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
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 211 Publications

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 M3TtVGFvfGmkYXP0[ZJq[WxiQYPzZZk> NV3hPFdRPzJiaB?= MnfhSG1UVw>? MVvBcpRqeGyjc33v[IlidCCjY4Tpeol1gSC5aYToJGlEPTBib3[gO{46PDN{ODFOwG0> NWXMVHJIOTl5M{S5NVA>
Plasmodium falciparum W2 MX7BcpRq[mGldHXybYFtKEG|c3H5 NVjyU2ltPzJiaB?= MkT3SG1UVw>? NYrJcIFHSW62aYDsZZNud2SrYXygZYN1cX[rdImge4l1cCCLQ{WwJI9nKDdwOUSzNlgh|ryP NXi4PWZYOTl5M{S5NVA>
Plasmodium falciparum 7G8 MlK5RY51cWKjY4TldolidCCDc4PhfS=> NUn1cHNiPzJiaB?= M3T4WGROW09? M{DYcGFvfGmybHHzcY9lcWGuIHHjeIl3cXS7IIfpeIghUUN3MDDv[kAyOCEQvF2= NYLvZXJDOTl5M{S5NVA>
Plasmodium falciparum 3D7 NUfTV3BNSW62aXLhZ5RmemmjbDDBd5NigQ>? MUO3NkBp MlPvSG1UVw>? MX3BcpRqeGyjc33v[IlidCCjY4Tpeol1gSC5aYToJGlEPTBib3[gNVIvPTh7MzFOwG0> Mne5NVk4OzR7MUC=
Plasmodium falciparum GB4 NH\vWFZCdnSrYnHjeIVzcWGuIFHzd4F6 NEj3dIY4OiCq MYfEUXNQ MlPNRY51cXCuYYPtc4Rq[WxiYXP0bZZqfHlid3n0bEBKSzVyIH;mJFEzNjV6OUROwG0> MVexPVc{PDlzMB?=
RAW264.7 M2nYdGZ2dmO2aX;uJGF{e2G7 MWSxNEDPxE1? NYHxTZJKOTJiaB?= MorIRY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFzQV{1qdmS3Y3XkJG5QKHC{b3T1Z5Rqd25id3n0bEBKSzVyIH;mJFE4|ryP NWnCcpJxOTl2OUe0NVg>
SH-SY5Y MljTSpVv[3Srb36gRZN{[Xl? M4ToelExKM7:TR?= NUHTWldnOSCq NIP4fHZFVVOR MoC0UoV2em:ycn;0[YN1cX[nIHHjeIl3cXS7IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iCjbnnzc416[2mwLXnu[JVk\WRiY3XscEBl\WG2aB?= NIf2TpgzOzR7OEmxOC=>
SH-SY5Y NIP4cYpMcW6jc3WgRZN{[Xl? NGLXNlYyOCEQvF2= MkC5NUBp MmTXSG1UVw>? MV\Jcohq[mm2aX;uJI9nKEqQS{OgZZN{\XO|ZXSgZZMh[myxY3vh[IUhd2ZiYX7pd49ugWOrbj3pcoR2[2WmIHOtbpVvKHCqb4PwbI9zgWyjdHnvckBifCC|ZYK3Ny=> NYfOfHEyOjN2OUi5NVQ>
RAW264.7 MUXGeY5kfGmxbjDBd5NigQ>? MYqxNEDPxE1? NGDTb24zPCCq MoKyRY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFnMMVFj\XSjIILlcIVie2V? MVmyN|c6OTB5OB?=
RAW264.7 M4nRfGZ2dmO2aX;uJGF{e2G7 NYDCfFN{OTBizszN NILET40zPCCq NWCxTpJ6SW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKGmQT2Og[ZhxemW|c3nvci=> MUeyN|c6OTB5OB?=
RAW264.7 MXXGeY5kfGmxbjDBd5NigQ>? MkW0NVAh|ryP M{nvfFIhcA>? MY\BcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgUm8heHKxZIXjeIlwdg>? NV\6Xm9ZOjN5OUGwO|g>
B16-F10 MnvRSpVv[3Srb36gRZN{[Xl? Mm\GNUBp MknGTY5pcWKrdHnvckBw\iCWTl[tZYxxcGFvaX7keYNm\CClLVrVUkBxcG:|cHjvdplt[XSrb36= M{fDbVIyQDF3NkO0
PC12 M2\sNGZ2dmO2aX;uJGF{e2G7 M33IeFExKM7:TR?= Mm\KOUBp M3;wXGROW09? NIflSI5C[3SrdnH0bY9vKG:oIF7y[lIwSVKHIHHzd4V{e2WmIHHzJGhQNTFicILveIVqdiCrbnT1Z5Rqd25icILleJJm[XSnZDD3bZRpKFCGOUiwOVk> NXH5RmhlOjF|NEW2PFU>
PC12 M{DWXmZ2dmO2aX;uJGF{e2G7 M2The|ExKM7:TR?= MXq1JIg> NUnVOGRrTE2VTx?= NXPwUI1sSWO2aY\heIlwdiCxZjDOdoYzN0GURTDhd5Nme3OnZDDhd{BJVy1zIIDyc5RmcW5iaX7keYN1cW:wIIDy[ZRz\WG2ZXSge4l1cCCXMEGyOi=> M{DYSVIyOzR3Nki1
