Home Tools
Log in
Cart

PF-3644022

Catalog No. T16501   CAS 1276121-88-0

PF-3644022 is an effective, selective, and ATP-competitive MAPKAPK2 (MK2) inhibitor (IC50: 5.2 nM and a Ki of 3 nM). PF-3644022 potently inhibits TNFα production and has an anti-inflammatory effect. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) (IC50s: 53 nM and 5.0 nM, respectively).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
PF-3644022 Chemical Structure
PF-3644022, CAS 1276121-88-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 119.00
5 mg In stock $ 297.00
10 mg In stock $ 472.00
25 mg In stock $ 777.00
50 mg In stock $ 1,090.00
100 mg In stock $ 1,460.00
500 mg In stock $ 2,930.00
1 mL * 10 mM (in DMSO) In stock $ 327.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 99.12%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description PF-3644022 is an effective, selective, and ATP-competitive MAPKAPK2 (MK2) inhibitor (IC50: 5.2 nM and a Ki of 3 nM). PF-3644022 potently inhibits TNFα production and has an anti-inflammatory effect. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) (IC50s: 53 nM and 5.0 nM, respectively).
Targets&IC50 MK3:53 nM, PRAK:5.0 nM, MK2:(ki)3 nM, MK2:5.2 nM
In vitro PF-3644022 potently inhibits TNFα production with similar activity (IC50 of 160 nM), in the human U937 monocytic cell line or peripheral blood mononuclear cells. PF-3644022 blocks TNFα and IL-6 production in LPS-stimulated human whole blood (IC50: 1.6 and 10.3 μM, respectively). The inhibitory activity of PF-3644022 against other MAPKAP kinase family members is evaluated. Other than MNK2 with an IC50 of 148 nM, other family members are largely not inhibited, showing at least several hundred-fold selectivity versus MK2[1].
In vivo PF-3644022 (3-100 mg/kg; oral gavage; twice a day; for 12 days; Lewis rats) treatment displays dose-dependent inhibition of chronic paw swelling. It is measured on day 21 after 12 days of oral dosing (ED50: 20 mg/kg)[1].
Molecular Weight 374.46
Formula C21H18N4OS
CAS No. 1276121-88-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 41.67 mg/mL (111.28 mM), ultrasonic and warming and heat to 80°C

TargetMolReferences and Literature

1. Mourey RJ, et al. A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor alpha production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation. J Pharmacol Exp Ther. 2010 Jun;333(3):797-807

Related compound libraries

This product is contained In the following compound libraries:
Pyroptosis Compound Library Anti-Liver Cancer Compound Library Immunology/Inflammation Compound Library NO PAINS Compound Library MAPK Inhibitor Library Anti-Prostate Cancer Compound Library HIF-1 Signaling Pathway Compound Library Anti-Colorectal Cancer Compound Library Bioactive Compounds Library Max Inhibitor Library

Related Products

Related compounds with same targets
Pseudolaric Acid B ent-11alpha-Hydroxy-15-oxokaur-16-en-19-oic acid Lucideric acid A Skatole p38 Kinase inhibitor 4 Obacunone p38α inhibitor 3 Manassantin B

TargetMolDose Conversion

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

TargetMol 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

TargetMolCalculator

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.

Keywords

PF-3644022 1276121-88-0 MAPK Proteases/Proteasome Serine Protease p38 MAPK MAPKAP kinase 2 monocytic lipopolysaccharide IL-6 TNFα safety Anti-inflammatory orally PRAK efficacious PF3644022 inhibit Mitogen-activated protein kinase activated protein kinase 2 Inhibitor MK3 PF 3644022 MAP kinase activated protein kinase 2 MAPKAPK2 (MK2) MAPK activated protein kinase 2 inhibitor

 

TargetMol