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Celastrol, Celastrus scandens - CAS 34157-83-0 - Calbiochem

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

Synonym: Celastrol, Celastrus scandens - CAS 34157-83-0 - Calbiochem, Tripterin, 3-Hydroxy-24-nor-2-oxo-1(10),3,5,7-friedelatetraen-29-oic Acid, Proteasome Inhibitor XIX

  • CAS Number 34157-83-0

  • Empirical Formula (Hill Notation) C29H38O4

  • Molecular Weight 450.61

  •  MDL number MFCD03424073

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Properties

Related Categories Molecular Biology, Post-Translational Modification, Proteomics, Ubiquitination Analysis
Quality Level   100
assay   ≥95% (TLC)
form   crystals
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   +2C to +8C
color   red
solubility   DMSO: 5 mg/mL
  ethanol: soluble
shipped in   ambient
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

Description

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.

Packaging

10 mg in Plastic ampoule

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.

Safety & Documentation

Safety Information

Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable
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