Application
PF-3644022 hydrate has been used for the inhibition of mitogen-activated protein kinase 2 (MK2) in human osteosarcoma cells (U2OS) and in colorectal carcinoma cells (CT26).
Biochem/physiol Actions
PF-3644022 hydrate is a MK2 inhibitor
PF-3644022 is a potent inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MK2; Ki = 3 nM). PF-3644022 inhibits TNFa and IL-6 production in LPS-stimulated human whole blood (IC50 = 1.6 and 10.3 μM, respectively) and blocks TNFα production and paw swelling in a streptococcal cell wall-induced arthritis in rats.
Features and Benefits
This compound is featured on the MAPKAPs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
Other Notes
PF3644022 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the PF3644022 probe summary on the Chemical Probes Portal website.
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | yellow to orange |
| solubility | DMSO: ≥15 mg/mL |
| storage temp. | 2-8°C |
| SMILES string | O.C[C@@H]1CNc2c(sc3ccc4nc(ccc4c23)-c5ccc(C)nc5)C(=O)N1 |
| InChI | 1S/C21H18N4OS.H2O/c1-11-3-4-13(10-22-11)15-6-5-14-16(25-15)7-8-17-18(14)19-20(27-17)21(26)24-12(2)9-23-19;/h3-8,10,12,23H,9H2,1-2H3,(H,24,26);1H2/t12-;/m1./s1 |
| InChI key | WHVUIWUUCVXAGR-UTONKHPSSA-N |
