tcsc0902 BIBR 1532

BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC₅₀ of 100 nM in a cell-free assay.

IC50 & Target: IC50: 100 nM (telomerase)

In Vitro: BIBR 1532 non-competitively inhibits telomerase activity^[1]. BIBR 1532 inhibits the proliferation of JVM13 leukemia cells with an IC₅₀ of 52 μM, and similar effect also occurs in other leukemia cell lines such as Nalm-1, HL-60, and Jurkat. BIBR 1532 exerts antiproliferative effect on acute myeloid leukemia (AML) with IC₅₀ of 56 μM with no effect on the proliferative capacity of normal hematopoietic progenitor cells^[2]. BIBR 1532 (2.5 μM) reduces colony-forming ability, induces telomere length shortening and causes chemotherapeutic sensitization via inhibiting telomerase activity in MCF-7/WT and melphalan-resistant MCF-7/MlnR cell lines^[3]. BIBR 1532 is cytotoxic in a dose-dependent manner in T-cell prolymphocytic leukemia (T-PLL)^[4]. BIBR 1532 in combination with carboplatin (a chemotherapeutic agent) eliminates ovarian cancer spheroid-forming cells in ES2, SKOV3, and TOV112D cell lines^[5].