| Identification | Back Directory | [Name]
MK-2 Inhibitor III | [CAS]
1186648-22-5 | [Synonyms]
MK2-IN-3 hydrate
MK-2 Inhibitor III
MK-2 INHIBITOR III (COMPOUND 16)
MK-2 Inhibitor III - CAS 1186648-22-5 - Calbiochem
2-(2-quinolin-3-ylpyridin-4-yl)-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one:hydrate | [Molecular Formula]
C21H18N4O2 | [MOL File]
1186648-22-5.mol | [Molecular Weight]
358.4 |
| Chemical Properties | Back Directory | [Melting point ]
>255°C (dec.) | [storage temp. ]
+2C to +8C | [solubility ]
DMSO (Slightly), Methanol (Slightly) | [form ]
Pale yellow solid | [color ]
Off-White to Pale Yellow |
| Hazard Information | Back Directory | [Description]
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-α in human monocyte-like U937 cells (IC50 = 4.4 μM). | [Uses]
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-α in human monocyte-like U937 cells (IC50 = 4.4 μM).[Cayman Chemical] | [storage]
Store at -20°C | [References]
[1] XIAOHUA HUANG* Gerald W S Jr. Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors[J]. ACS Medicinal Chemistry Letters, 2011, 2 8: 632-637. DOI: 10.1021/ml200113y
[2] XIAOZHE WANG. Phosphorylation of HSF1 by MAPK-activated protein kinase 2 on serine 121, inhibits transcriptional activity and promotes HSP90 binding.[J]. The Journal of Biological Chemistry, 2006, 281 2: 782-791. DOI: 10.1074/jbc.m505822200
[3] O. WERZ. Arachidonic Acid Promotes Phosphorylation of 5-Lipoxygenase at Ser-271 by MAPK-activated Protein Kinase 2 (MK2)*[J]. The Journal of Biological Chemistry, 2002, 25 1: 14793-14800. DOI: 10.1074/jbc.m111945200
[4] DAVID R. ANDERSON. Pyrrolopyridine Inhibitors of Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MK-2)[J]. Journal of Medicinal Chemistry, 2007, 50 11: 2647-2654. DOI: 10.1021/jm0611004 |
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