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MG-101 CAS: 110044-82-1

Category: Inhibitors
Product Name: MG-101
Cat No: I000413
CAS No: 110044-82-1
Synonyms: 2-acetamido-4-methyl-N-[4-methyl-1-oxo-1-(1-oxohexan-2-ylamino)pentan-2-yl]pentanamide
Molecular Formula: C20H37N3O4
Molecular Weight: 383.5
InChI: None
Solubility: 10 mM in DMSO
Target: Calpains
IC50: 150 nM (Ki)
Storage: Store at -20°C
CAS 110044-82-1,MG-101
  • Description

MG-101 is a potent inhibitor of cysteine proteases including calpain I (Ki = 190 nM), calpain II (Ki = 220 nM), cathepsin B (Ki = 150 nM), and cathepsin L (Ki = 500 pM).
IC50 value: 150 nM (Ki)
Target: cysteine protease
in vitro: MG-101 is a calpain inhibitor (IC50 = 0.09 μM) that activates p53-dependent apoptosis in tumor cell lines. At 10-100 μM MG-101 dose-dependently prevents the degradation of IκBα and IκBβ by the ubiquitin-proteasome complex, which blocks activation of NFκB and the production of TNF and IL-1β, suggesting a potential therapeutic effect for inflammatory diseases.2 At 10 μM, MG-101 can inhibit nitric oxide production by activated macrophages by interfering with transcription of the inducible nitric oxide synthase gene. In HCT116 cells, MG-101 decreases cell viability and tumor growth, and induces apoptosis response through Bax translocation from cytosol to mitochondria. [1]
in vivo: In mice bearing HCT116 xenografts, MG-101 (10 mg/kg i.p.) inhibits colon tumor formation. [1]

  • Spec

Appearance:white solid powder
Purity: > 98%

  • References

[1]. Li SZ, et al. ALLN hinders HCT116 tumor growth through Bax-dependent apoptosis. Biochem Biophys Res Commun. 2013 Jul 26;437(2):325-330.

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