PF 3644022

Pricing Availability   Qty
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)
Citations (7)
Literature (1)

Biological Activity for PF 3644022

PF 3644022 is a 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 for PF 3644022 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 for PF 3644022

M. Wt 374.46
Formula C21H18N4OS
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1276121-88-0
PubChem ID 44631903
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for PF 3644022

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 14.98 40

Preparing Stock Solutions for PF 3644022

The following data is based on the product molecular weight 374.46. Batch specific molecular weights may vary from batch to batch due to the degree 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
0.4 mM 6.68 mL 33.38 mL 66.76 mL
2 mM 1.34 mL 6.68 mL 13.35 mL
4 mM 0.67 mL 3.34 mL 6.68 mL
20 mM 0.13 mL 0.67 mL 1.34 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and 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.

Product Datasheets for PF 3644022

Certificate of Analysis / Product Datasheet
Select another batch:

References for PF 3644022

References are publications that support the biological activity of the product.

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: PF 3644022, PF 3644022 supplier, PF3644022, mapk, mitogen-activated, protein, kinase-activated, kinase, 2, MK-2, MK2, potent, anti-inflammatory, inhibitors, inhibits, pfizer, 4279, Tocris Bioscience

7 Citations 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

Stephen J et al (2019) Clinically Advanced p38 Inhibitors Suppress DUX4 Expression in Cellular and Animal Models of Facioscapulohumeral Muscular Dystrophy. J Pharmacol Exp Ther 370 219-230 PMID: 31189728

Simon et al (2023) PRMT5-mediated regulatory arginine methylation of RIPK3. Cell Death Discov 9 14 PMID: 36658119

Tang et al (2019) K63-linked ubiquitination regulates RIPK1 kinase activity to prevent cell death during embryogenesis and inflammation. Nat Commun 10 4157 PMID: 31519887

Jaco et al (2017) MK2 Phosphorylates RIPK1 to Prevent TNF-Induced Cell Death. Mol Cell 66 698 PMID: 28506461

Bouhaddou et al (2020) The Global Phosphorylation Landscape of SARS-CoV-2 Infection Cell 182 685 PMID: 32645325

Singh et al (2018) Differential effect of p38 and MK2 kinase inhibitors on the inflammatory and toxicity biomarkers in vitro. Hum Exp Toxicol 37 521 PMID: 28629242

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

Reviews for PF 3644022

There are currently no reviews for this product. Be the first to review PF 3644022 and earn rewards!

Have you used PF 3644022?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Cell Cycle & DNA Damage Repair Poster

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. 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.