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.
性状
Solid
体外研究(In Vitro)
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. has not independently co
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. Yumi Cho, et al. A histone demethylase inhibitor, methylstat, inhibits angiogenesis in vitro and in vivo. RSC Advances, 2014.[2]. Kac? FN, et al. Synergistic Apoptotic Effects of Bortezomib and Methylstat on Multiple Myeloma Cells. Arch Med Res. 2020 Apr;51(3):187-193.
溶解度数据
In Vitro: DMSO : 100 mg/mL (197.80 mM; Need ultrasonic)配制储备液
[1]. Yumi Cho, et al. A histone demethylase inhibitor, methylstat, inhibits angiogenesis in vitro and in vivo. RSC Advances, 2014.[2]. Kac? FN, et al. Synergistic Apoptotic Effects of Bortezomib and Methylstat on Multiple Myeloma Cells. Arch Med Res. 2020 Apr;51(3):187-193.