2-[[(2E)-3-(2-NAPHTHALENYL)-1-OXO-2-BUTEN-1-YL]AMINO]BENZOIC ACID

Описание

BIBR 1532 is a mixed-type non-competitive inhibitor of telomerase (IC₅₀ = 93 nM) that has little effect on several mammalian DNA and RNA polymerases, bacterial DNA helicase, or HIV-1 reverse transcriptase. It specifically targets the telomerase reverse transcriptase catalytic subunit, TERT. Through its effects on telomerase, BIBR 1532 induces senescence or apoptosis in cancer cells. Apoptosis in triple negative breast cancer cells induced by BIBR 1532 is potentiated by glucose restriction.

Биологическая активность

Selective telomerase inhibitor (IC 50 values are 93, > 100000 and > 100000 nM for human telomerase, human RNA polymerase I and human RNA polymerase II + III respectively). Causes telomere shortening in exponentially growing NCI-H460 lung carcinoma cells and eventual growth arrest.