staurosporine

Staurosporine is a natural indolocarbazole alkaloid originally isolated from the bacterium Streptomyces staurosporeus in 1977. It is a prototypical, highly potent, but non-selective ATP-competitive inhibitor of protein kinases, particularly protein kinase C (PKC), with an IC50 of approximately 0.7 nM. Staurosporine also inhibits other kinases such as PKA, PKG, CAMKII, myosin light chain kinase (MLCK), and GSK3β at higher concentrations. Its broad activity results from its strong affinity for the conserved ATP-binding site found in many kinases. In research settings, it is widely used to induce apoptosis and study cell signaling pathways due to its ability to activate caspase-dependent cell death mechanisms and arrest cells at various points in the cell cycle depending on concentration and context. Although it has shown cytotoxicity against cancer cells and potential anti-cancer effects in preclinical models, its lack of selectivity has precluded clinical use as a therapeutic agent; however, several analogues inspired by staurosporine are under investigation or approved for clinical use[1][2][5][8].

Other names

staurosporineStaurosporinAntibiotic 230Antibiotic230Antibiotic-230Antibiotic AM 2282CCRIS 3272CCRIS3272CCRIS-3272