Trypanothione synthetase-IN-1

Trypanothione synthetase-IN-1 (Compound 1) is a competitive Leishmania infantum trypanothione synthetase (TryS) inhibitor with an IC50 of 14.8 μM when triamine spermidine is as polyamine S[1].

Research Areas >> Infection

Signaling Pathways >> Others >> Others

IC50: 14.8 μM (LiTryS, triamine spermidine as polyamine S), 16.2 μM (LiTryS, glutathionylspermidine as polyamine S)[1]

Trypanothione synthetase-IN-1 (Compound 1) (0-75 μM; 24 or 72 h) shows leishmanicidal activity with cytotoxicity[1]. Trypanothione synthetase-IN-1 competes with ATP and the polyamine substrate for binding to LiTryS[1]. Cell Cytotoxicity Assay[1] Cell Line: L. infantum, HepG2 Concentration: 0-75 μM Incubation Time: 24 h (L. infantum axenic amastigotes) or 72 h Result: Showed leishmanicidal activity with EC50s of 21.5 ± 2.4 μM and 13.5 ± 0.9 μM against axenic amastigotes and intracellular amastigotes, respectively. Showed cytotoxicity with a CC50 of 15.9 ± 0.4 μM against HepG2 cells.

[1]. Alcón-Calderón M, et al. Identification of L. infantum trypanothione synthetase inhibitors with leishmanicidal activity from a (non-biased) in-house chemical library. European Journal of Medicinal Chemistry, 2022: 114675.