DY-46-2

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

DY-46-2 是一种高效、选择性高的新型非核苷 DNA 甲基转移酶 3A (DNMT3A) 抑制剂，其IC50 值为 1.3 μM。

DY-46-2 is a high potency and selectivity novel non-nucleoside DNA methyltransferase 3A (DNMT3A) inhibitor with an IC50 value of 0.39 μM.

DY-46-2 (0.1-100 μM, 24, 48 and 72 h) has an inhibitory activity of DNMT3A with an IC50 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 IC50 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 IC50 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.Cell Viability Assay Cell 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 (IC50 >100 μM).Cell Proliferation Assay Cell 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 Analysis Cell 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).

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Cell Cycle/DNA Damage

DNA/RNA Synthesis

DNA Methyltransferase

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1105110-83-5

446.48

C19H22N6O5S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (111.99 mM; 超声助溶 )

O=C(NC1=CN=C(C=C1)S(=O)(=O)N)C2=C(OC=3N=CN(C(=O)C32)CCN4CCCC4)C

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(-20℃)

With Ice Pack

≥ 2 years