SP600125

Catalog No.S1460 Synonyms: Nsc75890

For research use only.

SP600125 (Nsc75890) 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. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.

SP600125 Chemical Structure

CAS No. 129-56-6

Selleck's SP600125 has been cited by 913 publications

Purity & Quality Control

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Biological Activity

Description SP600125 (Nsc75890) 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. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase AFLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Targets
serine/threonine kinase [1] JNK1 [1]
(Cell-free assay)
JNK2 [1]
(Cell-free assay)
Aurora A [4]
(Cell-free assay)
TrkA [4]
(Cell-free assay)
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40 nM 40 nM 60 nM 70 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
Hep3B MW\GeY5kfGmxbjDBd5NigQ>? NIXiRoMyOCEQvF2= NHT5O5YyKGh? MmrvRoxw[2u|IHH1eI9xcGGpeTDhcoQhfXC{ZXf1cIF1cW:wIH;mJGJm[2yrbjCxJIV5eHKnc4Ppc44hcW6mdXPl[EBjgSClZYLhcYll\Q>? M3vkcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7ME[wPVIxLz5zOUC2NFkzODxxYU6=
BV-2 MojrSpVv[3Srb36gRZN{[Xl? NYnuWG4zOiEQvF2= MknKNUBp Mn60TY5pcWKrdIOgeIhmKGmwY4LlZZNmKG:oIIPCRWZHKHKnbHXhd4UhcW5iR33pfE11emWjdHXkJGJXNTJiY3XscJM> NUjH[5BoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm0NFY5OzFpPkG5OFA3QDNzPD;hQi=>
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PC3 M{fRbWZ2dmO2aX;uJGF{e2G7 NXLUNZd[OjBizszN MmPnNUBp NWr3WJhxTGWlcnXhd4V{KHSqZTDNUXAzKGGwZDDNUXA6KGW6cILld5Nqd25? MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTZ|M{m3OUc,OTl4M{O5O|U9N2F-
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PC12 NX62eXpyTnWwY4Tpc44hSXO|YYm= MVSxNEDPxE1? M1fBb|UhcA>? M3y5e2ROW09? NYC1UVFSSWO2aY\heIlwdiCxZjDOdoYzN0GURTDhd5Nme3OnZDDhd{BJVy1zIIDyc5RmcW5iaX7keYN1cW:wIIDy[ZRz\WG2ZXSge4l1cCCVUE[wNFEzPQ>? NVPwNW9pRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzOFU3QDVpPkKxN|Q2Pjh3PD;hQi=>
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RAW264.7 NGHTTGZCdnSraX7mcIFudWG2b4L5JIF{e2G7 NGSzbopCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKG2xdYPlJHJCXzJ4ND63JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgUm8heHKxZIXjeIlwdiC{ZXzheIl3\SC2bzDjc451em:uLDDJR|UxKD1iMUeg{txONg>? MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjh|MUe5PEc,OjJ6M{G3PVg9N2F-
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BT-37 MYfxTHRUKGG|c3H5 NVTmNWd6eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVM4KGOnbHzz M2rqOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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OHS-50 NEfLeFhyUFSVIHHzd4F6 MlTjdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= MonEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC NUj1U5pveUiWUzDhd5NigQ>? MXTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= M3n2eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 NI[4WlNyUFSVIHHzd4F6 M4DO[ZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
LAN-5 NUi2eYJkeUiWUzDhd5NigQ>? Mn7PdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Assay
Methods Test Index PMID
Western blot p-JNK ; p-IGF1R / IGF1R / p-Akt / Akt / p-ERK / ERK ; p-Src / Src ; p-c-Jun / c-Jun / pJNK / JNK ; Survivin / Bcl-2 / PARP ; p-FADD / FADD / p-c-Jun / c-Jun 25226534 27176481 22870247 21859840
Immunofluorescence AIF / Endo G ; E-cadherin / β-catenin ; α-catenin / Actin 21738692 21030692
Growth inhibition assay Cell viability (U-87 MG) ; Cell viability (A549) 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 (from reference)

Kinase Assay:

[4]

  • 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]

  • Cell lines: HCT116, A2780, and U2OS cells
  • Concentrations: 0–5 μM
  • 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.

Animal Research:

[1]

  • Animal Models: Mouse LPS/TNF model (female CD-1)
  • Dosages: 15 or 30 mg/kg
  • Administration: Administered via intravenous injection or orally

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
For best results, use promptly after mixing.

2mg/mL

Chemical Information

Molecular Weight 220.23
Formula

C14H8N2O

CAS No. 129-56-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C2C(=C1)C3=NNC4=CC=CC(=C43)C2=O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

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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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