MK2 Inhibitor III

MAP kinase-activated protein kinase 2 (MAPKAP2, MK2) is a stress-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-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-induced synthesis of TNF-alpha in human monocyte-like U937 cells (IC50 = 4.4 µM).Formal Name: 1,5,6,7-tetrahydro-2-[2-(3-quinolinyl)-4-pyridinyl]-4H-pyrrolo[3,2-c]pyridin-4-one, monohydrate. CAS Number: 1186648-22-5. Molecular Formula: C21H16N4O . H2O. Formula Weight: 358.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1.4 mg/ml, DMSO: 5 mg/ml, DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml. lambdamax: 208, 243, 309 nm. SMILES: O=C(NCC1)C2=C1NC(C3=CC(C4=CC(C=CC=C5)=C5N=C4)=NC=C3)=C2.O. InChi Code: 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. InChi Key: NIKCVKMHGQQSRN-UHFFFAOYSA-N.