Celastrol, Celastrus scandens

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).

Cell permeable: yes

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 2.5 µM inhibiting chymotrypsin-like activity of 20S proteasome

Packaged under inert gas

Yang, H., et al. 2006. Cancer Res.66, 4758.
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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.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)