产品说明书

Celastrol

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Chemical Structure| 34157-83-0 同义名 : Tripterine;Tripterin;NSC 70931
CAS号 : 34157-83-0
货号 : A364744
分子式 : C29H38O4
纯度 : 98%
分子量 : 450.61
MDL号 : MFCD03424073
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(77.67 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • 20S proteasome

    20S proteasome, IC50:2.5 μM
描述 Celastrol possesses multiple function as it is a novel HSP90 inhibitor which can disrupt nHsp90/Cdc37 complex[4], a potent inhibitor of lipid peroxidation in mitochondria[5] and exhibits anti-inflammatory activity[6]. Celastrol disrupted Hsp90-Cdc37 complex formation, whereas the classical Hsp90 inhibitors (e.g. geldanamycin) have no effect. Celastrol inhibited Hsp90 ATPase activity without blocking ATP binding. Proteolytic fingerprinting indicated celastrol bound to Hsp90 C-terminal domain to protect it from trypsin digestion[4]. Celastrol exhibited anti-peroxidative effect with IC50 value of 7μM and scavenged 1.5 molar equivalents of radicals in homogeneous aqueous ethanolic solution[5]. Celastrol potentiated the apoptosis induced by TNF and chemotherapeutic agents and inhibited invasion, both regulated by NF-κB activation. It suppressed TNF-induced the expression of gene products involved in antiapoptosis (IAP1, IAP2, Bcl-2, Bcl-XL, c-FLIP, and survivin), proliferation (cyclin D1 and COX-2), invasion (MMP-9), and angiogenesis (VEGF). Celastrol suppressed both inducible and constitutive NF-κB activation. It inhibited the TNF-induced activation of IκBalpha kinase, IκBalpha phosphorylation, IκBalpha degradation, p65 nuclear translocation and phosphorylation, TAK1-induced NF-κB activation and NF-κB-mediated reporter gene expression[6].
作用机制 Celastrol binds to Hsp90 C-terminal domain to protect it from trypsin digestion and disrupts Hsp90-Cdc37 complex formation.[4]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
HeLa cells Function assay Inhibition of NF-kappaB activity in human HeLa cells by SEAP reporter assay, IC50=0.15 μM 20469887
HeLa cells Function assay 3 h Amplification of HSF1 transcriptional activity in human HeLa cells assessed as granule formation pretreated for 3 hrs by immunocytochemical staining, EC50=2.6 μM 19502057
human 293T cells Function assay 30 mins Inhibition of LPS-induced NF-kappaB activation in human 293T cells incubated for 30 mins followed by treated with LPS for 6 hrs by dual-luciferase reporter assay, IC50=0.17 μM 21393004
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.22mL

0.44mL

0.22mL

11.10mL

2.22mL

1.11mL

22.19mL

4.44mL

2.22mL
参考文献

[1]Zhang T, Li Y, et al. Characterization of celastrol to inhibit hsp90 and cdc37 interaction. J Biol Chem. 2009 Dec 18;284(51):35381-9.

[2]Sassa H, Takaishi Y, et al. The triterpene celastrol as a very potent inhibitor of lipid peroxidation in mitochondria. Biochem Biophys Res Commun. 1990 Oct 30;172(2):890-7.

[3]Sethi G, Ahn KS, et al. Celastrol, a novel triterpene, potentiates TNF-induced apoptosis and suppresses invasion of tumor cells by inhibiting NF-kappaB-regulated gene products and TAK1-mediated NF-kappaB activation. Blood. 2007 Apr 1;109(7):2727-35.

[4]Zhang T, Li Y, Yu Y, Zou P, Jiang Y, Sun D. Characterization of celastrol to inhibit hsp90 and cdc37 interaction. J Biol Chem. 2009 Dec 18;284(51):35381-9. doi: 10.1074/jbc.M109.051532. PMID: 19858214; PMCID: PMC2790967.

[5]Sassa H, Takaishi Y, Terada H. The triterpene celastrol as a very potent inhibitor of lipid peroxidation in mitochondria. Biochem Biophys Res Commun. 1990 Oct 30;172(2):890-7. doi: 10.1016/0006-291x(90)90759-g. PMID: 2241977.

[6]Sethi G, Ahn KS, Pandey MK, Aggarwal BB. Celastrol, a novel triterpene, potentiates TNF-induced apoptosis and suppresses invasion of tumor cells by inhibiting NF-kappaB-regulated gene products and TAK1-mediated NF-kappaB activation. Blood. 2007 Apr 1;109(7):2727-35. doi: 10.1182/blood-2006-10-050807. Erratum in: Blood. 2013 Aug 15;122(7):1327. PMID: 17110449.