MK2-IN-3

Modify Date: 2024-04-06 19:10:29

MK2-IN-3 Structure
MK2-IN-3 structure
Common Name MK2-IN-3
CAS Number 724711-21-1 Molecular Weight 340.37800
Density N/A Boiling Point N/A
Molecular Formula C21H16N4O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of MK2-IN-3


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].

 Names

Name 2-(2-quinolin-3-ylpyridin-4-yl)-1,5,6,7-tetrahydropyrrolo[3,2-c]pyridin-4-one
Synonym More Synonyms

 MK2-IN-3 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
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

 Synonyms

Kinome_3179
2jbp
Pyrrolopyridine,16
2jbo
3fhr
P4O
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