530070

Pristimerin

A cell-permeable plant dienone-phenolic triterpenoid, naturally isolated from tripterygium wilfordii.

• Synonyme(s) : Pristimerin, Monoacylglycerol Lipase Inhibitor II, Proteasome Inhibitor XV, NF-κB Activation Inhibitor IX, MAGL Inhibitor II
• Formule empirique (notation de Hill): C₃₀H₄₀O₄
• Numéro CAS: 1258-84-0
• Poids moléculaire : 464.64
• Numéro MDL: MFCD01711331
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: red
• Solubilité: DMSO: 10 mg/mL; ethanol: 2.5 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• InChI: 1S/C30H40O4/c1-18-19-8-9-22-28(4,20(19)16-21(31)24(18)32)13-15-30(6)23-17-27(3,25(33)34-7)11-10-26(23,2)12-14-29(22,30)5/h8-9,16,23,32H,10-15,17H2,1-7H3/t23-,26-,27-,28+,29-,30+/m1/s1
• Clé InChI: JFACETXYABVHFD-WXPPGMDDSA-N

Description

Description générale

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).

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable