GM6001 is a broad spectrum matrix metalloprotease (MMP) inhibitor with Ki values of 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM and 0.36 nM for MMPs -1, -2, -3, -7, -8, -9, -12, -14 and -26, respectively. Galardin (GM6001) reduces infarct volume following middle cerebral artery occlusion in an ischemic mouse model. GM6001 also inhibits human skin fibroblast collagenase (Ki = 0.4 nM). GM6001 (Galardin) treatment also inhibited extracellular signal-regulated kinase (ERK) activation induced by bombesin or LPA. In addition, GM6001 inhibited bombesin- or LPA-induced DNA synthesis in a dose dependent manner, when stimulated by increasing concentrations of bombesin, and when added after bombesin stimulation.
Elife. 2020 Sep 28;9:e56006.
The dynamic interplay between ATP/ADP levels and autophagy sustain neuronal migration in vivo
GM6001 purchased from AbMole
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Source | Oncotarget (2017). Figure 3. GM6001 |
| Method | RT-PCR | |
| Cell Lines | SCC-9 cells | |
| Concentrations | 10 μM | |
| Incubation Time | 24 h | |
| Results | Suppression of MMP-9 expression by MMP-9 shRNA or GM6001 resulted in a significant reduction of the migration and invasion of CAIX-overexpressing SCC-9 cells |
| Molecular Weight | 388.46 |
| Formula | C20H28N4O4 |
| CAS Number | 142880-36-2 |
| Solubility (25°C) | DMSO 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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