Celastrol
Proteasome inhibitor / Displays potent antioxidant and anti-inflammatory activity. Inhibits NFκB (IC50=270 nM). It induces heat shock response and cytoprotection in various cells. Inhibits 20S proteasome chymotrypsin activity (IC50=2.5 μM). Induces autophagy by targeting AR/miR-101 in prostate cancer cells.4 Induces UPR-dependent cell death in cancer cells.5 Cell permeable.
Biochemicals & reagents
34157-83-0
1) Sethi et al. (2007), Celastrol, a novel triterpene, potentiates TNF-induced apoptosis and suppresses invasion of tumor cells by inhibiting NF-kappaC-regulated gene products and TAK1-mediated NF-kappaB activation ; Blood, 109 2727 2) Westerheide et al. (2004), Celastrols as inducers of the heat shock response and cytoprotection; J. Biol. Chem., 279 56053 3) Yang et al. (2006), Celastrol, a triterpene extracted from the Chinese “Thunder of God Vine” is a potent proteasome inhibitor and suppresses human prostate cancer cell growth in nude mice; Cancer Res., 66 4758 4) Guo et al. (2015), Celastrol Induces Autophagy by Targeting AR/miR-101 in Prostate Cancer Cells; PLoS One, 10(10) e0140745 5) Fribley et al. (2015), Celastrol induces unfolded protein response-dependent cell death in head and neck cancer; Exp. Cell Res., 330 412
-20°C
TARGET: Proteasome; Antioxidant; UPR (Unfolded protein response) -- PATHWAY: Degradation; Autophagy; NFkappaB; Redox; Cell migration; Cytokine -- RESEARCH AREA: Ubiquitin/Proteasome; Cell death; Neuroscience -- DISEASE AREA: Cancer; InflammationNeurodegeneration