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  • Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).

Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).

Bioorganic & medicinal chemistry (2009-04-15)
Frank Lovering, Steve Kirincich, Weiheng Wang, Kerry Combs, Lynn Resnick, Joan E Sabalski, John Butera, Julie Liu, Kevin Parris, J B Telliez
ABSTRACT

A novel series of inhibitors for mitogen activated protein kinase-activated protein kinase 2 (MK-2) are reported. These squarate based inhibitors were identified via a high-throughput screen. An MK2 co-structure with the starting ligand was obtained and a structure based approach was followed to optimize potency and selectivity.

MATERIALS
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Product Description

Sigma-Aldrich
3,4-Dihydroxy-3-cyclobutene-1,2-dione, ≥99.0% (HPLC)