SP600125

For research use only. Not for use in humans.

Catalog No.S1460 Synonyms: Nsc75890

652 publications

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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Selleck's SP600125 has been cited by 652 publications

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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 NFL5XGxCdnSrYnHjeIVzcWGuIFHzd4F6 MmfEO|IhcA>? NXXndXRLTE2VTx?= M3;4e2FvfGmybHHzcY9lcWGuIHHjeIl3cXS7IIfpeIghUUN3MDDv[kA4Njl2M{K4JO69VQ>? NWW0N2xxOTl5M{S5NVA>
Plasmodium falciparum W2 M3LubWFvfGmkYXP0[ZJq[WxiQYPzZZk> M3;VZlczKGh? Ml3lSG1UVw>? NHLFNnhCdnSrcHzhd41w\GmjbDDhZ5Rqfmm2eTD3bZRpKEmFNUCgc4YhPy57NEOyPEDPxE1? MWexPVc{PDlzMB?=
Plasmodium falciparum 7G8 NFfob4hCdnSrYnHjeIVzcWGuIFHzd4F6 Mlj1O|IhcA>? NEjUfldFVVOR MVfBcpRqeGyjc33v[IlidCCjY4Tpeol1gSC5aYToJGlEPTBib3[gNVAh|ryP NG[zNpkyQTd|NEmxNC=>
Plasmodium falciparum 3D7 M3v1UWFvfGmkYXP0[ZJq[WxiQYPzZZk> NEnqfFY4OiCq NIPV[VhFVVOR MVfBcpRqeGyjc33v[IlidCCjY4Tpeol1gSC5aYToJGlEPTBib3[gNVIvPTh7MzFOwG0> NHrvO3oyQTd|NEmxNC=>
Plasmodium falciparum GB4 NI[yVG5CdnSrYnHjeIVzcWGuIFHzd4F6 M2Dwc|czKGh? NIDDcWpFVVOR NFPET5JCdnSrcHzhd41w\GmjbDDhZ5Rqfmm2eTD3bZRpKEmFNUCgc4YhOTJwNUi5N:69VQ>? NYf3e5piOTl5M{S5NVA>
RAW264.7 NHHjdo9HfW6ldHnvckBCe3OjeR?= MYWxNEDPxE1? NWjIbXdjOTJiaB?= Ml7VRY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFzQV{1qdmS3Y3XkJG5QKHC{b3T1Z5Rqd25id3n0bEBKSzVyIH;mJFE4|ryP NIDzUWUyQTR7N{SxPC=>
SH-SY5Y NEWzVJVHfW6ldHnvckBCe3OjeR?= MUmxNEDPxE1? NFnWR5oyKGh? MYHEUXNQ NW[0bW9oVmW3cn;wdo91\WO2aY\lJIFkfGm4aYT5JIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCxZjDhcol{d227Y3nuMYlv\HWlZXSgZ4VtdCCmZXH0bC=> NWf2Z4t2OjN2OUi5NVQ>
SH-SY5Y NE\rXWhMcW6jc3WgRZN{[Xl? MlLvNVAh|ryP MUSxJIg> MmTiSG1UVw>? NYDRWYM{UW6qaXLpeIlwdiCxZjDKUms{KGG|c3Xzd4VlKGG|IHLsc4Ns[WSnIH;mJIFvcXOxbYnjbY4ucW6mdXPl[EBkNWq3bjDwbI9{eGixconsZZRqd25iYYSgd4VzPzN? NGfSZo4zOzR7OEmxOC=>
RAW264.7 MWXGeY5kfGmxbjDBd5NigQ>? MkPMNVAh|ryP NWe2SJVKOjRiaB?= NHrOcZVCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTWwuOWKndHGgdoVt\WG|ZR?= MVuyN|c6OTB5OB?=
RAW264.7 M1zMWmZ2dmO2aX;uJGF{e2G7 NWjsR|R[OTBizszN NFHvbXEzPCCq NXjafoFISW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKGmQT2Og[ZhxemW|c3nvci=> MnLTNlM4QTFyN{i=
RAW264.7 NH7jWJhHfW6ldHnvckBCe3OjeR?= NXK2fYpGOTBizszN MYiyJIg> NGqz[IxCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gUHBUNWmwZIXj[YQhVk9icILv[JVkfGmxbh?= NG\VRWgzOzd7MUC3PC=>
B16-F10 MnTESpVv[3Srb36gRZN{[Xl? MoDkNUBp M4naXWlvcGmkaYTpc44hd2ZiVF7GMYFteGijLXnu[JVk\WRiYz3KWW4heGixc4Doc5J6dGG2aX;u MXeyNVgyPTZ|NB?=
