219465
Celastrol, Celastrus scandens
A cell-permeable dienone-phenolic triterpene compound that exhibits antioxidant and anti-inflammatory properties.
别名:
Celastrol, Celastrus scandens , Tripterin, 3-Hydroxy-24-nor-2-oxo-1(10),3,5,7-friedelatetraen-29-oic Acid, Proteasome Inhibitor XIX
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关于此项目
经验公式（希尔记法）:
C29H38O4
化学文摘社编号:
分子量:
450.61
NACRES:
NA.77
UNSPSC Code:
12352200
MDL number:
Assay:
≥95% (TLC)
Form:
crystals
Storage condition:
OK to freeze, protect from light
Quality Segment
assay
≥95% (TLC)
form
crystals
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
red
solubility
DMSO: 5 mg/mL, ethanol: soluble
shipped in
ambient
storage temp.
2-8°C
InChI
1S/C29H38O4/c1-17-18-7-8-21-27(4,19(18)15-20(30)23(17)31)12-14-29(6)22-16-26(3,24(32)33)10-9-25(22,2)11-13-28(21,29)5/h7-8,15,22,31H,9-14,16H2,1-6H3,(H,32,33)/t22-,25-,26-,27+,28-,29+/m1/s1
InChI key
KQJSQWZMSAGSHN-JJWQIEBTSA-N
General description
A cell-permeable dienone-phenolic triterpene compound that exhibits antioxidant and anti-inflammatory properties. It suppresses LPS-induced pro-inflammatory cytokines release in macrophages and monocytes (IC50 = 40 nM for IL-1β and IL-1α, 80 nM for IL-6, 110 nM for PGE2, and 210 nM for IL-8 and TNF-α), as well as LPS-induced NF-κB activation (IC50 = 270 nM) and NO production (IC50 = 230 nM) in RAW264.7 cells. Preferentially inhibits chymotrypsin-like activity of 20S proteasome with an IC50 of 2.5 µM. Has also been shown to inhibit lipid peroxidation induced by ADP and Fe2+ in rat liver mitochondria (IC50 = 7 µM). Significantly improves the performance in memory, learning, and psychomotor activity in rats. May be useful to minimize inflammation in Alzheimer′s disease (AD).
Biochem/physiol Actions
Cell permeable: yes
Product does not compete with ATP.
Reversible: no
Target IC50: 2.5 µM inhibiting chymotrypsin-like activity of 20S proteasome
Packaging
Packaged under inert gas
Other Notes
Yang, H., et al. 2006. Cancer Res.66, 4758.
Westerheide, S.D., et al. 2004. J. Biol. Chem.279, 56053.
Jin, H.Z., et al. 2002. J. Nat. Prod.65, 89.
Allison, A.C., et al. 2001. Prog. Neuropsychopharmacol. Biol. Psychiatry25, 1341.
He, W., et al. 1998. Bioorg. Med. Chem. Lett.8, 3659.
Sassa, H., et al. 1990. Biochem. Biophys. Res. Commun.172, 890.
Westerheide, S.D., et al. 2004. J. Biol. Chem.279, 56053.
Jin, H.Z., et al. 2002. J. Nat. Prod.65, 89.
Allison, A.C., et al. 2001. Prog. Neuropsychopharmacol. Biol. Psychiatry25, 1341.
He, W., et al. 1998. Bioorg. Med. Chem. Lett.8, 3659.
Sassa, H., et al. 1990. Biochem. Biophys. Res. Commun.172, 890.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
怎么回事？
WGK 2
闪点 (F)
Not applicable
闪点 (°C)
Not applicable