产品
编 号:F115917
分子式:C28H31N3O6
分子量:505.56
产品类型
结构图
CAS No: 1310877-95-2
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产品详情
生物活性:
Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis.
体外研究:
Methylstat (0-5 μM; 48, 72 h) shows anti-proliferative activity with no cytotoxicity on HUVECs at 1-2 μM.Methylstat (0, 1, 2 μM; 48 h) induces cell cycle arrest at G0/G1 phase in a dose-dependent manner.Methylstat (0, 1, 2 μM; 48 h) increases the expression of p53 mRNA levels, the H3K27 methylation levels and the accumulation of p53 and p21 protein levels, but suppresses the protein level of cyclinD1.Methylstat (0, 1, 2 μM) shows anti-angiogenic activity induced by VEGF, bFGF and TNF-α in HUVEC cells, and inhibits the f capillary formation during CAM (chick embryo chorioallantoic membrane) development without any sign of thrombosis and hemorrhage.Methylstat (1.1, 2.2 mM for U266 cells, 2.1, 4.2 mM for ARH77 cells; 72 h) induces apoptosis significantly in U266 and ARH77 cells.