6mdXPl[EBmgHC{ZYPzbY9vKG:oIIXQRUBidmRiTV3QMVkhe2mpbnnmbYNidnSueR?= MkjJNlE5PTl2N{m=
LoVo NFH6NmFHfW6ldHnvckBCe3OjeR?= MXGxJO69VQ>? M2XJR|EhcA>? NGfyO5NDdG:la4PQS2UzNWmwZIXj[YQh[2WubDDtbYdz[XSrb36gd4lodmmoaXPhcpRtgQ>? M2TKZ|IyQDV7NEe5
A549 MUPGeY5kfGmxbjDBd5NigQ>? NGHzTHUzOCEQvF2= NYLOT3pxOSCq NHXhZW5KdmirYnn0bY9vKG:oIGTQRU1qdmS3Y3XkJG1OWC1{IHHu[EB2NVCDIHX4dJJme3Orb36= MkfzNlA1QTJzN{W=
HaCaT MnvvSpVv[3Srb36gRZN{[Xl? MVKyNEDPxE1? NYjocpNyPCCq NUPEdI14TE2VTx?= NYe0WGJlSmyxY3vzJJRp\SCWTl[t{tEucW6mdXPl[OKhS1mSNF[xNeKhfHKjboPjdolxfGmxbh?= MoTYNVk5OTJ|NEm=
HaCaT NHfZUWtHfW6ldHnvckBCe3OjeR?= NETacnIzOCEQvF2= MojHNlQhcA>? MWfEUXNQ NGnRTlVDdG:la4OgeIhmKHCqb4PwbI9zgWyjdHnvckBw\iClLVr1ckBxem:2ZXnu MnTXNVk5OTJ|NEm=
PC3 M4jRV2Z2dmO2aX;uJGF{e2G7 NX21b|BnOjBizszN NH\zUYIyKGh? NUKyUnE3TGWlcnXhd4V{KHSqZTDNUXAzKGGwZDDNUXA6KGW6cILld5Nqd25? Ml;LNVk3OzN7N{W=
BV-2 NYHXZXhOTnWwY4Tpc44hSXO|YYm= MUiyJO69VQ>? M3zL[|EhcA>? M4qxSWlvcGmkaYTzJJRp\SCrbnPy[YF{\SCxZjDzRmFHTiC{ZXzlZZNmKGmwIFftbZgufHKnYYTl[EBDXi1{IHPlcIx{ MkHpNVk1ODZ6M{G=
Hep3B NHvhNnRHfW6ldHnvckBCe3OjeR?= NEnUTFgyOCEQvF2= M4rRUVEhcA>? MVrCcI9kc3NiYYX0c5Bp[We7IHHu[EB2eHKnZ4XsZZRqd25ib3[gRoVkdGmwIEGg[ZhxemW|c3nvckBqdmS3Y3XkJIJ6KGOncnHtbYRm NGL0dWoyQTB4MEmyNC=>

... 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:
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
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

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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