Jasplakinolide

Jasplakinolide is a naturally occurring macrocyclic peptide which induces the polymerization of actin into filaments (F-actin). Jasplakinolide is demonstrated to bind to F-actin competitively with Phalloidin , an irreversible stabilizer of F-actin, to stabilize the filaments and to promote filamentous assembly of actin. Actin filaments form the structural foundation of the cytoskeleton and native regulation of actin polymerization/depolymerization is crucial for mechanical processes in the cell. Antiproliferative and cytotoxic effects are produced by Jasplakinolide, attributed to prevention of F-actin depolymerization and to induced overpolymerization of monomeric actin. Jasplakinolide was shown to enhance the interleukin-2 apoptotic signal in CTLL-20 interleukin-2-dependent T cells, suggesting a participation of the actin cytoskeleton in the transduction of proliferative signals to cells. Jasplakinolide prevents activation of store-mediated Ca²⁺ entry into human platelets, also through its effect on the actin cytoskeleton.

≥97%