General description

A cell-permeable plant dienone-phenolic triterpenoid, naturally isolated from tripterygium wilfordii, whose inhibitory activities against proteasome chymotrypsin subunit (IC₅₀ = 2.2 and 3.0 µM against purified rabbit 20S and human 26S proteasome, respectively) and cellular NF-κB pathway/IKK activation most likely account for its reported anticancer efficacy both in vitro (IC₅₀ ≤610 nM in A549, K562, KBM5, MCF-7, MDA-MB-231, HepG2, and primary human leukemia cell cultures) and in mice in vivo (1 to 2.5 mg/kg/day, s.c.), including imatinib/STI571-resistant cancer cells harboring Bcr-Abl T315I mutation. Also reported to inhibit the activity of monoacylglycerol lipase (MGL), the enzyme that hydrolyzes and deactivates the cannabionoid receptor ligand 2-Arachidonoyl-sn-glycerol (2-AG), in a reversible manner with high potency (IC₅₀ = 93 nM).

Legal Information

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

Other Notes

Lu, Z., et al. 2010. Mol. Cancer9, 112.King, A.R., et al. 2009. Chem. Biol.16, 1045.Tiedemann, R.E., et al. 2009. Blood113, 4027.Yang, H., et al. 2008. J. Cell. Biochem.103, 234.Wu, C.C., et al. 2005. Mol. Cancer Ther.4, 1277.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Warning

Toxicity: Standard Handling (A)