Isoindigotin exhibits a broad spectrum of bioactivities, including significant antiproliferative effects against various human tumor cell lines such as HL60, K562, and KB cells, with inhibitory percentages of 53.0%, 64.0%, and 92.0% at 10 µM after 72 hours, respectively. It has an IC50 value of 1600.0 nM for KB cells. In addition to its anticancer properties, it induces NQO1 and CYP1A1 activities in mouse Hepa-1c1c7 cells, showing a moderate induction at 0.1 µM after 48 hours by MTT and EROD assays. It also exhibits cytotoxicity against Hepa-1c1c7 cells over 48 hours. Isoindigotin acts as an inhibitor of human transglutaminase 2 with an IC50 value of 8000.0 nM and a Ki value of 41000.0 nM. Furthermore, it demonstrates growth inhibition activity across a variety of human tumor cell lines, including breast, renal, melanoma, lung, ovarian, prostate, colon, leukemia, and central nervous system cells, with GI50 values ranging from low to high nanomolar concentrations. Additionally, it has antimicrobial activity against Mycobacterium tuberculosis H37Rv in African green monkey Vero cells, with a MIC of 27000.0 nM..
Note: Summary generated by AI. Data source: ChEMBL 