UK-370106 is a potent and highly selective inhibitor of MMP-3 with IC50 of 23 nM and MMP-12 with IC50 of 42 nM, and potently inhibits cleavage of [3H]-fibronectin by MMP-3 (IC50: 320 nM).

MMP7:5.8 μM, MMP13:2.3 μM, MMP9:30.4 μM, MMP2:34.2 μM, MMP12:42 nM, MMP8:1.75 μM, MMP3:23 nM, MMP14:66.9 μM

UK-370106 potency for the inhibition of MMP-13 is 2.3 μM, some 100-fold less potent than its inhibition of MMP-3. UK-370106 is found to be inactive (IC50 > 100 μM) vs zinc metalloproteases PCP and TACE and possesses the following inhibitory potencies vs MMP-2 (IC50 of 34.2 μM), MMP-7 (IC50 of 5.8 μM), MMP-8 (IC50 of 1.75 μM), MMP-9 (IC50 of 30.4 μM) and MMP-14 (IC50 of 66.9 μM)[1]. UK-370106 potently inhibits cleavage of [3H]-fibronectin by MMP-3 (IC50 of 320 nM)[1].

Following iv (rat; 2 mg/kg) or topical administration to dermal wounds (rabbit), UK-370106 (compound 7) is cleared rapidly (t1/2 = 23 min) from plasma, but slowly (t1/2 approximately 3 days) from dermal tissue. Topical administration of UK-370106 for 6 days substantially inhibits MMP-3 ex vivo in a model of chronic dermal ulcers [1].