BIBR1532

**BIBR1532** is a synthetic, non-nucleosidic small molecule that acts as a potent and selective *telomerase inhibitor* (IC50 ~93 nM)[1][5]. It targets the human telomerase reverse transcriptase (hTERT), inhibiting telomerase activity via mixed-type non-competitive inhibition, resulting in interference with the enzyme's processivity[5]. This inhibition leads to telomere shortening, cellular senescence, growth arrest, and apoptosis in a variety of human cancer cell types including leukemia, multiple myeloma, squamous cell carcinoma, and endometrial carcinoma[1][2][3][4][6][7][8]. BIBR1532 downregulates TERT and c-MYC expression, destabilizes survival pathways via PI3K/AKT/mTOR and ERK/MAPK modulation, induces DNA damage response (DDR) including γ-H2AX, and upregulates cell cycle inhibitors (such as p21) and apoptotic proteins (Bax/Bcl-2 ratio)[2][3][4][8]. It also exhibits synergy with chemotherapeutics such as doxorubicin, bortezomib, paclitaxel, and arsenic trioxide[2][8].

Other names

2-[[(E)-3-naphthalen-2-ylbut-2-enoyl]amino]benzoic acid