PF 3644022

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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 (2)
Reviews
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.

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

Solubility Data

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

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.

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

Certificate of Analysis / Product Datasheet
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References

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

2 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

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


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