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PF 3644022

Catalog #: 4279
7 Citations Datasheet / COA / SDS
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4279/10
PF 3644022 | CAS No. 1276121-88-0 | MAPK Inhibitors
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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%

Product Details
Citations (7)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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.

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 40 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.

Product Datasheets

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Citations for PF 3644022

The citations listed below are publications that use Tocris products. Selected citations for PF 3644022 include:

7 Citations: Showing 1 - 7

  1. PRMT5-mediated regulatory arginine methylation of RIPK3.
    Authors: Simon Et al.
    Cell Death Discov  2023;9:14
  2. The Global Phosphorylation Landscape of SARS-CoV-2 Infection
    Authors: Bouhaddou Et al.
    Cell  2020;182:685
  3. Clinically Advanced p38 Inhibitors Suppress DUX4 Expression in Cellular and Animal Models of Facioscapulohumeral Muscular Dystrophy.
    Authors: Stephen J Et al.
    J Pharmacol Exp Ther  2019;370:219-230
  4. K63-linked ubiquitination regulates RIPK1 kinase activity to prevent cell death during embryogenesis and inflammation.
    Authors: Tang Et al.
    Nat Commun  2019;10:4157
  5. Differential effect of p38 and MK2 kinase inhibitors on the inflammatory and toxicity biomarkers in vitro.
    Authors: Singh Et al.
    Hum Exp Toxicol  2018;37:521
  6. MK2 Phosphorylates RIPK1 to Prevent TNF-Induced Cell Death.
    Authors: Jaco Et al.
    Mol Cell  2017;66:698
  7. Geldanamycin Enhances Retrograde Transport of Shiga Toxin in HEp-2 Cells.
    Authors: Lingelem Et al.
    PLoS One  2015;10:e0129214

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