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Cinobufotalin

Catalog No. T4A2399   CAS 1108-68-5

Cinobufotalin is a main cardiac toxin in toad, it is a novel anti-HCC agent, it induces growth inhibition and apoptosis in cultured HCC cells through ceramide production. Cinobufotalin is also an effective reversal agent for the multidrug resistance of tumors, it can reverse the adriamycin-resistance in Raji/ADR cells and the expression of P-gp and MRP-1 proteins. Cinobufotalin can promote the dendritic cells(DCs) derived from peripheral blood of patients with chronic hepatitis B to mature and effectively enhance its(the DCs') capabilities, therefore the treatment of cinobufotalin may potentiate the antiviral immunity of the patients with chronic hepatitis B(CHB).

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Cinobufotalin Chemical Structure
Cinobufotalin, CAS 1108-68-5
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1 mg In stock $ 44.00
2 mg In stock $ 62.00
5 mg In stock $ 89.00
10 mg In stock $ 150.00
25 mg In stock $ 251.00
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1 mL * 10 mM (in DMSO) In stock $ 97.00
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Purity: 99.94%
Purity: 99.85%
Purity: 99.52%
Purity: 98.92%
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Biological Description
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Description Cinobufotalin is a main cardiac toxin in toad, it is a novel anti-HCC agent, it induces growth inhibition and apoptosis in cultured HCC cells through ceramide production. Cinobufotalin is also an effective reversal agent for the multidrug resistance of tumors, it can reverse the adriamycin-resistance in Raji/ADR cells and the expression of P-gp and MRP-1 proteins. Cinobufotalin can promote the dendritic cells(DCs) derived from peripheral blood of patients with chronic hepatitis B to mature and effectively enhance its(the DCs') capabilities, therefore the treatment of cinobufotalin may potentiate the antiviral immunity of the patients with chronic hepatitis B(CHB).
In vitro Hepatocellular carcinoma (HCC) is a highly aggressive and lethal neoplasm with poor prognosis. The aim of this study is to investigate the anticancer activity of Cinobufotalin, a bufadienolide isolated from toad venom, in cultured HCC cells, and to study the underlying mechanisms. METHODS AND RESULTS:We found that Cinobufotalin (at nmol/L) significantly inhibited HCC cell growth and survival while inducing considerable cell apoptosis. Further, Cinobufotalin inhibited sphingosine kinase 1 (SphK1) activity and induced pro-apoptotic ceramide production. Ceramide synthase-1 small hairpin RNA (shRNA)-depletion inhibited Cinobufotalin-induced ceramide production and HCC cell apoptosis. On the other hand, the glucosylceramide synthase (GCS) inhibitor 1-phenyl-2-decanoylamino-3-morpholino-1-propanol (PDMP) facilitated Cinobufotalin-induced ceramide production and cell apoptosis. SphK1 inhibitor II (SKI-II), similar to Cinobufotalin, increased cellular ceramide level and promoted HCC cell apoptosis. Finally, we observed that Cinobufotalin inactivated Akt-S6K1 signaling in HepG2 cells, which was again inhibited by ceramide synthase-1 shRNA-depletion. CONCLUSIONS:In conclusion, the results of this study suggest that Cinobufotalin induces growth inhibition and apoptosis in cultured HCC cells through ceramide production. Cinobufotalin may be investigated as a novel anti-HCC agent.
Molecular Weight 458.54
Formula C26H34O7
CAS No. 1108-68-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (89.82 mM), sonification is recommended.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Infection Compound Library Angiogenesis related Compound Library Neural Regeneration Compound Library Anti-Pancreatic Cancer Compound Library Bioactive Compound Library PI3K-AKT-mTOR Compound Library Antidepressant Compound Library

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Keywords

Cinobufotalin 1108-68-5 Cytoskeletal Signaling Immunology/Inflammation Membrane transporter/Ion channel Neuroscience PI3K/Akt/mTOR signaling IL Receptor P-gp Akt MRP inhibit Inhibitor inhibitor

 

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