PC12 NXfme21GTnWwY4Tpc44hSXO|YYm= M{fROlExKM7:TR?= MmjyOUBp NITEelBFVVOR MnLHRYN1cX[jdHnvckBw\iCQcn[yM2FTTSCjc4Pld5Nm\CCjczDIU{0yKHC{b4TlbY4hcW6mdXP0bY9vKHC{ZYTy[YF1\WRid3n0bEBRTDl6MEW5 M2rtV|IyOzR3Nki1
PC12 NEPuUJNHfW6ldHnvckBCe3OjeR?= Mn3vNVAh|ryP MUS1JIg> NInmNY5FVVOR M3njb2FkfGm4YYTpc44hd2ZiToLmNk9CWkViYYPz[ZN{\WRiYYOgTG8uOSCycn;0[YlvKGmwZIXjeIlwdiCycnX0doVifGWmIIfpeIghXTBzMk[= NY\4[IxmOjF|NEW2PFU>
PC12 NYXLOo9vTnWwY4Tpc44hSXO|YYm= MYOxNEDPxE1? NFHMeI02KGh? MYDEUXNQ M2rmV2FkfGm4YYTpc44hd2ZiToLmNk9CWkViYYPz[ZN{\WRiYYOgTG8uOSCycn;0[YlvKGmwZIXjeIlwdiCycnX0doVifGWmIIfpeIghW1B4MECxNlU> NXPZZ|k6OjF|NEW2PFU>
PC12 NHjpe2NHfW6ldHnvckBCe3OjeR?= M2PV[lExKM7:TR?= MV[1JIg> MYnEUXNQ MXzBZ5RqfmG2aX;uJI9nKE6{ZkKvRXJGKGG|c3Xzd4VlKGG|IFjPMVEheHKxdHXpckBqdmS3Y4Tpc44heHKndILlZZRm\CC5aYToJHNDOjB|NUiw MWSyNVM1PTZ6NR?=
A549 M{[yWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HzZ|IxKM7:TR?= MmjOO|IhcA>? NIf2N4NFVVOR MXPSZZBq\CCjbnSgdI91\W62IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9v NWf3WllROjN7MUK4OFA>
PC3 MnrISpVv[3Srb36gRZN{[Xl? NFXLSokzPSEQvF2= MVqyOEBp M1X3fWlvcGmkaYTpc44hd2ZiQWCtNUBidmRicEKxJIx2[2moZYLhd4Uh[WO2aY\peJkhcW6mdXPl[EBjgSCVMUe5SEBRWkx? MnXpNlMyPjJ4NUK=
THP-1 MX3GeY5kfGmxbjDBd5NigQ>? MYO5NEBvVQ>? Ml;YN|AhdWmw MWXJcohq[mm2aX;uJI9nKHSrc4P1[UBn[WO2b4Kg[ZhxemW|c3nvci=> MV[yNlk1ODB3OR?=
LoVo M2DVU2Z2dmO2aX;uJGF{e2G7 M{j3RVEh|ryP NVXvUm1lOSCq MWjJcohq[mm2aX;uJI9nKFCJRUKtbY5lfWOnZDDlfJBz\XO|aX;uJI9nKHWSQTDhcoQhVU2SLUmgd4lodmmoaXPhcpRtgQ>? MkT0NlE5PTl2N{m=
LoVo NWXadFl2TnWwY4Tpc44hSXO|YYm= MVixJO69VQ>? MYWxJIg> MV7CcI9kc3OSR1WyMYlv\HWlZXSgZ4VtdCCvaXfyZZRqd25ic3nncolncWOjboTsfS=> NYnSXpZ7OjF6NUm0O|k>
A549 MkHaSpVv[3Srb36gRZN{[Xl? NWnpe3FtOjBizszN NF\FdHQyKGh? NXPiNGRZUW6qaXLpeIlwdiCxZjDUVGEucW6mdXPl[EBOVVBvMjDhcoQhfS2SQTDlfJBz\XO|aX;u MYOyNFQ6OjF5NR?=
HaCaT M4rjO2Z2dmO2aX;uJGF{e2G7 MkjRNlAh|ryP MXS0JIg> MWnEUXNQ MVTCcI9kc3NidHjlJHRPTi4QsT3pcoR2[2WmwrDDXXA1TjFzwrD0doFve2O{aYD0bY9v NXixXFk5OTl6MUKzOFk>
HaCaT Mor1SpVv[3Srb36gRZN{[Xl? MX2yNEDPxE1? NFzTSGczPCCq NFP4bVNFVVOR NX\ETGNXSmyxY3vzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiYz3KeY4heHKxdHXpci=> MnHNNVk5OTJ|NEm=
PC3 M1fzV2Z2dmO2aX;uJGF{e2G7 MnPaNlAh|ryP MVmxJIg> MYXE[YNz\WG|ZYOgeIhmKE2PUEKgZY5lKE2PUEmg[ZhxemW|c3nvci=> MlL2NVk3OzN7N{W=
BV-2 Mnu2SpVv[3Srb36gRZN{[Xl? NFPnUFczKM7:TR?= NX;iPW5POSCq NGHydIpKdmirYnn0d{B1cGViaX7jdoVie2Vib3[gd2JCTkZicnXs[YF{\SCrbjDHcYl5NXS{ZXH0[YQhSlZvMjDj[Yxtew>? MVKxPVQxPjh|MR?=
Hep3B MnmySpVv[3Srb36gRZN{[Xl? NH[5O2QyOCEQvF2= MoexNUBp MXnCcI9kc3NiYYX0c5Bp[We7IHHu[EB2eHKnZ4XsZZRqd25ib3[gRoVkdGmwIEGg[ZhxemW|c3nvckBqdmS3Y3XkJIJ6KGOncnHtbYRm NV6xTXhROTlyNkC5NlA>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-JNK; 

