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CAS No.: 34157-83-0

雷公藤红素 Catalog No. CSN16303

Synonyms: Tripterine;TripterinTripterinTripterinTripterinTripterin;雷公藤红素

Celastrol is an inhibitor of HSP90 with antioxidant and anti-inflammatory activities.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
动物研究
剂量
Mice: 0.5 mg/kg^[4] (i.p.); 2 mg/kg^[4] (i.g.)

给药途径
i.p., i.g.
参考文献

动物研究
剂量	Mice: 0.5 mg/kg^[4] (i.p.); 2 mg/kg^[4] (i.g.)
给药途径	i.p., i.g.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2192 mL
- 11.0961 mL
- 22.1922 mL
- 5 mM
- 0.4438 mL
- 2.2192 mL
- 4.4384 mL
- 10 mM
- 0.2219 mL
- 1.1096 mL
- 2.2192 mL

技术信息

CAS号

34157-83-0

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H38O4

运输

蓝冰

分子量

450.61

别名

Tripterine;TripterinTripterinTripterinTripterinTripterin;雷公藤红素

溶解度

DMSO	103.33 mg/mL (229.3 mM)
Water	insoluble

动物实验配方

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

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
human 293T cells	-	Cytotoxic assay	-	Cytotoxicity against human 293T cells assessed as cell viability by dual-luciferase reporter assay, IC50=0.67 μM	21393004
human HeLa cells	-	Cytotoxic assay	72 h	Cytotoxicity against human HeLa cells after 72 hrs by MTS assay, IC50=3 μM	19502057
human HepG2 cells	-	Function assay	48 h	Anticancer activity against human HepG2 cells assessed as cell survival after 48 hrs by MTT assay, IC50=4.01 μM	25812966
human LNCAP cells	-	Function assay	-	Antitumor activity against human LNCAP cells, IC50=2.5 μM	20627556
human MCF7 cells	-	Cytotoxic assay	72 h	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay, IC50=0.153 μM	25756299
human MCF7 cells	-	Function assay	24 h	Inhibition of HSP90 in human MCF7 cells assessed as Raf degradation at 5 times IC50 after 24 hrs by Western blot analysis	25756299
human MGC803 cells	-	Function assay	48 h	Anticancer activity against human MGC803 cells assessed as cell survival after 48 hrs by MTT assay, IC50=1.55 μM	25812966
human NCI-H460 cells	-	Cytotoxic assay	-	Cytotoxicity against human NCI-H460 cells after overnight incubation by MTT assay, IC50=12.3 μM	21942765
human RPMI8226 cells	-	Growth inhibition assay	-	Growth inhibition of human RPMI8226 cells, IC50=3 μM	18164197
human SGC7901 cells	-	Function assay	48 h	Anticancer activity against human SGC7901 cells assessed as cell survival after 48 hrs by MTT assay, IC50=0.15 μM	25812966
human SH-SY5Y cells	-	Function assay	-	Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in human SH-SY5Y cells assessed as lactate dehydrogenase release, EC50=0.03764 μM	19138859
human SK-N-SH cells	-	Cytotoxic assay	72 h	Cytotoxicity against human SK-N-SH cells after 72 hrs by MTS assay, CC50=1.6 μM	19502057
human SMMC7721 cells	-	Function assay	48 h	Anticancer activity against human SMMC7721 cells assessed as cell survival after 48 hrs by MTT assay, IC50=0.58 μM	25812966
human THP1 cells	-	Function assay	24 h	Induction of apoptosis in TRAIL-resistant human THP1 cells after 24 hrs by annexin-V staining, EC50=15 μM	20864342
mouse RAW264.7 cells	-	Function assay	18 h	Inhibition of LPS-stimulated NFkappaB activation transfected in mouse RAW264.7 cells after 18 hrs by luciferase reporter gene assay, IC50=0.2 μM	22705020
rat PC12 cells	-	Function assay	-	Cytoprotective activity against t-BPH-induced cell damage in rat PC12 cells assessed as cell viability, IC50=3.15 μM	20627556

雷公藤红素 Catalog No. CSN16303

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