TLSC702 is a human glyoxalase I ( hGLO I ) inhibitor with an IC50 of 2.0 μM. TLSC702 inhibits the activity of human glyoxalase I, thereby leading to the accumulation of methylglyoxal and its derived advanced glycation end products. TLSC702 inhibits tumor cell proliferation, induces apoptotic morphological changes, internucleosomal DNA fragmentation and PARP cleavage in tumor cells. TLSC702 can be used in research related to leukemia and lung cancer [1].
In Vitro, TLSC702 (24 h) suppresses the proliferation of human myeloid leukemia HL-60 cells in a dose-dependent manner with an EC50 of approximately 400 μM[1]. TLSC702 (100-1000 μM; 24 h) induces apoptosis in human myeloid leukemia HL-60 cells in a dose-dependent manner, as evidenced by morphological changes, DNA ladder formation, and PARP cleavage, with necrotic cell death also occurring at 1000 μM[1]. TLSC702 (24 h (both cell lines); 24, 48, 72 h (NCI-H522 cells only)) preferentially suppresses the proliferation of GLO I-high human lung cancer NCI-H522 cells compared to GLO I-low human lung cancer NCI-H460 cells, with a time-dependent antiproliferative effect on NCI-H522 cells that yields EC50 values of >300 μM (24 h), 202 μM (48 h), and 145 μM (72 h)[1]. TLSC702 (300 μM; 24, 48, 72 h) induces accumulation of argpyrimidine adducts in human lung cancer NCI-H522 cells[1].
References:
[1]. Takasawa R, et al. TLSC702, a Novel Inhibitor of Human Glyoxalase I, Induces Apoptosis in Tumor Cells. Biol Pharm Bull. 2016;39(5):869-873.
In Vitro, TLSC702 (24 h) suppresses the proliferation of human myeloid leukemia HL-60 cells in a dose-dependent manner with an EC50 of approximately 400 μM[1]. TLSC702 (100-1000 μM; 24 h) induces apoptosis in human myeloid leukemia HL-60 cells in a dose-dependent manner, as evidenced by morphological changes, DNA ladder formation, and PARP cleavage, with necrotic cell death also occurring at 1000 μM[1]. TLSC702 (24 h (both cell lines); 24, 48, 72 h (NCI-H522 cells only)) preferentially suppresses the proliferation of GLO I-high human lung cancer NCI-H522 cells compared to GLO I-low human lung cancer NCI-H460 cells, with a time-dependent antiproliferative effect on NCI-H522 cells that yields EC50 values of >300 μM (24 h), 202 μM (48 h), and 145 μM (72 h)[1]. TLSC702 (300 μM; 24, 48, 72 h) induces accumulation of argpyrimidine adducts in human lung cancer NCI-H522 cells[1].
References:
[1]. Takasawa R, et al. TLSC702, a Novel Inhibitor of Human Glyoxalase I, Induces Apoptosis in Tumor Cells. Biol Pharm Bull. 2016;39(5):869-873.