LysRs-IN-2 is a lysyl-tRNA synthetase (KRS) inhibitor with IC 50 s of 0.015 μM and 0.13 μM for Plasmodium falciparum lysyl-tRNA synthetase ( Pf KRS) and Cryptosporidium parvum lysyl-tRNA synthetase ( Cp KRS), respectively.
Storage Temp
Store at 2-8°C
Shipped In
Wet ice
This product requires cold chain shipping. Ground and other economy services are not available.
Product Description
LysRs-IN-2 is a lysyl-tRNA synthetase (KRS) inhibitor with IC 50 s of 0.015 μM and 0.13 μM for Plasmodium falciparum lysyl-tRNA synthetase ( Pf KRS) and Cryptosporidium parvum lysyl-tRNA synthetase ( Cp KRS), respectively
In Vitro
LysRs-IN-2 is active against whole-cell bloodstream P. falciparum 3D7 (EC 50 =0.27 μM), Hs KRS (IC 50 =1.8 μM), HepG2 cells (EC 50 =49 μM), and Cryptosporidium parvum (EC 50 =2.5 µM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
LysRs-IN-2 (1.5 mg/kg; orally once a day for 4 days) reduces parasitemia by 90% in the murine P. falciparum SCID model. LysRs-IN-2 (20 mg/kg; orally once a day for 7 days) reduces parasite shedding in NOD SCID gamma mice and INF-γ-knockout mice ( Cryptosporidium mouse models) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Murine P. falciparum NODscidIL2Rγ (SCID) model Dosage: 1.5 mg/kg Administration: Orally once a day for 4 days Result: Reduced parasitemia by 90% in the malaria SCID mouse model. Animal Model: NOD SCID gamma and INF-γ–knockout mouse models ( Cryptosporidium mouse models) Dosage: 20 mg/kg Administration: Orally once a day for 7 days Result: Reduced parasite shedding below detection level, and this reduction was sustained for 3 wk after treatment had stopped in INF-γ-knockout mice.\nDosed orally at a concentration of 20 mg/kg once a day for 7 days showed 96% reduction of parasite shedding comparable to paromomycin in NOD SCID gamma mice.
This compound belongs to the class of organic compounds known as chromones. These are compounds containing a benzopyran-4-one moiety.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
