Trypanothione synthetase-IN-1

Modify Date: 2024-04-03 19:47:55

Trypanothione synthetase-IN-1 Structure
Trypanothione synthetase-IN-1 structure
Common Name Trypanothione synthetase-IN-1
CAS Number 2355349-41-4 Molecular Weight 785.83
Density N/A Boiling Point N/A
Molecular Formula C40H38F3N7O5S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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].

 Names

Name Trypanothione synthetase-IN-1

 Trypanothione synthetase-IN-1 Biological Activity

Description 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].
Related Catalog
Target

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

In Vitro 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.
References

[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.

 Chemical & Physical Properties

Molecular Formula C40H38F3N7O5S
Molecular Weight 785.83