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Merck
CN

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
Quality level:
Storage condition:
OK to freeze, protect from light
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Quality Level

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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)


存储类别

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable



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