PF 3644022

Pricing Availability Delivery Time Qty
Cat.No. 4279 - PF 3644022 | C21H18N4OS | CAS No. 1276121-88-0
Description: Potent MK2 inhibitor
Chemical Name: (10R)-9,10,11,12-Tetrahydro-10-methyl-3-(6-methyl-3-pyridinyl)-8H-[1,4]diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Literature

Biological Activity

Potent, ATP-competitive inhibitor of mitogen-activated protein kinase (MAPK)-activated protein kinase-2 (MK2) (IC50 = 5.2 nM; Ki = 3 nM). Inhibits tumor necrosis factor α (TNFα) production in U937 monocytic cells and peripheral blood mononuclear cells (PBMCs) (IC50 = 160 nM); exhibits oral efficacy in acute and chronic inflammatory models.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PF 3644022 is reviewed on the chemical probes website..

Technical Data

M. Wt 374.46
Formula C21H18N4OS
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1276121-88-0
PubChem ID 44631903
InChI Key CMWRPDHVGMHLSZ-GFCCVEGCSA-N
Smiles O=C(N[C@H](C)CN4)C3=C4C1=C(S3)C=CC2=C1C=CC(C5=CC=C(C)N=C5)=N2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 37.45 100

Preparing Stock Solutions

The following data is based on the product molecular weight 374.46. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.67 mL 13.35 mL 26.71 mL
5 mM 0.53 mL 2.67 mL 5.34 mL
10 mM 0.27 mL 1.34 mL 2.67 mL
50 mM 0.05 mL 0.27 mL 0.53 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

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

Reconstitution Calculator

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.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Mourey et al (2010) A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor α production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation. J.Pharmacol.Exp.Ther. 333 797 PMID: 20237073


If you know of a relevant reference for PF 3644022, please let us know.

View Related Products by Target

View Related Products by Product Action

View all MK2 Inhibitors

Keywords: PF3644022 mapk mitogen-activated protein kinase-activated protein kinase 2 MK-2 MK2 potent anti-inflammatory inhibitors inhibits pfizer MK2

1 Citation for PF 3644022

Citations are publications that use Tocris products. Selected citations for PF 3644022 include:

Lingelem et al (2015) Geldanamycin Enhances Retrograde Transport of Shiga Toxin in HEp-2 Cells. PLoS One 10 e0129214 PMID: 26017782


Do you know of a great paper that uses PF 3644022 from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Immunology

Immunology Product Listing

A collection of over 190 products for immunology research, the guide includes research tools for the study of:

  • Chemokine and Cytokine Signaling
  • Chemotaxis
  • Complement System
  • Immune Cell Signaling
  • Inflammation
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.

Pathways for PF 3644022

Protocols

TODO: Add Protocols