219465

Celastrol, Celastrus scandens

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

• 別名: Celastrol, Celastrus scandens , Tripterin, 3-Hydroxy-24-nor-2-oxo-1(10),3,5,7-friedelatetraen-29-oic Acid, Proteasome Inhibitor XIX
• 実験式（ヒル表記法）: C₂₉H₃₈O₄
• CAS番号: 34157-83-0
• 分子量: 450.61
• MDL番号: MFCD03424073
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥95% (TLC)
• 形状: crystals
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: red
• 溶解性: DMSO: 5 mg/mL; ethanol: soluble
• 輸送温度: ambient
• 保管温度: 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

詳細

詳細

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.

生物化学的／生理学的作用

Cell permeable: yes

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 2.5 µM inhibiting chymotrypsin-like activity of 20S proteasome

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 2
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable