Potent and selective inhibitor of matrix metalloprotease-3 (MMP-3) (IC50 = 5.9 nM). Displays selectivity over a range of MMPs (IC50 values are 73, 840, 1790, 1900 and 51000 for MMP-13, MMP-9, MMP-2, MMP-14 and MMP-1 respectively).
ChEBI: (2R)-N-[(2S)-3,3-dimethyl-1-oxo-1-[[(1R)-1-phenylethyl]amino]butan-2-yl]-N'-hydroxy-2-[3-(3-methyl-4-phenylphenyl)propyl]butanediamide is a secondary carboxamide.
UK 356618 has the potential to inhibit interleukin (IL)-6-induced cell migration in NCI H446 small cell lung cancer cells in vitro.', 'UK-356,618 is a potent, selective inhibitor of Matrix metalloproteinase MMP3 (stromelysin-1). MMP-3 IC50 = 5.9 nM, selectivity is 140-fold vs MMP-1, -2, -9, and -14.
UK 356618 (15 mg/kg; intravenous injection; for 24 h or 7 days; male Wistar rats) treatment at reperfusion significantly reduces MMP3 activity in the brain[3].
| Animal Model: | Hyperglycemic male Wistar rats injected with middle cerebral artery occlusion (MCAO)[3] |
| Dosage: | 15 mg/kg |
| Administration: | Intravenous injection; for 24 h or 7 days |
| Result: | Significantly reduced MMP3 activity in the brain.
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MMP-3: 5.9 nM (IC50); MMP-13: 73 nM (IC50); MMP-9: 0.84 μM (IC50); MMP-2: 1.79 μM (IC50); MMP-14: 1.9 μM (IC50); MMP-1: 51 μM (IC50)