Chemical Structure : PF-3644022
CAS No.: 1276121-88-0
Catalog No.: PC-70143Not For Human Use, Lab Use Only.
PF-3644022 is a potent and selective, freely reversible, ATP-competitive inhibitor of MAPKAP2 (MK2) with Ki of 3 nM.
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PF-3644022 is a potent and selective, freely reversible, ATP-competitive inhibitor of MAPKAP2 (MK2) with Ki of 3 nM.
PF-3644022 shows good selectivity against a panel of 200 human kinases.
PF-3644022 potently inhibits TNFα production with similar activity (IC50=160 nM) in U937 cells and hPBMCs, blocks TNFα and IL-6 production in LPS-stimulated human whole blood with IC50 of 1.6 and 10.3 uM, respectively.
PF-3644022 is activite in the rat LPS-induced TNFalpha model and orally efficacious.
M.Wt | 374.46 | |
Formula | C21H18N4OS | |
Appearance | Solid | |
Storage |
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Solubility |
100 mM in DMSO (37.4 mg/mL) |
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Chemical Name/SMILES |
(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 |
1. Mourey RJ, et al. J Pharmacol Exp Ther. 2010 Jun;333(3):797-807.
2. Song H, et al. Am J Transl Res. 2015 Nov 15;7(11):2355-63.
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