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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 |
| Related Proteasome Products |
|---|
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Bortezomib (PS-341) is a highly selective proteasome inhibitor with a ki value of 6nM. |
| CTP-518
CTP-518 is a novel HIV protease inhibitor. CTP-518 has the potential to be the first HIV protease inhibitor toeliminate the need to co-dose with a boosting agent. |
| ITMN-191
ITMN-191 (Danoprevir, RG7227) is a potent and orally active inhibitor of hepatitis C virus (HCV) NS3/4A serine protease with an IC50 of 1.6 nM. |
| MG132
MG132 is a specific and potent cell-permeable proteasome inhibitor (IC50 = 100 nM, Ki = 4 nM). MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132 is also a calpain inhibitor with IC50 of 1.2 μM. |
| IU1
IU1 is a reversible, small molecule inhibitor of deubiquitination by USP14 that demonstrates an IC50 value of 4-5 μM. |
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