Ilomastat (GM6001, Galardin)
Molecular Weight(MW): 388.46
Ilomastat (GM6001, Galardin) is a broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with Ki 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, respectively.
3 Customer Reviews
ARPE-19 cells were seeded on Millicell inserts for growth to form the monolayer. Monolayers were treated with or without recombinant HIV-1 gp120 glycoprotein during the last 2 days of cell culture. Some samples were pretreated with anti-DC-SIGN antibodies or GM6001 before incubation with gp120. A, the TEER value was measured. B, the paracellular permeability for FITC-dextran flux was assessed. Date represent mean ± S.D. *, p < 0.05; **, p < 0.01; ***, p < 0.001. Ω, ohm.
J Biol Chem, 2016, 291(44):22977-22987. Ilomastat (GM6001, Galardin) purchased from Selleck.
Effect of the broad spectrum hydroxamate inhibitors batimastat and ilomastat on a disintegrin and metalloproteinase with thombospondin type 1 motifs (ADAMTS) 13 and ADAMTS15. (A) While batimastat is a good inhibitor against ADAMTS15, ilomastat has no ability to inhibit the enzyme. ADAMTS15 (20 nM) was pre-incubated with two doses (300 nM or 3 µM) of batimastat and ilomastat prior to the addition of aggrecan substrate G1-IGD-G2. The inhibitory effect of batimastat can be clearly discerned from the undigested 130 kDa G1-IGD-G2 bands.
Biomed Rep, 2016, 4(1):73-78. . Ilomastat (GM6001, Galardin) purchased from Selleck.
Purity & Quality Control
Choose Selective MMP Inhibitors
|Description||Ilomastat (GM6001, Galardin) is a broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with Ki 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, respectively.|
GM6001 inhibits human skin fibroblast collagenase with Ki 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.  GM 6001 (0.1 nM - 10 nM) inhibits gelatinase A and gelatinase B produced by T-cells, thus inhibits T-cell homing. 
|In vivo||Topical application of GM6001 (400 μg/ml) prevents corneal ulceration after severe alkali injury.  In rabbit model after stenting, GM6001 significantly inhibits intimal hyperplasia and intimalcollagen content, and it increases lumen area in stented arteries without effects on proliferation rates. |
|In vitro||DMSO||78 mg/mL (200.79 mM)|
|Ethanol||8 mg/mL warmed (20.59 mM)|
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