SGC0946 is a selective inhibitor of DOT1L methyltransferase with IC50 of 0.3 nM and can kill mixed lineage leukaemia cells.
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SGC0946 is a selective DOT1LH3K79 methyltransferase) inhibitor, with an IC50 of 0.3 nM. SGC0946 results in G1 arrest, inhibit potential of cell self-renewal and metastatic, and also induces cell differentiation. SGC0946 can be used in studies of leukemia and solid tumors and also serve as a probe to further investigate the cellular mechanism of DOT1L in both normal and diseased cells[1].[2].[3].
SGC0946 细胞研究
细胞系
浓度
检测类型
检测时间
活性说明
数据源
human MCF10A cells
Function assay
Inhibition of DOT1L in human MCF10A cells assessed as reduction of H3K79 level, IC50=0.0088 μM
25406853
SGC0946 动物研究
Animal study
Administering SGC0946 at 10 mg/kg intraperitoneally twice weekly for six weeks notably hinders tumor growth in a mouse model of orthotopic xenograft ovarian cancer, while concurrently reducing DOT1L enzymatic action and the levels of H3K79me2, CDK6, and cyclin D3 within the tumors.
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