triciribine

Triciribine is a synthetic tricyclic nucleoside analog and small molecule inhibitor primarily developed as an anticancer agent. It was first synthesized in the 1970s and initially studied clinically in the 1980s and 1990s without success. Renewed interest followed discoveries that it selectively inhibits all three isoforms of Akt (Akt1/PKBα, Akt2/PKBβ, Akt3/PKBγ), key serine/threonine kinases in the PI3K/Akt signaling pathway involved in cell proliferation and survival. Triciribine blocks phosphorylation and activation of Akt but does not inhibit upstream kinases such as PI3K or PDK1. It has shown antitumor activity particularly against cancers with hyperactivated Akt signaling. The drug has also demonstrated antiviral activity against HIV-1 at nanomolar concentrations[2][5]. As PTX-200 (triciribine phosphate), it has been investigated by Prescient Therapeutics for breast cancer, ovarian cancer, and acute myeloid leukemia[2][3].

Brand names

PTX-200PTX200PTX 200

Other names

triciribinatriciribinumpentaazacentopthylene