Pristimerin – CAS 1258-84-0 – Calbiochem

Descrição detalhada : 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-kappaB 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).
Sinónimos : Pristimerin - CAS 1258-84-0 - Calbiochem; Monoacylglycerol Lipase Inhibitor II, Proteasome Inhibitor XV, NF-kappaB Activation Inhibitor IX, MAGL Inhibitor II
Fórmula molecula r: C30H40O4
Armazenamento : 2-8C; 2-8C; 2-8C
Embalagem : 1X5MG