Home Tools
Log in
Cart

SP600125

Catalog No. T3109   CAS 129-56-6
Synonyms: Pyrazolanthrone, JNK Inhibitor II, 1PMV, SP-600125, Nsc75890

SP600125 is a JNK1/2/3 inhibitor (IC50: 40/40/90 nM) and 10-fold higher selectivity than MKK4, 25-fold higher selectivity than MKK3, MKK6, PKCα, and PKB.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
SP600125, CAS 129-56-6
Please contact us for prices and availability for the specification of product you are interested at.
Product consultation
Get quote
Purity 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description SP600125 is a JNK1/2/3 inhibitor (IC50: 40/40/90 nM) and 10-fold higher selectivity than MKK4, 25-fold higher selectivity than MKK3, MKK6, PKCα, and PKB.
In vitro In cells, SP600125 dose-dependently inhibited the phosphorylation of c-Jun ( IC50s: 5–10 μM), the expression of inflammatory genes COX-2, IL-2, IFN-gamma, TNF-alpha, and prevented the activation and differentiation of primary human CD4 cell cultures [1]. Fas agonistic antibody CH11-induced autophagy was blocked by SP600125, and the CH11-induced apoptosis was increased by SP600125 [2]. In synchronized cells, SP600125 prevents the entry of cells into mitosis and leads to endoreplication of DNA from G2 phase. The inhibitory effect of SP600125 on mitotic entry predominantly occurs upstream of Aurora A kinase and Polo-like kinase 1, resulting in a failure to remove the inhibitory phosphorylation of Cdk1 [3].
In vivo In control animals, CD4+ CD8+ thymocytes represented just less than 40% of total thymocytes. Forty-eight hours after exposure to CD3 Ab in vivo, the percentage of CD4+ CD8 + cells had declined to 10%. Mice receiving SP600125 showed almost complete resistance to CD3 Ab-mediated apoptosis with CD4+ CD8+ numbers the same as control animals [1]. Pulmonary edema, the expression of inflammatory cytokines and pathological alterations were found to be significantly attenuated in LPS-induced ALI following treatment with SP600125 in vivo [4].
Cell Research Multiarray plate screening of mRNA was performed by High Throughput Genomics. In brief, cell lysates were prepared by using a single-step proprietary lysis buffer. Lysates were incubated with a 16-gene capture array manufactured into each well of a 96-well plate. Detection was by luminescence and was performed by HTG. SDs for triplicate samples were typically 3–8% for samples with high levels of gene expression and 15–25% for samples with very low (near-threshold) levels of cytokine gene expression [1].
Animal Research Mouse LPS/TNF assay was performed as follows: Female CD-1 mice (8–10 weeks of age) were dosed i.v. or per os with SP600125 in PPCES vehicle (30% PEG-400/20% polypropylene glycol/15% Cremophor EL/5% ethanol/30% saline), final volume of 5 ml/kg, 15 min before i.v. injection with LPS in saline (0.5 mg/kg; Escherichia coli 055:B5). At 90 min, a terminal bleed was obtained from the abdominal vena cava, and the serum was recovered. Samples were analyzed for mouse TNF-α by using an ELISA. The in-life phase of the thymocyte apoptosis assay was performed in female C57BL/6 mice. SP600125 was administered at 0, 12, 24, and 36 h, 15 mg/kg s.c. in PPCES vehicle. Anti-CD3 (50 μg) i.p. (clone 145-2C11) was administered as a single dose immediately after SP600125 at time 0. After 48 h, mice were killed, and the thymus was dissected for thymocyte isolation. Treated and untreated mice thymuses were excised and immediately placed in complete medium (RPMI medium 1640 with 10% FBS, penicillin/streptomycin, and l-glutamine) on ice. Each thymus was then pressed between the frosted ends of 2 microscope slides to form a single cell suspension and collected through a 30 μm nylon mesh. Cells were stained for cell surface CD4 and CD8 and apoptosis and measured by flow cytometry [1].
Synonyms Pyrazolanthrone, JNK Inhibitor II, 1PMV, SP-600125, Nsc75890
Molecular Weight 220.23
Formula C14H8N2O
CAS No. 129-56-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: 1.1 mg/mL (5 mM)), with gentle warming

DMSO: 22 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature

Related compound libraries

This product is contained In the following compound libraries:
Anti-Alzheimer's Disease Compound Library Anti-Cancer Compound Library Endoplasmic Reticulum Stress Compound Library Preclinical Compound Library Autophagy Compound Library Anti-Lung Cancer Compound Library HIF-1 Signaling Pathway Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Neural Regeneration Compound Library

Related Products

Related compounds with same targets
GW779439X Monomethyl auristatin E NSC697923 Carnosic acid Eprenetapopt OTS514 Calycosin β-Elemonic Acid

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

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

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 n 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.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.