Bioactivity | 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[1][2]. |
Invitro | Methylstat (0-5 µM; 48, 72 h) shows anti-proliferative activity with no cytotoxicity on HUVECs at 1-2 µM[1].Methylstat (0, 1, 2 µM; 48 h) induces cell cycle arrest at G0/G1 phase in a dose-dependent manner[1].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[1].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[1].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[2]. Cell Cytotoxicity Assay[1] Cell Line: |
Name | Methylstat |
CAS | 1310877-95-2 |
Formula | C28H31N3O6 |
Molar Mass | 505.56 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |