Cinobufotalin

SKU: orb1302378

Description

Cinobufotalin, a cardiac toxin from toad venom, exhibits anti-hepatocellular carcinoma (HCC) activity by inducing growth arrest and apoptosis via ceramide generation in vitro. It reverses multidrug resistance by downregulating P-gp and MRP-1, and enhances the maturation and function of dendritic cells from chronic hepatitis B patients, potentially boosting antiviral immunity.

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 1108-68-5
• MW: 458.54
• Purity: 99.94%
• Formula: C₂₆H₃₄O₇
• SMILES: CC(=O)O[C@H]1[C@H]2O[C@]22[C@@H]3CC[C@]4(O)C[C@@H](O)CC[C@]4(C)[C@H]3CC[C@]2(C)[C@H]1c1ccc(=O)oc1
• Target: IL Receptor,P-gp,Akt,MRP
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.36 mM);DMSO:50 mg/mL (109.04 mM)

Bioactivity

• In Vitro:
  Hepatocellular carcinoma (HCC) is a highly aggressive and lethal neoplasm with poor prognosis the aim of this study is to investigat the anticancer activity of Cinobufotalin, a bufadienolide isolated from toad venom, in cultured HCC cells, and to stud 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 s All hairpin RNA (shRNA)-depletion inhibited Cinobufotalin-induced ceramide production and HCC cell apoptosis. O the Other an 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.

Storage & Handling

• Storage: keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

P-gp, Pgp, Akt, Cinobufotalin, ILReceptor, IL Receptor, Inhibitor, inhibit, MRP1, MRP-1

Compound Identifiers

PubChem CID

259776