Radicicol

Radicicol is an inhibitor of Hsp90 with an IC₅₀ value < 1 μM, and leads to proteasomal degradation^[1]. Radicicol exhibits inhibition on PDK with IC₅₀s of 230 μM (PDK1) and 400 μM (PDK3). Radicicol is an antifungal and antimalarial antibiotic, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB^[2]. Radicicol is also an inhibitor of fat mass and obesity-associated protein (FTO), with an IC₅₀ value of 16.04 μM^[3]. IC50 & Target:IC50: <1 μM (Hsp90), 230 μM (PDK1), 400 μM (PDK3)^[1]; topoisomerase VIB^[2]; 16.04 μM (fat mass and obesity-associated protein, FTO)^[3] In Vitro:Radicicol (1 μM or 100 μM) inhibits the activities of Hsp90 and Topo VI by blocking ATP binding^[1].
Radicicol (100 μM; 10 min) binds to ATP-binding site in the C-terminal domain of PDK3 and prevents maturation of Hsp90 clients^[1].
Radicicol (0.25-18 μM; 48 h) inhibits P. falciparum 3D7 growth with an IC₅₀ value of 8.563 μM, and (8 μM; 50 h) delays the schizont-to-ring transition^[2].
Radicicol (1.5 μM; 40 h) suppresses mitochondrial DNA replication without affecting nuclear and apicoplast genomes^[2].
Radicicol (0.001-5 μM; 72 h) induces myoblast differentiation with the myoblast toxicity concentration of 0.1 μM^[5].
In Vivo:Radicicol (20 mg/kg or 60 mg/kg; i.p.; twice dosages; 1 h before and after) has renoprotection effect, and ameliorates renal ischemia reperfusion (I/R) injury and increases renal HSP70 mRNA and protein in renal injury mice^[4].
Radicicol (0.05 mg/20 g; s.c.; single dose) enhances the regeneration of skeletal muscle injured by crotoxin via decrease of NF-kB activation^[5].