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CAS No. : 1561178-17-3
MCE 国际站:SGC0946
产品活性:SGC0946 是一种选择性的 DOT1L (histone 3 lysine 79 methyltransferase) 抑制剂,其 IC50 值为 0.3 nM。SGC0946 可通过抑制 DOT1L,导致 G1 停滞以及抑制癌细胞的自我更新和转移潜力,诱导细胞分化。SGC0946 可用于白血病和乳腺癌的研究,也可作为探针以进一步研究 DOT1L 在正常和病变细胞中的细胞机制。
研究领域:Epigenetics
作用靶点:Histone Methyltransferase
In Vitro: SGC0946 (0-100 µM; 4 days) inhibits DOT1L with IC50 of 2.65 nM in A431 cells.
SGC0946 (1, 5 µM; 14 days) displays selective reduction of cell viability in an experimental leukaemia model derived from human cord blood cells (transformed with the MLL-AF9 fusion oncogene).
SGC0946 (1 µM; 3-7 days) shows time- and dose-dependent reductions in the H3K79me2 mark in the Molm13 MLL cell line that has the MLL/AF9 translocation.
SGC0946 (1 µM, 7 days) effectively inhibits MLL target genes, HOXA9 and Meis1.
SGC0946 (0.2, 2, or 20 μM; 12 days) reduces proliferation and survival of ovarian cancer cells by inhibiting DOT1L enzymatic activity.
SGC0946 (10 μM; 12 days) induces G1 phase arrest by blocking DOT1L in SK-OV-3 and TOV21G cells.
In Vivo: SGC0946 (10 mg/kg; i.p.; twice a week for 6 weeks) significantly suppresses tumor progression in a mouse orthotopic xenograft ovarian cancer model and also inhibits DOT1L enzymatic activity and levels of H3K79me2,CDK6, and cyclin D3 in the tumors.
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