Molecular Formula | C27H23N7O
|
Molar Mass | 461.52 |
Density | 1.387±0.06 g/cm3(Predicted) |
Melting Point | >280℃ |
Solubility | Soluble in DMSO, not in water |
Appearance | powder |
Color | white to light brown |
pKa | 13.31±0.70(Predicted) |
Storage Condition | 2-8°C |
Stability | Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
Use | SGI-1027, a DNA methyltransferase (DNMT) inhibitor, had IC50 values of 7.5 μM,8 μM and 12.5 μM for DNMT3B,DNMT3A and DNMT1 with poly(dI-dC) as substrate, respectively. |
In vitro study | SGI-1027 inhibits DNA methylation by direct inhibition of DNMTs and leads to selective degradation of DNMT1 in various human cancer cell lines. SGI-1027 showed little or no toxic effect in rat hepatoma H4IIE cells. SGI-1027 (0-100 μm) exhibited a modest pro-apoptotic effect in the U937 human leukemia cell line with no associated changes in the cell cycle. |