There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
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]
Celastrol/雷公藤红素 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Mouse embryonic fibroblasts (MEFs)
250 nM
7 hours
Analyze gene expression profiles regulated by celastrol for subsequent CMAP database query
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
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