PF 3644022

Cat. No. 4279

PF 3644022 C21H18N4OS [1276121-88-0]

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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

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
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
1276121-88-0

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

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.

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.

View Related Products by Target

MK2

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Keywords: PF 3644022, supplier, PF3644022, mapk, mitogen-activated, protein, kinase-activated, protein, kinase, 2, MK-2, MK2, potent, anti-inflammatory, inhibitors, inhibits, pfizer, Tocris Bioscience, MK2 Inhibitor products

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