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MK-2 Inhibitor III

Names

[ CAS No. ]:
1186648-22-5

[ Name ]:
MK-2 Inhibitor III

[Synonym ]:
2-[2-(3-Quinolinyl)-4-pyridinyl]-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-c]pyridin-4-one hydrate (1:1)
4H-Pyrrolo[3,2-c]pyridin-4-one, 1,5,6,7-tetrahydro-2-[2-(3-quinolinyl)-4-pyridinyl]-, hydrate (1:1)

Biological Activity

[Description]:

MK-2 Inhibitor III (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 0.85 nM, and is exceptional selectivity against MK-3 (IC50=0.21 μM), MK-5 (IC50=0.081 μM), ERK2 (IC50=3.44 μM), MNK1(IC50=5.7 μM) as well as CDK2, JNK2, IKK2, MSK1, and MSK2[1].

[Related Catalog]:

Signaling Pathways >> MAPK/ERK Pathway >> MAPKAPK2 (MK2)
Research Areas >> Inflammation/Immunology

[Target]

IC50: 0.85 nM (MK-2), 0.21 μM (MK-3), 0.081 μM (MK-5), 3.44 μM (ERK2), 5.7 μM (MNK1)[1]


[In Vitro]

MK-2 Inhibitor III suppresses TNFα production in U397 cells with an IC50 of 4.4 μM[1].

[References]

[1]. Anderson DR, et al. Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). J Med Chem. 2007 May 31;50(11):2647-54.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H18N4O2

[ Molecular Weight ]:
358.393

[ Exact Mass ]:
358.142975

Safety Information

[ Hazard Codes ]:
Xi


Related Compounds