Apoptolidin

Apoptolidin (194874-06-1) is a powerful inducer of apoptosis in a variety of cancer cell lines.1Is believed to act via inhibition of F0F1-ATPase2but correlation studies indicate that a second mechanism may be the actual mode of action3. Cell permeable.

Apoptolidin, originally isolated from a Nocardiopsis sp., induces apoptotic cell death in rat glial cells transformed with the adenovirus E1A oncogene (IC50 = 11 ng/ml). Apoptolidin is among the most selective cytotoxic agents tested by the NCI in human cancer cell lines. Although the apoptotic activity of apoptolidin correlates with F0F1-ATPase inhibition, recent evidence suggests the existence of a secondary biological target or more complex mode of action.

[1] J W KIM. Apoptolidin, a new apoptosis inducer in transformed cells from Nocardiopsis sp.[J]. Journal of Antibiotics, 1997, 50 7: 628-630. DOI:10.7164/antibiotics.50.628
[2] A. SALOMON. Apoptolidin, a selective cytotoxic agent, is an inhibitor of F0F1-ATPase.[J]. Chemistry & biology, 2001, 28 4 1: 71-80. DOI:10.1016/s1074-5521(00)00057-0
[3] PAUL A. WENDER. Correlation of F0F1-ATPase Inhibition and Antiproliferative Activity of Apoptolidin Analogues[J]. Organic Letters, 2006, 8 4: 589-592. DOI:10.1021/ol052800q