MG-101 is an inhibitor of Calpain 1 (Ki = 190 nM), Calpain 2 (Ki = 220 nM), cathepsin B (Ki = 150 nM), and cathepsin L (Ki = 500 pM). It inhibits neutral cysteine proteases and proteasome (Ki = 6 μM). It inhibits apoptosis in thymocytes and metamyelocytes. MG-101 also inhibits cell cycle progression at the G1/S border and metaphase/anaphase in CHO cells by inhibiting cyclin B degradation. MG-101 inhibits the proteolysis of IκBα and IκBβ by the ubiquitin-proteasome complex. Furthermore, it protects against neuronal damage caused by hypoxia and ischemia. MG-101 also prevents nitric oxide production by activated macrophages by interfering with transcription of the inducible nitric oxide synthase gene.
| Cell Experiment | |
|---|---|
| Cell lines | HCT116，HCT116/p53−/−，和 HCT116/Bax−/− |
| Preparation method | Cells viability is assayed using Cell Counting Kit-8 following manufacturer’s protocol. All HCT116 cell typesare seeded into each well of 96-well plate, cultured to 80% density and treated with different doses of ALLN for 24 h. Medium is then replaced by 100 μl fresh McCoy’s 5A complete medium with 10% CCK-8 reagent and incubated for 1 h. Absorbance is measured at 450 nm using a microplate reader. Results are shown as death percentages. |
| Concentrations | ~26 μM |
| Incubation time | 24h |
| Animal Experiment | |
|---|---|
| Animal models | Female athymic nude mice bearing HCT116 xenografts |
| Formulation | Saline |
| Dosages | 10 mg/kg |
| Administration | i.p. |
| Molecular Weight | 383.53 |
| Formula | C20H37N3O4 |
| CAS Number | 110044-82-1 |
| Solubility (25°C) | DMSO 75 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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| Ac-WLA-AMC
Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate. |
| Ac-Nle-Pro-Nle-Asp-AMC
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PSI (Proteasome Inhibitor 1) is a potent proteasome inhibitor. |
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