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MG-101

Cat. No. M5221

MG-101 Structure

Synonym: Calpain inhibitor-1

Size Price Availability Quantity
5mg USD 87 In stock
10mg USD 135 In stock
50mg USD 450 In stock
100mg USD 723 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 383.53
Formula C20H37N3O4
CAS Number 110044-82-1
Purity >99%
Solubility 76mg/ml in DMSO
Storage at -20°C
References

ALLN hinders HCT116 tumor growth through Bax-dependent apoptosis.
Li SZ, et al. Biochem Biophys Res Commun. 2013 Jul 26;437(2):325-30. PMID: 23831472.

Cysteine proteinase inhibitors and ras gene products share the same biological activities including transforming activity toward NIH3T3 mouse fibroblasts and the differentiation-inducing activity toward PC12 rat pheochromocytoma cells.
Hiwasa, et al. Carcinogenesis. 1990 Jan;11(1):75-80. PMID: 2403861.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MG-101, Calpain inhibitor-1 supplier, Proteasome, inhibitors

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