1138549-36-6

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CX-5461/CX5461/

1138549-36-6

Cat.No.ABP000959 Chemical NameCX-5461/CX5461/ MolFormulaC27H27N7O2S MolWeight513.614 Purity >99%

Chemical Name : CX-5461/CX5461/

CAS : 1138549-36-6

Synonyms: 2-(4-methyl-1,4-diazepan-1-yl)-N-[(5-methylpyrazin-2-yl)methyl]-5-oxo-[1,3]benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxamide

Storage:at -20℃ 2 years

Biologieal

MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50 of 0.1 and 1.2 μM for the inhibition of proteasome and calpain, respectively. The Ki of MG132  is 4 nM. MG132 inhibits TNF-α-induced NF-κB activation and IκBα degradation with an IC50 of 3 µM and prevents β-secretase cleavage. MG132  induces neurite outgrowth in PC12 cells and has anticancer properties in vitro. MG132  reduces the degradation of ubiquitin-conjugated proteins in mammalian cells and permeable strains of yeast by the 26S complex without affecting its ATPase or isopeptidase activities. MG132 activates c-Jun N-terminal kinase (JNK1), which initiates apoptosis. [1][2][3]

Reference

[1] http://en.wikipedia.org/wiki/MG132

[2] Steinhilb ML et al. J Biol Chem. 2001 Feb 9;276(6):4476-84.

[3] Tsubuki S et al. J Biochem. 1996 Mar;119(3):572-6. 

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