Clofazimine

Clofazimine is an orally-active anti-mycobacterial agent with a wide range of anti-mycobacterial activity including leprosy and tuberculosis. Clofazimine exerts anti-inflammatory activities and anti-tumor activities by interfering DNA replication and inhibiting IL2 (IC₅₀ = 1.10 ± 0.26 μM, Jurkat T) production. Clofazimine can be used in mycobacterial and cancer research^{[1][2][3][4][5]}. IC50 & Target:IC50: 1.10±0.26 μM (IL2)^[5] In Vitro:Clofazimine (0.0625-2 mg/L, 14 d) exerts no apparent activity against M. tuberculosis during the first 2–4 days of exposure, exhibits a concentration-dependent antimicrobial activity after 1 week: bacteriostatic activity at concentrations at or below the 0.25 mg/L MIC and bactericidal activity at concentrations above the MIC. INH is used as positive control.^[3].
Clofazimine (10 μM, 24 h) inhibits the growth of hematological cancer cell lines (Jurkat, U266, Namalwa, K562, HL60). For U266, Clofazimine (1-50 μM, 12-48 h) shows a dose- and time-dependent inhibitory effect^[4].
Clofazimine (10 μM, 24-48 h) depolarizes the mitochondrial membrane, significantly increases active caspase-3 level (25-fold) and increases the percentage of early and late apoptotic cells in U266^[4].
In Vivo:Clofazimine (100,50 mg/kg, p.o., once per day for 14 d) exhibits a delayed antimicrobial activity against Mycobacterium tuberculosis in mice^[3].