A cell-permeable dienone-phenolic triterpene compound that exhibits antioxidant and anti-inflammatory properties. It suppresses LPS-induced pro-inflammatory cytokines release in macrophages and monocytes (IC50 = 40 nM for IL-1β and IL-1α, 80 nM for IL-6, 110 nM for PGE2, and 210 nM for IL-8 and TNF-α), as well as LPS-induced NF-κB activation (IC50 = 270 nM) and NO production (IC50 = 230 nM) in RAW264.7 cells. Preferentially inhibits chymotrypsin-like activity of 20S proteasome with an IC50 of 2.5 µM. Has also been shown to inhibit lipid peroxidation induced by ADP and Fe2+ in rat liver mitochondria (IC50 = 7 µM). Significantly improves the performance in memory, learning, and psychomotor activity in rats. May be useful to minimize inflammation in Alzheimer′s disease (AD).
生化／生理作用
Cell permeable: yes
Product does not compete with ATP.
Reversible: no
Target IC50: 2.5 µM inhibiting chymotrypsin-like activity of 20S proteasome
包裝
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
其他說明
Yang, H., et al. 2006. Cancer Res.66, 4758. Westerheide, S.D., et al. 2004. J. Biol. Chem.279, 56053. Jin, H.Z., et al. 2002. J. Nat. Prod.65, 89. Allison, A.C., et al. 2001. Prog. Neuropsychopharmacol. Biol. Psychiatry25, 1341. He, W., et al. 1998. Bioorg. Med. Chem. Lett.8, 3659. Sassa, H., et al. 1990. Biochem. Biophys. Res. Commun.172, 890.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
The Journal of biological chemistry, 293(38), 14758-14774 (2018-08-11)
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Select different protease inhibitor types based on your needs to prevent protein degradation during isolation and characterization and safeguard proteins in sample prep.
