Catalog No.: PC-20079Not For Human Use, Lab Use Only.
JSF-3285 (JSF3285) is a potent small molecule inhibitor of the M. tuberculosis β-ketoacyl synthase KasA with Kd of 70.7 nM in MST assays, shows activity against H37Rv strain with MIC 0.2 uM.
JSF-3285 (JSF3285) is a potent small molecule inhibitor of the M. tuberculosis β-ketoacyl synthase KasA with Kd of 70.7 nM in MST assays, shows activity against H37Rv strain with MIC 0.2 uM.
JSF-3285 demonstrated whole-cell activity versus a panel of 48 drug-sensitive and drug-resistant clinical strains comparable with its efficacy versus the H37Rv strain (MIC, 0.2 uM).
JSF-3285 dispplayed a 30-fold increase in mouse plasma exposure compared with GSK3011724A (DG167, Catalog# PC-35948).
JSF-3285 (100 and 200 mg/kg qd po) achieved a ~2 log10 reduction in bacterial burden in M. tuberculosis infection CD-1 mice.
KasA is the only essential member of three β-ketoacyl synthases encoded in the M. tuberculosis genome.
KasA catalyzes the 2-carbon elongation of growing fatty acyl chains in the FAS-II pathway, critical to the biosynthesis of mycolic acids and, in turn, the bacterial cell wall.
