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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Cited by 638 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 MnrQRY51cWKjY4TldolidCCDc4PhfS=> NUOxbYhjPzJiaB?= MV7EUXNQ MnXFRY51cXCuYYPtc4Rq[WxiYXP0bZZqfHlid3n0bEBKSzVyIH;mJFcvQTR|Mkig{txO NUf6dpZvOTl5M{S5NVA>
Plasmodium falciparum W2 NFfwcG9CdnSrYnHjeIVzcWGuIFHzd4F6 MlfyO|IhcA>? NEC4cnpFVVOR MmrTRY51cXCuYYPtc4Rq[WxiYXP0bZZqfHlid3n0bEBKSzVyIH;mJFcvQTR|Mkig{txO NGPafpYyQTd|NEmxNC=>
Plasmodium falciparum 7G8 NYHUT3ZySW62aXLhZ5RmemmjbDDBd5NigQ>? MmXoO|IhcA>? MV;EUXNQ MV7BcpRqeGyjc33v[IlidCCjY4Tpeol1gSC5aYToJGlEPTBib3[gNVAh|ryP NUXufnQ6OTl5M{S5NVA>
Plasmodium falciparum 3D7 MkPRRY51cWKjY4TldolidCCDc4PhfS=> MYe3NkBp M3\TNWROW09? Mk\RRY51cXCuYYPtc4Rq[WxiYXP0bZZqfHlid3n0bEBKSzVyIH;mJFEzNjV6OUOg{txO NF\RfGcyQTd|NEmxNC=>
Plasmodium falciparum GB4 MXfBcpRq[mGldHXybYFtKEG|c3H5 NVHoUW1TPzJiaB?= NVrqRmlwTE2VTx?= MkC3RY51cXCuYYPtc4Rq[WxiYXP0bZZqfHlid3n0bEBKSzVyIH;mJFEzNjV6OUROwG0> MnO0NVk4OzR7MUC=
RAW264.7 NFX1cmhHfW6ldHnvckBCe3OjeR?= M{TmdFExKM7:TR?= M4DkVlEzKGh? NEDLfVJCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gUHBUNWmwZIXj[YQhVk9icILv[JVkfGmxbjD3bZRpKEmFNUCgc4YhOTgQvF2= NEjqbWgyQTR7N{SxPC=>
SH-SY5Y NELPRXNHfW6ldHnvckBCe3OjeR?= M1zWS|ExKM7:TR?= M3vLelEhcA>? NE\CWotFVVOR MWXO[ZVzd3C{b4TlZ5RqfmViYXP0bZZqfHliYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKGGwaYPvcZlkcW5vaX7keYNm\CClZXzsJIRm[XSq M4GzXVI{PDl6OUG0
SH-SY5Y MW\LbY5ie2ViQYPzZZk> MlnlNVAh|ryP MXWxJIg> M{HMSGROW09? MmHGTY5pcWKrdHnvckBw\iCMTluzJIF{e2W|c3XkJIF{KGKub3PrZYRmKG:oIHHubZNwdXmlaX6tbY5lfWOnZDDjMYp2diCyaH;zdIhwenmuYYTpc44h[XRic3XyO|M> NH7FTlUzOzR7OEmxOC=>
RAW264.7 M4\Q[GZ2dmO2aX;uJGF{e2G7 NInafYYyOCEQvF2= MUOyOEBp MWfBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiSVytNYJmfGFicnXs[YF{\Q>? MoLNNlM4QTFyN{i=
RAW264.7 NHfuZ5RHfW6ldHnvckBCe3OjeR?= NHf5eHkyOCEQvF2= MlLHNlQhcA>? NFvl[VlCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gUHBUNWmwZIXj[YQhcU6RUzDlfJBz\XO|aX;u MXGyN|c6OTB5OB?=
RAW264.7 MX;GeY5kfGmxbjDBd5NigQ>? NV\1NlNmOTBizszN Ml3QNkBp MV7BcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgUm8heHKxZIXjeIlwdg>? NETscG0zOzd7MUC3PC=>
B16-F10 MoTSSpVv[3Srb36gRZN{[Xl? MlLXNUBp NEPwUZZKdmirYnn0bY9vKG:oIGTOSk1idHCqYT3pcoR2[2WmIHOtTnVPKHCqb4PwbI9zgWyjdHnvci=> NHrDeZUzOThzNU[zOC=>
PC12 MXHGeY5kfGmxbjDBd5NigQ>? NHjNdG0yOCEQvF2= MUO1JIg> MlniSG1UVw>? NVKzb3F2SWO2aY\heIlwdiCxZjDOdoYzN0GURTDhd5Nme3OnZDDhd{BJVy1zIIDyc5RmcW5iaX7keYN1cW:wIIDy[ZRz\WG2ZXSge4l1cCCSREm4NFU6 NHnQV20zOTN2NU[4OS=>
