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].
体内研究
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.
体外研究
SGC0946 demonstrates a capacity to inhibit DOT1L activity with an IC50 of 2.65 nM in A431 cells over a period of 4 days at concentrations ranging from 0 to 100 μM[1].
When administered at 1 and 5 μM for 14 days, SGC0946 selectively diminishes cell viability in a leukaemia model derived from human cord blood cells harboring the MLL-AF9 fusion gene[1].
At a concentration of 1 μM over 3 to 7 days, SGC0946 progressively diminishes the H3K79me2 mark in the Molm13 MLL cell line, which possesses the MLL/AF9 translocation[1].
With a 7-day treatment of 1 μM, SGC0946 effectively downregulates the expression of MLL target genes, namely HOXA9 and Meis1[1].
Through 12 days of treatment with SGC0946 at doses of 0.2, 2, or 20 μM, the proliferation and survival of ovarian cancer cells are curtailed by the inhibition of DOT1L's enzymatic function[2].
Employing 10 μM of SGC0946 for 12 days results in G1 phase arrest in SK-OV-3 and TOV21G cells by targeting DOT1L[2].
SGC0946 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 MCF10A cells
Function assay
Inhibition of DOT1L in human MCF10A cells assessed as reduction of H3K79 level, IC50=0.0088 μM
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