PC12 Mn;kSpVv[3Srb36gRZN{[Xl? NXK0So1qOTBizszN MlLwOUBp NIDkVZZFVVOR NFG2XG9C[3SrdnH0bY9vKG:oIF7y[lIwSVKHIHHzd4V{e2WmIHHzJGhQNTFicILveIVqdiCrbnT1Z5Rqd25icILleJJm[XSnZDD3bZRpKFOSNkCwNVI2 M4DMNlIyOzR3Nki1
PC12 M3;Nc2Z2dmO2aX;uJGF{e2G7 NGf3Z2cyOCEQvF2= M{G2WVUhcA>? MnfESG1UVw>? NXqxd3BTSWO2aY\heIlwdiCxZjDOdoYzN0GURTDhd5Nme3OnZDDhd{BJVy1zIIDyc5RmcW5iaX7keYN1cW:wIIDy[ZRz\WG2ZXSge4l1cCCVQkKwN|U5OA>? MkHXNlE{PDV4OEW=
A549 NWPRTJhJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPo[5gzOCEQvF2= NIPTTGc4OiCq MYfEUXNQ Mo[5VoFxcWRiYX7kJJBwfGWwdDDpcohq[mm2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdg>? M4fQcVI{QTF{OESw
PC3 M1LaOmZ2dmO2aX;uJGF{e2G7 MX:yOUDPxE1? M3\kPFI1KGh? NICzXHBKdmirYnn0bY9vKG:oIFHQMVEh[W6mIICyNUBtfWOrZnXyZZNmKGGldHn2bZR6KGmwZIXj[YQh[nliU{G3PWQhWFKO M2LJNFI{OTZ{NkWy
THP-1 NIfnWW9HfW6ldHnvckBCe3OjeR?= M3f5W|kxKG6P MoH4N|AhdWmw NEXFXnNKdmirYnn0bY9vKG:oIITpd5N2\SCoYXP0c5Ih\XiycnXzd4lwdg>? MWKyNlk1ODB3OR?=
LoVo MUjGeY5kfGmxbjDBd5NigQ>? MnmxNUDPxE1? Ml;jNUBp NHXJNm9KdmirYnn0bY9vKG:oIGDHSVIucW6mdXPl[EBmgHC{ZYPzbY9vKG:oIIXQRUBidmRiTV3QMVkhe2mpbnnmbYNidnSueR?= MYiyNVg2QTR5OR?=
LoVo NWjCRnJsTnWwY4Tpc44hSXO|YYm= NWHwSoxwOSEQvF2= NIfmb2syKGh? M1L4VWJtd2Otc2DHSVIucW6mdXPl[EBk\WyuIH3p[5JifGmxbjDzbYdvcW[rY3HueIx6 NFTCVoEzOTh3OUS3PS=>
A549 Moe5SpVv[3Srb36gRZN{[Xl? MX2yNEDPxE1? M370S|EhcA>? NH3jbYNKdmirYnn0bY9vKG:oIGTQRU1qdmS3Y3XkJG1OWC1{IHHu[EB2NVCDIHX4dJJme3Orb36= NXi2cmlUOjB2OUKxO|U>
HaCaT MVTGeY5kfGmxbjDBd5NigQ>? NF\JeYIzOCEQvF2= M1HKc|QhcA>? NInQXpZFVVOR Mn\NRoxw[2u|IITo[UBVVkZvzsGtbY5lfWOnZNMgR3lRPEZzMdMgeJJidnOlcnnweIlwdg>? NIe4R3MyQThzMkO0PS=>
HaCaT MYrGeY5kfGmxbjDBd5NigQ>? M4DnR|IxKM7:TR?= M1XlN|I1KGh? NF3pRYdFVVOR NYrIVZg2SmyxY3vzJJRp\SCyaH;zdIhwenmuYYTpc44hd2ZiYz3KeY4heHKxdHXpci=> MnH5NVk5OTJ|NEm=
PC3 NGrjVGtHfW6ldHnvckBCe3OjeR?= NGTBdoMzOCEQvF2= NFP4T|MyKGh? MWjE[YNz\WG|ZYOgeIhmKE2PUEKgZY5lKE2PUEmg[ZhxemW|c3nvci=> M1rlWlE6PjN|OUe1
BV-2 M3PF[WZ2dmO2aX;uJGF{e2G7 M1;ieVIh|ryP NFy5OpUyKGh? MmTZTY5pcWKrdIOgeIhmKGmwY4LlZZNmKG:oIIPCRWZHKHKnbHXhd4UhcW5iR33pfE11emWjdHXkJGJXNTJiY3XscJM> NGfUengyQTRyNkizNS=>
Hep3B NYLiNnVpTnWwY4Tpc44hSXO|YYm= NXO5eGp5OTBizszN M3nJTlEhcA>? Mlj3Roxw[2u|IHH1eI9xcGGpeTDhcoQhfXC{ZXf1cIF1cW:wIH;mJGJm[2yrbjCxJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSClZYLhcYll\Q>? MomzNVkxPjB7MkC=

... 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]
+ 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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

  • * Indicates a Required Field

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.

JNK Signaling Pathway Map

Related JNK Products

Tags: buy SP600125 | SP600125 supplier | purchase SP600125 | SP600125 cost | SP600125 manufacturer | order SP600125 | SP600125 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID