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Celastrol, Celastrus scandens

A cell-permeable dienone-phenolic triterpene compound that exhibits antioxidant and anti-inflammatory properties.

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Synonym(s):
Celastrol, Celastrus scandens , Tripterin, 3-Hydroxy-24-nor-2-oxo-1(10),3,5,7-friedelatetraen-29-oic Acid, Proteasome Inhibitor XIX
Empirical Formula (Hill Notation):
C29H38O4
CAS Number:
Molecular Weight:
450.61
MDL number:

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

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This Item
C0869523310529685
Celastrol ≥98% (HPLC), solid

Sigma-Aldrich

C0869

Celastrol

form

crystals

form

solid

form

solid

form

solid

manufacturer/tradename

Calbiochem®

manufacturer/tradename

-

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

storage condition

-

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

color

red

color

red

color

off-white

color

dark red

solubility

DMSO: 5 mg/mL, ethanol: soluble

solubility

DMSO: >10 mg/mL, H2O: insoluble

solubility

DMSO: 10 mg/mL, methanol: 10 mg/mL

solubility

DMF: soluble, DMSO: soluble, ethanol: soluble, methanol: soluble

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).
A cell-permeable dienone-phenolic triterpene compound with antioxidant and anti-inflammatory properties. It suppresses LPS-induced release of pro-inflammatory cytokines in macrophages and monocytes (IC50 = 40 nM for IL-1β and IL-1α, 80 nM for IL-6, 110 nM for PEG2, and 210 nM for IL-8 and TNF-α). Also suppresses 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. Shown to inhibit lipid peroxidation induced by ADP and Fe2+ in rat liver mitochondria (IC50 = 7 µM). Improves performance in memory, learning, and psychomotor activity in rats. May be useful in minimizing inflammation in Alzheimer′s disease animal models.

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

Warning

Toxicity: Standard Handling (A)

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


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Aoi Nakazono et al.
The Journal of biological chemistry, 293(38), 14758-14774 (2018-08-11)
Amyloid and amyloid-like protein aggregations are hallmarks of multiple, varied neurodegenerative disorders, including Alzheimer's and Parkinson's diseases. We previously reported that spinocerebellar ataxia type 14 (SCA14), a dominant-inherited neurodegenerative disease that affects cerebellar Purkinje cells, is characterized by the intracellular
Md Akram Hossain et al.
Frontiers in cell and developmental biology, 9, 738502-738502 (2021-11-20)
The maintenance of genome integrity and fidelity is vital for the proper function and survival of all organisms. Recent studies have revealed that APE2 is required to activate an ATR-Chk1 DNA damage response (DDR) pathway in response to oxidative stress

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