Triacsin C

Triacsin C (WS 1228A), is an orally active and intracellular long-chain acyl-CoA synthetases (ACSL) inhibitor, which can be isolated from Streptomyces aureofaciens. Triacsin C inhibits TAG accumulation into lipid droplets (LD) by suppressing ACSL activity^[1]. Triacsin C exhibits highly inhibitory effect against rotavirus replication^[2]. IC50 & Target:IC50: 3.70 μM (CpACS1), 2.32 μM (CpACS2)^[3] In Vitro:Triacsin C (0-16 μM; 41 h) inhibits parasite fatty acyl-coenzyme A synthetases, and reduces CpACS1 and CpACS2 enzymes activities with IC₅₀s of 3.70 μM and 2.32 μM, respectively, with K_i values of 595 nM and 106 nM, respectively^[3].
Triacsin C (0-16 μM; 41 h) shows anti-parasitic and inhibits Cryptosporidium parvum with an IC₅₀ value of 136 nM^[3].
Triacsin C (0, 0.25, 0.5 μM; 30 min) has no effect on parasite invasion^[3].
In Vivo:Triacsin C (8-15 mg/kg/d; p.o.; 1 week) shows anticryptosporidial efficacy and improves Cryptosporidium parvum infection by targeting parasite fatty acyl-coenzyme A synthetases^[3].
Triacsin C (10 mg/kg/d; p.o.; 2 months) exhibits anti-atherosclerotic activity in aortic atherosclerosis LDLR^-/- mice^[4].