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Merck

530070

Pristimerin

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

別名:

Pristimerin, Monoacylglycerol Lipase Inhibitor II, Proteasome Inhibitor XV, NF-κB Activation Inhibitor IX, MAGL Inhibitor II

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この商品について

実験式(ヒル表記法):
C30H40O4
CAS番号:
分子量:
464.64
NACRES:
NA.77
UNSPSC Code:
12352200
MDL number:
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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Quality Segment

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

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

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).

Packaging

Packaged under inert gas

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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)


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保管分類

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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