530070
Pristimerin
A cell-permeable plant dienone-phenolic triterpenoid, naturally isolated from tripterygium wilfordii.
别名:
Pristimerin, Monoacylglycerol Lipase Inhibitor II, Proteasome Inhibitor XV, NF-κB Activation Inhibitor IX, MAGL Inhibitor II
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关于此项目
经验公式（希尔记法）:
C30H40O4
化学文摘社编号:
分子量:
464.64
NACRES:
NA.77
UNSPSC Code:
12352200
MDL number:
产品名称
Pristimerin, A cell-permeable plant dienone-phenolic triterpenoid, naturally isolated from tripterygium wilfordii.
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
InChI key
JFACETXYABVHFD-WXPPGMDDSA-N
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
red
solubility
DMSO: 10 mg/mL
ethanol: 2.5 mg/mL
shipped in
ambient
storage temp.
2-8°C
Quality Level
Disclaimer
Toxicity: Standard Handling (A)
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).
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.
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
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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