A cardiotonic steroid that has diverse biological activities; inhibits Na+/K+-ATPase activity in guinea pig heart ventricular muscle homogenates at 0.3 μM; is cytotoxic to HCT116 cells in vitro (IC50s =

Cinobufagin – 5 mg

Brand:
Cayman
CAS:
470-37-1
Storage:
-20
UN-No:
Non-Hazardous - 2811 / 6.1

Cinobufagin is a cardiotonic steroid that has been found in the skin of toads of genus Bufo and has diverse biological activities.{48257,48258,48259,48260} It inhibits Na+/K+-ATPase activity in guinea pig heart ventricular muscle homogenates by 45% when used at a concentration of 0.3 μM.{48257} Cinobufagin is cytotoxic to HCT116 colorectal cancer cells in vitro with IC50 values of less than 50 ng/ml at 48- and 72-hour time points and induces apoptosis in a concentration-dependent manner.{48258} In vivo, cinobufagin (10 mg/kg) reduces tumor growth in an HCT116 mouse xenograft model. Cinobufagin (1 μg/ml) inhibits LPS-induced expression of MHC class II, CD80, and CD86 and release of IL-6, IL-8, TNF-α, and IL-10 in human monocyte-derived dendritic cells.{48259} It also increases expression of the antimicrobial peptides hBD2 and hBD3 in dendritic cells. Cinobufagin exhibits dose-dependent antinociceptive effects in the hot-plate, acetic acid writhing, and formalin tests in mice.{48260}  

 

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Description

A cardiotonic steroid that has diverse biological activities; inhibits Na+/K+-ATPase activity in guinea pig heart ventricular muscle homogenates at 0.3 μM; is cytotoxic to HCT116 cells in vitro (IC50s = <50 ng/ml at 48- and 72-hour time points) and induces apoptosis; reduces tumor growth in an HCT116 mouse xenograft model at 10 mg/kg; inhibits LPS-induced expression of MHC class II, CD80, and CD86 and release of IL-6, IL-8, TNF-α, and IL-10 in human monocyte-derived dendritic cells at 1 μg/ml; increases expression of hBD2 and hBD3 in dendritic cells; exhibits antinociceptive effects in mice

Formal name: (5β)-16β-(acetyloxy)-14,15β-epoxy-3β-hydroxy-bufa-20,22-dienolide

Synonyms:  NSC 90325

Molecular weight: 442.5

CAS: 470-37-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Lipids|Sterol Lipids||Product Type|Biochemicals|Natural Products||Product Type|Biochemicals|Small Molecule Inhibitors|ATPases||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cardiovascular System|Cardiovascular Diseases|Heart Failure||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Infectious Disease||Research Area|Neuroscience|Pain Research

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