PC12 MlHLSpVv[3Srb36gRZN{[Xl? M{X1eVExKM7:TR?= M1;pd|UhcA>? Ml;nSG1UVw>? NGDxdWhC[3SrdnH0bY9vKG:oIF7y[lIwSVKHIHHzd4V{e2WmIHHzJGhQNTFicILveIVqdiCrbnT1Z5Rqd25icILleJJm[XSnZDD3bZRpKFVyMUK2 M3rW[|IyOzR3Nki1
PC12 MmfFSpVv[3Srb36gRZN{[Xl? NGOySGoyOCEQvF2= M1zpfFUhcA>? NYfHSFZwTE2VTx?= M1z0VGFkfGm4YYTpc44hd2ZiToLmNk9CWkViYYPz[ZN{\WRiYYOgTG8uOSCycn;0[YlvKGmwZIXjeIlwdiCycnX0doVifGWmIIfpeIghW1B4MECxNlU> NYHUOlBxOjF|NEW2PFU>
PC12 M1LORmZ2dmO2aX;uJGF{e2G7 MVixNEDPxE1? MnrpOUBp Mmj3SG1UVw>? M{LDSWFkfGm4YYTpc44hd2ZiToLmNk9CWkViYYPz[ZN{\WRiYYOgTG8uOSCycn;0[YlvKGmwZIXjeIlwdiCycnX0doVifGWmIIfpeIghW0J{MEO1PFA> NWexZYVPOjF|NEW2PFU>
A549 Mle3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37LV|IxKM7:TR?= NEDkcFk4OiCq Mo\iSG1UVw>? NFf2dZhT[XCrZDDhcoQheG:2ZX70JIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:w MY[yN|kyOjh2MB?=
PC3 NX\Nbow5TnWwY4Tpc44hSXO|YYm= NF7SfZYzPSEQvF2= MYWyOEBp MYTJcohq[mm2aX;uJI9nKEGSLUGgZY5lKHB{MTDseYNq\mW{YYPlJIFkfGm4aYT5JIlv\HWlZXSgZpkhWzF5OVSgVHJN MXuyN|E3OjZ3Mh?=
THP-1 Ml;5SpVv[3Srb36gRZN{[Xl? MlXGPVAhdk1? MUKzNEBucW5? NWLnfIVFUW6qaXLpeIlwdiCxZjD0bZN{fWViZnHjeI9zKGW6cILld5Nqd25? NVv2VYZxOjJ7NECwOVk>
LoVo NX;aZ3J2TnWwY4Tpc44hSXO|YYm= NEDaSHEyKM7:TR?= NF[4cFgyKGh? MV\Jcohq[mm2aX;uJI9nKFCJRUKtbY5lfWOnZDDlfJBz\XO|aX;uJI9nKHWSQTDhcoQhVU2SLUmgd4lodmmoaXPhcpRtgQ>? MkXpNlE5PTl2N{m=
LoVo MkPNSpVv[3Srb36gRZN{[Xl? NEHSXm4yKM7:TR?= MYWxJIg> MYHCcI9kc3OSR1WyMYlv\HWlZXSgZ4VtdCCvaXfyZZRqd25ic3nncolncWOjboTsfS=> NYDMbo55OjF6NUm0O|k>
A549 MkDMSpVv[3Srb36gRZN{[Xl? Mo\HNlAh|ryP NVvM[I1qOSCq MYDJcohq[mm2aX;uJI9nKFSSQT3pcoR2[2WmIF3NVE0zKGGwZDD1MXBCKGW6cILld5Nqd25? NIrVTIozODR7MkG3OS=>
HaCaT MWnGeY5kfGmxbjDBd5NigQ>? NV3pU2ZyOjBizszN MVG0JIg> MWTEUXNQ NVPHOlcxSmyxY3vzJJRp\SCWTl[t{tEucW6mdXPl[OKhS1mSNF[xNeKhfHKjboPjdolxfGmxbh?= NHPYSFgyQThzMkO0PS=>
HaCaT NUXN[W9VTnWwY4Tpc44hSXO|YYm= MVGyNEDPxE1? MmP0NlQhcA>? MnTVSG1UVw>? NWXsb3pOSmyxY3vzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiYz3KeY4heHKxdHXpci=> MYexPVgyOjN2OR?=
PC3 NEPHcXVHfW6ldHnvckBCe3OjeR?= MkfCNlAh|ryP NH3nRpIyKGh? MVjE[YNz\WG|ZYOgeIhmKE2PUEKgZY5lKE2PUEmg[ZhxemW|c3nvci=> M2XsXFE6PjN|OUe1
BV-2 M4rVcmZ2dmO2aX;uJGF{e2G7 M37yO|Ih|ryP NIT1SmIyKGh? MV3Jcohq[mm2czD0bIUhcW6lcnXhd4Uhd2Zic1LBSmYhemWuZXHz[UBqdiCJbXn4MZRz\WG2ZXSgRnYuOiClZXzsdy=> M1TZblE6PDB4OEOx
Hep3B M1vGZmZ2dmO2aX;uJGF{e2G7 MUixNEDPxE1? NEjpTIgyKGh? M1;2dWJtd2OtczDheZRweGijZ4mgZY5lKHWycnXneYxifGmxbjDv[kBD\WOuaX6gNUBmgHC{ZYPzbY9vKGmwZIXj[YQh[nliY3XyZY1q\GV? NVrQ[2ZtOTlyNkC5NlA>

... 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

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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