In vitro
BIBR 1532 is a non peptidic, non nucleosidic small molecule capable of inhibiting the catalytic activity of telomerase. This synthetic antitelomerase compound interferes with the in vitro processivity of telomerase in a dose-dependent manner with half maximal inhibitory concentrations (IC50) of 93 nM.Telomerase inhibition using BIBR 1532 in human cancer cells from fibrosarcoma, prostate, breast, and lung carcinoma lead to progressive shortening of telomeres down to a critical checkpoint followed by triggering a DNA damage response. High doses of BIBR 1532 induce caspase 3 activity. BIBR 1532 inhibits telomerase activity in a dose-dependent manner. BIBR 1532 disturbs transcriptional balanced ratio between Bcl-2 and Bax in favor of apoptosis. BIBR 1532 can also downregulates c-Myc and hTERT expression and induce p21 mRNA overexpression.
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