Description
(S)-
MG115 is a potent and reversible proteasome inhibitor, targeting the chymotryptic site on the 20S particle (K
i = 21 nM). It reduces the degradation of ubiquitin-
conjugated proteins in extracts. (S)-
MG115 also blocks the degradation of long-
and short-
lived proteins in intact cells as well as the proteolytic generation of diverse proteins, including NF-
κB, antigens, and p53. Proteasome inhibitors, including (S)-
MG115, can induce a heat shock response and apoptosis, particularly in cancer cells.
Uses
(S)-MG115 is a potent and reversible proteasome inhibitor, targeting the chymotryptic site on the 20S particle (Ki = 21 nM). It reduces the degradation of ubiquitin-conjugated proteins in extracts. (S)-MG115 also blocks the degradation of long- and short-lived proteins in intact cells as well as the proteolytic generation of diverse proteins, including NF-κB, antigens, and p53. Proteasome inhibitors, including (S)-MG115, can induce a heat shock response and apoptosis, particularly in cancer cells.[Cayman Chemical]
Uses
MG-115 is a compound that inhibits the chymotrypsin-like activity of the proteasome.
Definition
ChEBI: N-[(2S)-4-methyl-1-[[(2S)-4-methyl-1-oxo-1-[[(2S)-1-oxopentan-2-yl]amino]pentan-2-yl]amino]-1-oxopentan-2-yl]carbamic acid (phenylmethyl) ester is a peptide.
General Description
Potent reversible proteasome inhibitor (K
i = 21 nM and 35 nM for 20S and 26S proteasome, respectively).
Biochem/physiol Actions
Product does not compete with ATP.
References
1. involvement of heat shock protein 90 in the degradation of mutant insulin receptors by the proteasome. imamura, t., haruta, t., takata, y., usui, i., iwata, m., ishihara, h., ishiki, m., ishibashi, o., ueno, e., sasaoka, t., kobayashi, m. j. biol. chem. (1998)
