219465

Celastrol, Celastrus scandens

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

• 동의어(들): Celastrol, Celastrus scandens , Tripterin, 3-Hydroxy-24-nor-2-oxo-1(10),3,5,7-friedelatetraen-29-oic Acid, Proteasome Inhibitor XIX
• 실험식(Hill 표기법): C₂₉H₃₈O₄
• CAS Number: 34157-83-0
• Molecular Weight: 450.61
• MDL number: MFCD03424073
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥95% (TLC)
• 형태: crystals
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: red
• solubility: DMSO: 5 mg/mL; ethanol: soluble
• 배송 상태: ambient
• 저장 온도: 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

설명

일반 설명

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.

생화학적/생리학적 작용

Cell permeable: yes

Product does not compete with ATP.

Reversible: no

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

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

기타 정보

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.

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable