DNMT1-IN-5 is a selective inhibitor targeting DNA methyltransferases DNMT1 and DNMT3A, with IC50 values of 2.42 μM and 14.4 μM, respectively. This compound demonstrates significant antiproliferative activity across various cancer cell lines, exhibiting IC50 values ranging from 0.19 to 2.37 μM in TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226, and HCT116. In addition to inducing cell cycle arrest at the G2/M phase, DNMT1-IN-5 promotes apoptosis in TMD-8 and DOHH2 cells and has shown antitumor efficacy in xenograft mouse models.
DNMT1-IN-5 is a selective inhibitor targeting DNA methyltransferases DNMT1 and DNMT3A, with IC50 values of 2.42 μM and 14.4 μM, respectively. This compound demonstrates significant antiproliferative activity across various cancer cell lines, exhibiting IC50 values ranging from 0.19 to 2.37 μM in TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226, and HCT116. In addition to inducing cell cycle arrest at the G2/M phase, DNMT1-IN-5 promotes apoptosis in TMD-8 and DOHH2 cells and has shown antitumor efficacy in xenograft mouse models.
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