NSC116565

NSC116565 (30 min) potently inhibits Mycobacterium tuberculosis KARI via a slow-binding kinetic mechanism, with an apparent inhibition constant of 0.36 μM^[1].
NSC116565 (0.78-50 μM; 5 days) inhibits the growth of Mycobacterium tuberculosis strains H37Ra (MIC₅₀ = 2.93 μM, MIC₉₀ = 9.86 μM) and H37Rv (MIC₅₀ = 6.06 μM, MIC₉₀ = 20.42 μM) in defined minimal medium, and its activity decreases when branched-chain amino acids are added to the medium^[2].
NSC116565 (30 min) inhibits Oryza sativa KARI with an apparent inhibition constant of 2.4 μM, and shows no time-dependent binding^[1].
NSC116565 (100 μM) inhibits the growth of Mycobacterium tuberculosis H37Rv, with an MIC of 20.4 μM, and its target is the branched-chain amino acid biosynthetic pathway^[1].
NSC116565 (10-100 mg/mL; 72 h) inhibits root growth of Brassica campestris by up to 95% at a concentration of 100 mg/mL and by 70% at 10 mg/mL^[1].
NSC116565 (750-1500 g/ha) exhibits herbicidal activity against a variety of weeds, with the strongest post-emergence inhibitory effect on Amaranthus retroflexus (64.6% at 1500 g/ha)^[1].
NSC116565 (1.6-200.0 μM; 24 h) exhibits no toxicity toward HEK293 and SW620 mammalian cell lines at the highest concentration of 200 μM^[1].
NSC116565 is a potent, time-dependent competitive inhibitor of purified Mycobacterium tuberculosis ketol-acid reductoisomerase (MtKARI), with a K_i value of 95.4 nM^[2].

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