aplyronine A

Aplyronine A is a specific actin-depolymerizing agent. Aplyronine A has antitumor and apoptosis effect. Aplyronine A can be used for the research of cancer and muscle contraction, cell motility and cell division[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Autophagy >> Autophagy

IC50: 0.01 nM (HeLa S3 cells)[1]. EC50: 1.3 μM (F-actin)[1]

Aplyronine A (compound 1) has cytotoxicity against HeLa S3 cells with IC50 value of 0.01 nM[1]. Aplyronine A depolymerizes fibrous actin (F-actin) and inhibits the polymerization of actin with an EC50 value of 1.3 μM in vitro actin-depolymerizing assay[1]. Aplyronine A (0-1 μM, 0-2 h) causes prominent caspase-dependent apoptosis in human epithelial carcinoma HeLa S3 cells[1]. Aplyronine A (100 nM, 24 h) causes malfunction of cell adhesion and dephosphorylation of focal adhesion kinase with apoptosis[1]. Western Blot Analysis[1] Cell Line: HeLa S3 cells Concentration: 0-1 μM Incubation Time: 0-2 h Result: Induced the dephosphorylation of FAK in HeLa S3 cells. Apoptosis Analysis[1] Cell Line: HeLa S3 cells Concentration: 100 nM Incubation Time: 24 h Result: Significantly reduced cellular viabilities in tumor cells and significant activation of caspase 3 in HeLa S3 cells.

Aplyronine A (0.08 mg/kg) exhibits remarkable antitumor activities in vivo against P388 murine leukemia cells[1].

[1]. Masaki Kita, et al. Fluorescent aplyronine a: intracellular accumulation and disassembly of actin cytoskeleton in tumor cells. Chembiochem. 2012 Aug 13;13(12):1754-8, 1702.