PF-00356231 hydrochloride 是一种非肽、非锌螯合的基质金属蛋白酶 MMP-12 的配体和抑制剂 (IC50=1.4 μM)。它对 MMP-12 具有特异性并形成 PF-00356231/MMP-12 复合体。PF-00356231 hydrochloride 对 MMP-13、MMP-8、MMP-9、MMP-3 有抑制作用，IC50 分别为 0.00065、1.7、0.98、0.39 μM。
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].
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.
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