tcsc1701 Ilomastat

Ilomastat (Galardin; GM6001) is a broad spectrum matrix metalloprotease (MMP) inhibitor, with K_i of 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM, 0.36 nM for MMP-1/2/3/7/8/9/12/14/26, respectively.

IC50 & Target: Ki: 0.4 nM (MMP-1), 0.5 nM (MMP-2), 27 nM (MMP-3), 3.7 nM (MMP-7), 0.1 nM (MMP-8), 0.2 nM (MMP-9), 3.6 nM (MMP-12), 13.4 nM (MMP-14), 0.36 nM (MMP-26)

In Vitro: Ilomastat (GM6001) inhibits human skin fibroblast collagenase with K_i of 0.4 nM when assayed with a synthetic thio ester substrate at pH 6.5, with 50-fold selectivity over two bacterial enzymes, thermolysin and Pseudomonas aeruginosa elastase^[1]. Ilomastat (0.1 nM-10 nM) inhibits gelatinase A and gelatinase B produced by T-cells, and thus inhibits T-cell homing^[4].

In Vivo: Ilomastat (GM6001) (400 μg/mL) prevents corneal ulceration after severe alkali injury^[2]. Ilomastat (GM6001) significantly inhibits intimal hyperplasia and intimalcollagen content, and it increases lumen area in stented arteries without effects on proliferation rates in rabbit model after stenting^[3].