The compound was first reported by Japanese researcher Hirokazu Kawagishi and colleagues in 2002, who isolated about 190 milligrams of the chemical from 30.3 kg (67 lb) of fresh mushrooms and determined its complete structure.

[1] Ustalic acid is an inhibitor of the sodium-potassium pump (Na+/K+-ATPase), found in the plasma membrane of all animal cells.

When force-fed to mice, ustalic acid causes them to sit still in a crouched position, hesitant to move, and induces tremors and abdominal contractions.

[1] Biosynthetically, ustalic acid is thought to originate from oxidative cleavage of the red pigment phlebiarubron.

[2] A low-yield total synthesis of the dimethyl ester of ustalic acid was reported in 2006, starting with phlebiarubrone.