DY-46-2 (C09-1126-308)

DY-46-2 is a high potency and selectivity novel non-nucleoside DNA methyltransferase 3A (DNMT3A) inhibitor with an IC 50 value of 0.39 μMIn VitroDY-46-2 (0.1-100 μM, 24, 48 and 72 h) has an inhibitory activity of DNMT3A with an IC 50 value of 0.39 μM, which increases linearly with DNA concentration (IDT-01). DY-46-2 (0.1-100 μM, 24, 48 and 72 h) has inhibitory activity against DNMT1, DNMT3B and G9a with IC 50 values of 13.0 μM, 105 μM and ＞500 μM, respectively. DY-46-2 (0.1-100 μM, 24, 48 and 72 h) has cell viability in cancer cells with IC 50 values of 0.7 μM, 0.3 μM, 0.7 μM, 0.5 μM, 2.1 μM, 1.7 μM and 91 μM for THP-1, HCT116, U937, K562, A549, DU145 and PBMC cell, respectively. DY-46-2 (0.1-100 μM, 24, 48 and 72 h) markedly inhibits the proliferation of cancer cells and shows low cytotoxicity in peripheral blood mononuclear cells (PBMCs). DY-46-2 (1 μM, 72 h) obviously decreases DNMT3A protein levels, as well as reactive expression of a silenced TSG (p53) in HCT116 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: THP-1, HCT116, U937, K562, A549, DU145 and PBMC cell Concentration: 0.1-100 μM Incubation Time: 24, 48 and 72 h Result: Had remarkable inhibitory potency in the dose- and time-dependent manners and no cytotoxicity in non-tumoral PBMCs (IC 50 >100 μM). Cell Proliferation AssayCell Line: THP-1, HCT116, U937, K562, A549, DU145 and PBMC cell Concentration: 0.1-100 μM Incubation Time: 24, 48 and 72 h Result: Exhibited high anti-proliferative activity with a micromolar range cytotoxicity in all cancer cells. Western Blot AnalysisCell Line: HCT116 cells Concentration: 1 μM Incubation Time: 72 h Result: Decreased DNMT3A and p53 protein levels in the HCT116 cells, apparently sufficient to reactive expression of a silenced TSG (p53).Form:SolidIC50& Target:DNMT3A 0.39 μM (IC 50 ). Specification: 0.98 Molecular Formula: C19H22N6O5S Molecular Weight: 446.48