Chemical Name |
MG-101 |
CAS Number |
110044-82-1 |
MDL Number |
MFCD00065505 |
Molecular Formula |
C20H37N3O4 |
Molecular Weight |
383.53 |
Synonyms |
Calpain inhibitor I;Ac-LLnL-CHO;ALLN |
Introduction of 110044-82-1 :
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]
Purity |
NLT 98% |
Storage |
at 20ºC 2 years |
*The above information is for reference only.