For research use only. Not for therapeutic Use.
LysRs-IN-2 is a lysyl-tRNA synthetase (KRS) inhibitor with IC50s of 0.015 μM and 0.13 μM for Plasmodium falciparum lysyl-tRNA synthetase (PfKRS) and Cryptosporidium parvum lysyl-tRNA synthetase (CpKRS), respectively[1].
LysRs-IN-2 is active against whole-cell bloodstream P. falciparum 3D7 (EC50=0.27 μM), HsKRS (IC50=1.8 μM), HepG2 cells (EC50=49 μM), and Cryptosporidium parvum (EC50=2.5 µM)[1].
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)[1].
| Catalog Number | I019156 |
| CAS Number | 2170696-76-9 |
| Synonyms | N-[(4,4-difluoro-1-hydroxycyclohexyl)methyl]-6-fluoro-4-oxochromene-2-carboxamide |
| Molecular Formula | C17H16F3NO4 |
| Purity | ≥95% |
| InChI | InChI=1S/C17H16F3NO4/c18-10-1-2-13-11(7-10)12(22)8-14(25-13)15(23)21-9-16(24)3-5-17(19,20)6-4-16/h1-2,7-8,24H,3-6,9H2,(H,21,23) |
| InChIKey | PJBRCGHQNUWERQ-UHFFFAOYSA-N |
| SMILES | C1CC(CCC1(CNC(=O)C2=CC(=O)C3=C(O2)C=CC(=C3)F)O)(F)F |
| Reference | [1]. Baragaña B, et al. Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis. Proc Natl Acad Sci U S A. 2019 Apr 2;116(14):7015-7020. |
