Radicicol is a macrocyclic antifungal antibiotic that inhibits protein tyrosine kinase. Isolated from Monocillium nordinii, it binds to and inhibits Hsp90 at very low concentrations (20nM). Heat shock Protein 90(Hsp90), is a molecular chaperone that mediates the folding of  a number of oncogenic proteins, it is an attractive target for inhibiton by anticancer agents.

Radicicol binds to a highly conserved pocket in the Hsp90 protein and inhibits the intrinsic ATPase activity of Hsp90. Radicicol induces the differentiation of HL-60 cells into macrophages, blocking cell cycle at G1 and G2. It suppresses NIH 3T3 cell transformation by diverse oncogenes such as src, ras and mos and also suppresses the expression of mitogen-inducible cyclooxygenase-2. As a cell differentiation modulator, radicicol has anti-angiogenic activity in vivo, inhibiting the proliferation of and plasminogen activator production by vascular endothelial cells.

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