For research use only. Not for therapeutic Use.
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). PF-3644022 inhibits tumor necrosis factor α (TNFα) production in U937 monocytic cells and peripheral blood mononuclear cells (PBMCs) (IC50 = 160 nM).
| Catalog Number | R057373 |
| CAS Number | 1276121-88-0 |
| Synonyms | (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; |
| Molecular Formula | C21H18N4OS |
| Purity | ≥95% |
| Target | MAPKAPK2 (MK2) |
| Solubility | Soluble in DMSO > 10 mM |
| Storage | Store at +4C |
| InChI | InChI=1S/C21H18N4OS/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)/t12-/m1/s1 |
| InChIKey | CMWRPDHVGMHLSZ-GFCCVEGCSA-N |
| SMILES | O=C1C2=C(C3=C(S2)C=CC4=NC(C5=CC=C(C)N=C5)=CC=C34)NC[C@@H](C)N1 |
| Reference | </br>1: Song H, Fang X, Wen M, Yu F, Gao K, Sun C, Wang Z. Role of MK2 signaling pathway in the chronic compression of cervical spinal cord. Am J Transl Res. 2015 Nov 15;7(11):2355-63. eCollection 2015. PubMed PMID: 26807183; PubMed Central PMCID: PMC4697715.</br>2: Mourey RJ, Burnette BL, Brustkern SJ, Daniels JS, Hirsch JL, Hood WF, Meyers MJ, Mnich SJ, Pierce BS, Saabye MJ, Schindler JF, South SA, Webb EG, Zhang J, Anderson DR. A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor alpha production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation. J Pharmacol Exp Ther. 2010 Jun;333(3):797-807. doi: 10.1124/jpet.110.166173. Epub 2010 Mar 17. PubMed PMID: 20237073.</br></br> |
