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Submit ReviewPF 3644022
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)
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
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 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 |
| 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.
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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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 |
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Product Datasheets for PF 3644022
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
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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:
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
Simon et al (2023) PRMT5-mediated regulatory arginine methylation of RIPK3. Cell Death Discov 9 14 PMID: 36658119
Lingelem et al (2015) Geldanamycin Enhances Retrograde Transport of Shiga Toxin in HEp-2 Cells. PLoS One 10 e0129214 PMID: 26017782
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
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
Bouhaddou et al (2020) The Global Phosphorylation Landscape of SARS-CoV-2 Infection Cell 182 685 PMID: 32645325
Do you know of a great paper that uses PF 3644022 from Tocris? Please let us know.
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