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Beschreibung

A macrocyclic lactone with antitumor properties. Potently activates protein kinase C and exhibits a high binding affinity (Ki = 1.35 nM). Effectively translocates and down-regulates PKC isozymes alpha, delta, and epsilon. Induces a biphasic activation of PKD through a PKC-dependent pathway in intact cells. Also shown to activate Ras in Jurkat T cells and in rat2 cells., A macrocyclic lactone that exhibits anti-tumor properties. Potently activates protein kinase C and exhibits high binding affinity (Ki = 1.35 nM). Effectively translocates protein kinase C (PKC) isozymes alpha, beta, and epsilon and induces a biphasic, concentration-dependent, down-regulation of PKC delta. Reported to compete with phorbol esters in binding to PKC. Stimulates protein kinase D (PKD) activity in a biphasic, PKC-dependent manner in intact cells. Also activates Ras in Jurkat T cells and in rat2 cells.