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.

Product information

CAS Number: 724711-21-1

Molecular Weight: 340.38

Formula: C21H16N4O

Chemical Name: 2-[2-(quinolin-3-yl)pyridin-4-yl]-1H, 4H, 5H, 6H, 7H-pyrrolo[3, 2-c]pyridin-4-one

Smiles: O=C1NCCC2NC(=CC=21)C1=CC(=NC=C1)C1=CC2=CC=CC=C2N=C1

InChiKey: OWFLADWRSCINST-UHFFFAOYSA-N

InChi: InChI=1S/C21H16N4O/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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 62.5 mg/mL (183.62 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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.

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.

Products are for research use only. Not for human use.