530070

Pristimerin

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

• Sinonimo/i: Pristimerin, Monoacylglycerol Lipase Inhibitor II, Proteasome Inhibitor XV, NF-κB Activation Inhibitor IX, MAGL Inhibitor II
• Formula empirica (notazione di Hill): C₃₀H₄₀O₄
• Numero CAS: 1258-84-0
• Peso molecolare: 464.64
• Numero MDL: MFCD01711331
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: red
• Solubilità: DMSO: 10 mg/mL; ethanol: 2.5 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 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; JFACETXYABVHFD-WXPPGMDDSA-N

Descrizione

Descrizione generale

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).

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable