MK2 Inhibitor III

• CAT Number: R065138
• CAS Number: 1186648-22-5
• Molecular Formula: C21H18N4O2
• Molecular Weight: 358.401
• Purity: ≥95%
• Synonyms: 1,5,6,7-tetrahydro-2-[2-(3-quinolinyl)-4-pyridinyl]-4H-pyrrolo[3,2-c]pyridin-4-one, monohydrate
• Target: MAPKAPK2 (MK2)
• Storage: -20°C
• IUPAC Name: 2-(2-quinolin-3-ylpyridin-4-yl)-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one;hydrate
• InChI: InChI=1S/C21H16N4O.H2O/c26-21-16-11-20(25-18(16)6-8-23-21)14-5-7-22-19(10-14)15-9-13-3-1-2-4-17(13)24-12-15;/h1-5,7,9-12,25H,6,8H2,(H,23,26);1H2
• InChIKey: NIKCVKMHGQQSRN-UHFFFAOYSA-N
• SMILES: C1CNC(=O)C2=C1NC(=C2)C3=CC(=NC=C3)C4=CC5=CC=CC=C5N=C4.O

MAP kinase-<wbr></wbr>activated protein kinase 2 (MAPKAP2, MK2) is a stress-<wbr></wbr>activated serine/threonine protein kinase that is phosphorylated by p38 MAP kinase and is involved in diverse cellular functions with a central role in inflammation. MK2 inhibitor III is a potent, cell-<wbr></wbr>permeable inhibitor of MK2 (IC50 = 8.5 nM). It less potently blocks MK3 and MK5 (IC50s = 210 and 81 nM, respectively) and is weak or inactive against several other kinases, including other p38 MAP kinase targets. MK2 inhibitor III prevents LPS-<wbr></wbr>induced synthesis of TNF-<wbr></wbr>α in human monocyte-<wbr></wbr>like U937 cells (IC50 = 4.4 µM).

Reference

1.Huang, X.,Shipps, G.W., Jr.,Cheng, C.C., et al. Discovery and hit-to-lead optimization of non-ATP competitive MK2 (MAPKAPK2) inhibitors. ACS Med.Chem.Lett. 2, 632-637 (2011).