PubMed: 25226534     


(A) HepG2 cells were treated with increasing doses of SP600125 for 48 h, followed by western blot analysis of c-Jun N-terminal kinases (JNK) phosphorylation;

p-IGF1R / IGF1R / p-Akt / Akt / p-ERK / ERK; 

PubMed: 25226534     


(B) HepG2 cells were treated with SP600125 for 48 h at the indicated doses, followed by western blot analysis of phosphorylated IGF-1R, Akt, Erk1/2 and total IGF-1R, Akt, Erk1/2; (C) HepG2 cells were treated with 15 µM SP600125 for indicated periods, followed by western blot analysis of phosphorylated IGF-1R, Akt, Erk1/2 and total IGF-1R, Akt, Erk1/2;

p-Src / Src; 

PubMed: 25226534     


HepG2 cells were treated with 15 µM SP600125 for the indicated time. Total protein extracts were harvested and subjected to western blot analysis of phosphorylated Src and total Src.

p-c-Jun / c-Jun / pJNK / JNK; 

PubMed: 27176481     


JNK inhibitor SP600125 suppressed JNK signaling via reducing c-Jun phosphorylation, whereas JNK phosphorylation was not affected

Survivin / Bcl-2 / PARP; 

PubMed: 22870247     


The effect of SP600125 on the apoptosis regulator proteins in SW1116/HCPT cells were measured by Western-blot analysis.

p-FADD / FADD / p-c-Jun / c-Jun ; 

PubMed: 21859840     


A549-FKR cells were treated as described for FKR reporter assay and lysates analyzed with specific antibodies by western blot. Treatment with FADD-kinase inhibitor SP600125 shows dose dependent decrease in phosphorylated FADD protein that correlates with FKR activity.

25226534 27176481 22870247 21859840
Immunofluorescence
AIF / Endo G; 

PubMed: 21738692     


Representative confocal images showing translocation of AIF and Endo G to the nucleus, and nuclear condensation, at the indicated times after treatment with 5 µM of β-lap for 6 h in the presence or absence of SP600125 (30 µM). Nuclear translocation of AIF and Endo G is demonstrated by overlap of AIF or Endo G (green) and nuclear staining (red), resulting in a yellow color. 

E-cadherin / β-catenin ; 

PubMed: 21030692     


Human primary keratinocytes were treated with 10 μM SP600125 for 30 min or transduced with recombinant lentivirus encoding for flag-JNK1DN. Confocal of cells stained for β-catenin (red) and E-cadherin (green). Cell nuclei were stained with Hoechst (blue). 

α-catenin / Actin ; 

PubMed: 21030692     


Confocal images of the cells stained with α-catenin (red) and actin phalloidin (green). Cell nuclei were stained with Hoechst (blue). Scale bars = 20 μm.

21738692 21030692
Growth inhibition assay
Cell viability (U-87 MG); 

PubMed: 27176481     


U-87 MG cells were treated with SP600125 at different concentrations for 48 h. DMSO was used as a carrier control. Cell viability of U-87 MG cells sharply decreased when treated with SP600125.

Cell viability (A549); 

PubMed: 24944614     


Cells were treated with different concentrations of SP600125 (between 0 and 40 nM). The Cell Counting kit (CCK)-8 assay were then performed to measure the A549 cell viability. *P<0.05 vs. control; #P<0.05 vs. ALI.

27176481 24944614
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]
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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]
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  • 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]
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  • 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
Smiles O=C1C2=C(C=CC=C2)C3=N[NH]C4=CC=CC1=C34

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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.

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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