UK 356618 (Compound 4j) is a potent and selective inhibitor ofmatrix metalloprotease-3 (MMP-3)with anIC₅₀of 5.9 nM. UK 356618 is less potent againstMMP-1,MMP-2,MMP-9,MMP-13andMMP-14compared withMMP-3^[1].

Inhibition of MMP-3 and selectivity over MMP-2 was remarkably sensitive to the size of the substituent and is clearly optimal for a methyl group (UK 356618, compound 4j). UK 356618 is more widely profiled against other MMPs^[1].
MMP-13 is closely involved in IL-6 or TNF-α increasing tumor metastasis. MMP-13 deficiency abrogate TNF-α effect on lung cancer cell migration. UK 356618 treatment efficiently abolished the effect of TNF-α on cell migration in NCI-H446 cells^[2].

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].

557.72

Solid

C₃₄H₄₃N₃O₄

230961-08-7

Room temperature in continental US; may vary elsewhere.

DMSO : 25 mg/mL(44.83 mM;Need ultrasonic and warming)

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