(S)-MG115

(S)-MG115 is a potent and reversible proteasome inhibitor, targeting the chymotryptic site on the 20S particle (K_i = 21 nM).¹ It reduces the degradation of ubiquitin-conjugated proteins in extracts.¹ (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.^1,2,3 Proteasome inhibitors, including (S)-MG115, can induce a heat shock response and apoptosis, particularly in cancer cells.^3,4,5

WARNING This product is not for human or veterinary use.

1. Rock, K.L., Gramm, C., Rothstein, L., et al. Inhibitors of the proteasome block the degradation of most cell proteins and the generation of peptides presented on MHC class I molecules. Cell 78(5), 761-771 (1994).

2. Palombella, V.J., Rando, O.J., Goldberg, A.L., et al. The ubiquitin-proteasome pathway is required for processing the NF-κB₁ precursor protein and the activation of NF-κB. Cell 78(5), 773-785 (1994).

3. Lopes, U.G., Erhardt, P., Yao, R., et al. p53-dependent induction of apoptosis by proteasome inhibitors. The Journal of Biological Chemisty 272(20), 12893-12896 (1997).

4. Bush, K.T., Goldberg, A.L., and Nigam, S.K. Proteasome inhibition leads to a heat-shock response, induction of endoplasmic reticulum chaperones, and thermotolerance. The Journal of Biological Chemisty 272(14), 9086-9092 (1997).

5. Gartel, A.L. A new target for proteasome inhibitors: FoxM1. Expert Opin. Investig. Drugs 19(2), 235-242 (2010).