PF-00356231 hydrochloride

PF-00356231 hydrochloride is a specific, non-peptidic, non-zinc chelating ligand and inhibitor of matrix metalloproteinase MMP-12 (IC50=1.4 μM). PF-00356231 hydrochloride binds to MMP-12 and forms PF-00356231/MMP-12 complex. PF-00356231 hydrochloride shows potency against MMP-13, MMP-8, MMP-9, MMP-3 with IC50s of 0.00065, 1.7, 0.98, 0.39 μM, respectively[1].

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Metabolic Enzyme/Protease >> MMP

MMP-12:1.4 μM (IC50)

MMP13:0.65 nM (IC50)

MMP-3:0.39 μM (IC50)

MMP-8:1.7 μM (IC50)

MMP-9:0.98 μM (IC50)

PF-00356231 hydrochloride against MMP-12/13 can be affected significantly by the presence of acetohydroxamate (AH). PF-00356231 hydrochloride decreases the IC50 values of MMP-12 (0.014 μM) and MMP-13 (0.27 μM) in the presence AH[1].

[1]. Morales R, et al. Crystal structures of novel non-peptidic, non-zinc chelating inhibitors bound to MMP-12. J Mol Biol. 2004 Aug 20;341(4):1063-76.