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MK2-IN-3

Names

[ CAS No. ]:
724711-21-1

[ Name ]:
MK2-IN-3

[Synonym ]:
Kinome_3179
2jbp
Pyrrolopyridine,16
2jbo
3fhr
P4O

Biological Activity

[Description]:

MK2-IN-3 is a potent and selective inhibitor of MAPKAP-K2 (MK-2), with an IC50 of 8.5 nM. MK2-IN-3 shows selectivity for MK-2 over MK-3, MK-5, ERK2, MNK1, p38a (IC50s=0.21, 0.081, 3.44, 5.7, and >100 μM, respectively) and MSK1, MSK2, CDK2, JNK2, IKK2 (IC50s>200 μM). MK2-IN-3 can reduce TNFα production in both U937 cells and in vivo[1].

[Related Catalog]:

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

[Target]

IC50: 8.5 nM (MK-2); 81 nM (MK-5); 210 nM (MK-3); 3.44 μM (ERK2); 5.7 μM (MNK1)[1]


[In Vitro]

MK2-IN-3 (compound 16) inhibits MK-2 and TNFα production in U937 cells, with IC50s of 8.5 nM and 4.4 μM, respectively[1].

[In Vivo]

MK2-IN-3 (compound 16) (20 mg/kg; a single p.o. before LPS challenge) inhibits 20% TNFα production in rat LPS (rLPS) model[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 ]:
C21H16N4O

[ Molecular Weight ]:
340.37800

[ Exact Mass ]:
340.13200

[ PSA ]:
74.16000

[ LogP ]:
3.58820

[ Storage condition ]:
2-8°C

Related Compounds