BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay[1]. BIBR 1532 inhibits telomerase activity in a non-competitive manner[1]. BIBR 1532 reduces the proliferation of JVM13 leukemia cells, achieving an IC50 of 52 μM, a similar inhibition observed in other leukemia lines like Nalm-1, HL-60, and Jurkat. BIBR 1532's antiproliferative effects on acute myeloid leukemia (AML) are noted with an IC50 of 56 μM, while it does not affect the proliferative ability of normal hematopoietic progenitor cells[2]. At a concentration of 2.5 μM, BIBR 1532 diminishes colony-forming ability, induces telomere shortening, and sensitizes cells to chemotherapy by inhibiting telomerase activity in both MCF-7/WT and MCF-7/MlnR cell lines resistant to melphalan[3]. BIBR 1532 exhibits dose-dependent cytotoxicity in T-cell prolymphocytic leukemia (T-PLL)[4]. When combined with carboplatin, BIBR 1532 eradicates spheroid-forming ovarian cancer cells in ES2, SKOV3, and TOV112D cell lines[5].
体外研究
BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay[1].
BIBR 1532 inhibits telomerase activity in a non-competitive manner[1].
BIBR 1532 reduces the proliferation of JVM13 leukemia cells, achieving an IC50 of 52 μM, a similar inhibition observed in other leukemia lines like Nalm-1, HL-60, and Jurkat. BIBR 1532's antiproliferative effects on acute myeloid leukemia (AML) are noted with an IC50 of 56 μM, while it does not affect the proliferative ability of normal hematopoietic progenitor cells[2].
At a concentration of 2.5 μM, BIBR 1532 diminishes colony-forming ability, induces telomere shortening, and sensitizes cells to chemotherapy by inhibiting telomerase activity in both MCF-7/WT and MCF-7/MlnR cell lines resistant to melphalan[3].
BIBR 1532 exhibits dose-dependent cytotoxicity in T-cell prolymphocytic leukemia (T-PLL)[4].
When combined with carboplatin, BIBR 1532 eradicates spheroid-forming ovarian cancer cells in ES2, SKOV3, and TOV112D cell lines[5].
BIBR 1532 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
human HeLa cells
Function assay
2 h
Inhibition of telomerase in human HeLa cells after 2 hrs by [alpha-32P]dGTP incorporation assay, IC50=93 nM
22413845
human MDA-MB-231 cells
Function assay
24 h
Inhibition of telomerase in human MDA-MB-231 cells after 24 hrs by TRAP-PCR-ELISA, IC50=0.17 μM
25965778
human MGC803 cells
Function assay
24 h
Inhibition of telomerase in human MGC803 cells after 24 hrs by TRAP-PCR-ELISA, IC50=0.28 μM
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