530070

Pristimerin

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

• Sinônimo(s): Pristimerin, Monoacylglycerol Lipase Inhibitor II, Proteasome Inhibitor XV, NF-κB Activation Inhibitor IX, MAGL Inhibitor II
• Fórmula empírica (Notação de Hill): C₃₀H₄₀O₄
• Número CAS: 1258-84-0
• Peso molecular: 464.64
• Número MDL: MFCD01711331
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: red
• solubilidade: DMSO: 10 mg/mL; ethanol: 2.5 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 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
• chave InChI: JFACETXYABVHFD-WXPPGMDDSA-N

Descrição

Descrição geral

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).

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Outras notas

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.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable