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 NXuzSG92SW62aXLhZ5RmemmjbDDBd5NigQ>? NXfZUYplPzJiaB?= MWLEUXNQ NYrDe3JKSW62aYDsZZNud2SrYXygZYN1cX[rdImge4l1cCCLQ{WwJI9nKDdwOUSzNlgh|ryP MWWxPVc{PDlzMB?=
Plasmodium falciparum W2 Mk\hRY51cWKjY4TldolidCCDc4PhfS=> NHqweoo4OiCq M1K2e2ROW09? NG[2PIVCdnSrcHzhd41w\GmjbDDhZ5Rqfmm2eTD3bZRpKEmFNUCgc4YhPy57NEOyPEDPxE1? MmCzNVk4OzR7MUC=
Plasmodium falciparum 7G8 MlXQRY51cWKjY4TldolidCCDc4PhfS=> MnrKO|IhcA>? NYGzSnE2TE2VTx?= M{TvemFvfGmybHHzcY9lcWGuIHHjeIl3cXS7IIfpeIghUUN3MDDv[kAyOCEQvF2= MX[xPVc{PDlzMB?=
Plasmodium falciparum 3D7 MnfTRY51cWKjY4TldolidCCDc4PhfS=> NEm0Rnc4OiCq NVe5W2liTE2VTx?= NVTKSZY2SW62aYDsZZNud2SrYXygZYN1cX[rdImge4l1cCCLQ{WwJI9nKDF{LkW4PVMh|ryP M{nCV|E6PzN2OUGw
Plasmodium falciparum GB4 NWf3[IF3SW62aXLhZ5RmemmjbDDBd5NigQ>? NXXiUo9lPzJiaB?= NGjUR5lFVVOR NUS1bJFvSW62aYDsZZNud2SrYXygZYN1cX[rdImge4l1cCCLQ{WwJI9nKDF{LkW4PVPPxE1? NUHSPYNpOTl5M{S5NVA>
RAW264.7 NWXrT2ZwTnWwY4Tpc44hSXO|YYm= NV;EVFZrOTBizszN MVSxNkBp NE\TPYFCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gUHBUNWmwZIXj[YQhVk9icILv[JVkfGmxbjD3bZRpKEmFNUCgc4YhOTgQvF2= NUnYfW45OTl2OUe0NVg>
SH-SY5Y NY\XRlhQTnWwY4Tpc44hSXO|YYm= MlrINVAh|ryP M4LFOlEhcA>? NV\iUFNSTE2VTx?= M33nXG5mfXKxcILveIVkfGm4ZTDhZ5Rqfmm2eTDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZiYX7pd49ugWOrbj3pcoR2[2WmIHPlcIwh\GWjdHi= NYjDOFRTOjN2OUi5NVQ>
SH-SY5Y MXnLbY5ie2ViQYPzZZk> Ml3CNVAh|ryP NHO4cGUyKGh? Mo[0SG1UVw>? NHrITVlKdmirYnn0bY9vKG:oIFrOT|Mh[XO|ZYPz[YQh[XNiYnzvZ4ti\GVib3[gZY5qe2:veXPpck1qdmS3Y3XkJIMucnWwIIDoc5NxcG:{eXzheIlwdiCjdDDz[ZI4Ow>? M4HnUVI{PDl6OUG0
RAW264.7 Mn7aSpVv[3Srb36gRZN{[Xl? MlHxNVAh|ryP M{THZlI1KGh? NFPCN|NCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWwuOWKndHGgdoVt\WG|ZR?= NEX1UlczOzd7MUC3PC=>
RAW264.7 M1X5N2Z2dmO2aX;uJGF{e2G7 NXPaOZF2OTBizszN M4DNU|I1KGh? NWTxU5B1SW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKGmQT2Og[ZhxemW|c3nvci=> NWPte5BLOjN5OUGwO|g>
RAW264.7 MmHHSpVv[3Srb36gRZN{[Xl? NF;sTnYyOCEQvF2= NF\mdHYzKGh? MWXBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgUm8heHKxZIXjeIlwdg>? MmPjNlM4QTFyN{i=
B16-F10 NHviTppHfW6ldHnvckBCe3OjeR?= MVSxJIg> MkTpTY5pcWKrdHnvckBw\iCWTl[tZYxxcGFvaX7keYNm\CClLVrVUkBxcG:|cHjvdplt[XSrb36= MYiyNVgyPTZ|NB?=
PC12 MlexSpVv[3Srb36gRZN{[Xl? NGLjd2wyOCEQvF2= NGnXcpA2KGh? NWX5WW51TE2VTx?= MnHDRYN1cX[jdHnvckBw\iCQcn[yM2FTTSCjc4Pld5Nm\CCjczDIU{0yKHC{b4TlbY4hcW6mdXP0bY9vKHC{ZYTy[YF1\WRid3n0bEBRTDl6MEW5 NELKVGczOTN2NU[4OS=>
PC12 NWj1NVkzTnWwY4Tpc44hSXO|YYm= M3jSRVExKM7:TR?= M{PZO|UhcA>? MlSySG1UVw>? MVXBZ5RqfmG2aX;uJI9nKE6{ZkKvRXJGKGG|c3Xzd4VlKGG|IFjPMVEheHKxdHXpckBqdmS3Y4Tpc44heHKndILlZZRm\CC5aYToJHUxOTJ4 M3u2dlIyOzR3Nki1
PC12 MVnGeY5kfGmxbjDBd5NigQ>? NYe3O4tNOTBizszN MVm1JIg> NX3xelVITE2VTx?= NFfHS|lC[3SrdnH0bY9vKG:oIF7y[lIwSVKHIHHzd4V{e2WmIHHzJGhQNTFicILveIVqdiCrbnT1Z5Rqd25icILleJJm[XSnZDD3bZRpKFOSNkCwNVI2 Ml;HNlE{PDV4OEW=
PC12 NV3LXY1{TnWwY4Tpc44hSXO|YYm= NHf5WpkyOCEQvF2= NUezSmJtPSCq M1;ucWROW09? M3XKTmFkfGm4YYTpc44hd2ZiToLmNk9CWkViYYPz[ZN{\WRiYYOgTG8uOSCycn;0[YlvKGmwZIXjeIlwdiCycnX0doVifGWmIIfpeIghW0J{MEO1PFA> M{[0OFIyOzR3Nki1
A549 MnPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXHcJRxOjBizszN MWO3NkBp M17ONWROW09? MnXnVoFxcWRiYX7kJJBwfGWwdDDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdg>? NILDT3gzOzlzMki0NC=>
PC3 NED4UFdHfW6ldHnvckBCe3OjeR?= MlT3NlUh|ryP NEm0XXYzPCCq MWnJcohq[mm2aX;uJI9nKEGSLUGgZY5lKHB{MTDseYNq\mW{YYPlJIFkfGm4aYT5JIlv\HWlZXSgZpkhWzF5OVSgVHJN NXvsfoRSOjNzNkK2OVI>
THP-1 NIqyO5RHfW6ldHnvckBCe3OjeR?= MW[5NEBvVQ>? MnjXN|AhdWmw MWDJcohq[mm2aX;uJI9nKHSrc4P1[UBn[WO2b4Kg[ZhxemW|c3nvci=> MU[yNlk1ODB3OR?=
LoVo M1LhdGZ2dmO2aX;uJGF{e2G7 MWSxJO69VQ>? NHzZUXMyKGh? NWjIdY1qUW6qaXLpeIlwdiCxZjDQS2UzNWmwZIXj[YQh\XiycnXzd4lwdiCxZjD1VGEh[W6mIF3NVE06KHOrZ37p[olk[W62bIm= MVqyNVg2QTR5OR?=
LoVo MofYSpVv[3Srb36gRZN{[Xl? MnfENUDPxE1? M{K5SFEhcA>? MWHCcI9kc3OSR1WyMYlv\HWlZXSgZ4VtdCCvaXfyZZRqd25ic3nncolncWOjboTsfS=> MluzNlE5PTl2N{m=
A549 M3S4ZmZ2dmO2aX;uJGF{e2G7 M3SybVIxKM7:TR?= MWmxJIg> M3;EZWlvcGmkaYTpc44hd2ZiVGDBMYlv\HWlZXSgUW1RNTJiYX7kJJUuWEFiZYjwdoV{e2mxbh?= M1L6NlIxPDl{MUe1
HaCaT MmfySpVv[3Srb36gRZN{[Xl? MVmyNEDPxE1? MYm0JIg> Ml7pSG1UVw>? NInrPYdDdG:la4OgeIhmKFSQRj5OtU1qdmS3Y3XkxsBEYVB2RkGxxsB1emGwc3PybZB1cW:w NYn5fHR{OTl6MUKzOFk>
HaCaT NUfyUoJ7TnWwY4Tpc44hSXO|YYm= M1jnSlIxKM7:TR?= M4fZUVI1KGh? M{TOPWROW09? NUXkb2U4SmyxY3vzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiYz3KeY4heHKxdHXpci=> MW[xPVgyOjN2OR?=
PC3 NVW4[oxiTnWwY4Tpc44hSXO|YYm= M4nKTFIxKM7:TR?= M2HLOFEhcA>? MYLE[YNz\WG|ZYOgeIhmKE2PUEKgZY5lKE2PUEmg[ZhxemW|c3nvci=> MnzTNVk3OzN7N{W=
BV-2 MV;GeY5kfGmxbjDBd5NigQ>? NU\FZWJuOiEQvF2= MkC3NUBp NXXoeHFtUW6qaXLpeJMhfGinIHnuZ5Jm[XOnIH;mJJNDSU[IIILlcIVie2ViaX6gS41qgC22cnXheIVlKEKYLUKgZ4VtdHN? MmnjNVk1ODZ6M{G=
Hep3B NV7UPVh2TnWwY4Tpc44hSXO|YYm= NF3WSVAyOCEQvF2= M4DsdFEhcA>? NVThXFdsSmyxY3vzJIF2fG:yaHHnfUBidmRidYDy[Yd2dGG2aX;uJI9nKEKnY3zpckAyKGW6cILld5Nqd25iaX7keYNm\CCkeTDj[ZJidWmmZR?= M1K2ZVE6ODZyOUKw

... 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID