I2906

I2906 is an orally active isocitrate lyase (ICL) inhibitor with a Mycobacterium tuberculosis IC₅₀ of 134.3 μg/mL. I2906 inhibits the growth of Mycobacterium tuberculosis. I2906 can be used for the research of tuberculosis^[1]. In Vitro:I2906 (134.3 μg/mL) inhibits Mycobacterium tuberculosis isocitrate lyase with an IC₅₀ of 134.3 μg/mL^[1].
I2906 inhibits growth of Mycobacterium tuberculosis H37Ra with an MIC of 0.5 μg/mL^[1].
I2906 inhibits growth of Mycobacterium tuberculosis H37Rv and multidrug-resistant strain OB35 with an MIC of 0.50 μg/mL for each^[1].
I2906 inhibits growth of all fully susceptible clinical Mycobacterium tuberculosis isolates with an MIC of 0.54 μg/mL^[1].
I2906 inhibits growth of non-XDR clinical drug-resistant Mycobacterium tuberculosis isolates with MIC₅₀s ranging from 0.54 to 8.0 μg/mL^[1].
I2906 inhibits growth of all extensively drug-resistant Mycobacterium tuberculosis isolates with an MIC of ≥4.33 μg/mL^[1].
I2906 (0-200 μg/mL; 24 h) exhibits low cytotoxicity against THP-1 human acute monocytic leukemia cells with an IC₅₀ of 60.26 μg/mL, resulting in a selectivity index of ~120 for Mycobacterium tuberculosis H37Rv and ~30 for most multidrug-resistant strains^[1]. In Vivo:I2906 (625 mg/kg; p.o.; 5 days/week; 8 weeks) reduces bacterial loads in the lungs and spleen of M. tuberculosis H37Rv-infected mice at week 4 and eliminates infection-related mortality^[1].
I2906 (312.5-625 mg/kg; p.o.; 5 days/week; 6 weeks) reduces bacterial loads in the lungs and spleen of multidrug-resistant M. tuberculosis-infected mice at the 312.5 mg/kg dose, reduces mortality, and lessens lung lesion severity^[1].