Acivicin hydrochloride

Acivicin hydrochloride (AT-125 hydrochloride), a natural product produced by Streptomyces sviceus, is a γ−glutamyl transpeptidase (GGT) inhibitor. Acivicin hydrochloride can across the blood-brain barrier and has anti-cancer, anti-parasitic properties[1][2].

Research Areas >> Cancer

Research Areas >> Infection

γ−glutamyl transpeptidase[1]

Acivicin hydrochloride (AT-125 hydrochloride; 0.1-50 μM; 5 days) has an IC50 of 0.7 μM in human HepG2 cells[1].

Acivicin hydrochloride (AT-125 hydrochloride; 0.1-50 μM; 5 days; for 4 days) reduces urinary gamma-GT by 70-78%[1]. Animal Model: Male pigmented Long-Evans rats weighed between 250 g and 300 g exposed to Toluene[1] Dosage: 5 mg/kg Administration: IP; twice weekly (monday and wednesday); for 4 days Result: Reduced urinary gamma-GT by 70-78%.

[1]. Kreuzer J, et al. Target discovery of acivicin in cancer cells elucidates its mechanism of growth inhibition†Electronic supplementary information (ESI) available: Synthesis, cloning, protein expression, purification and biochemical assays. Chem Sci. 2014 Dec 1;6(1):237-245. Epub 2014 Sep 26.

[2]. Chikhale EG, et al. Carrier-mediated transport of the antitumor agent acivicin across the blood-brain barrier. Biochem Pharmacol. 1995 Mar 30;49(7):941-5.

[3]. Delphine Waniusiow, et al. Toluene-induced hearing loss in acivicin-treated rats. Neurotoxicol Teratol. May-Jun 2008;30(3):154-60.