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SGI-1027 is a DNMT inhibitor with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B
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Source | Front Neurosci (2016). Figure 6. SGI-1027 |
| Method | RT-PCR | |
| Cell Lines | Magnetic-Activated Cell Sorting | |
| Concentrations | 10 μM | |
| Incubation Time | 24 h | |
| Results | Our results show that SGI-1027 allows the sustained expression of Oct4 after retinal injury, only in the GLAST-positive fraction of retinas |
| Cell Experiment | |
|---|---|
| Cell lines | Rat hepatoma H4IIE cells |
| Preparation method | Using the rat hepatoma H4IIE cells as the test system. These cells are grown in DMEM which is supplemented with fetal bovine serum (10%) and calf serum (10%). Cells are seeded into 96-well plates , 48 h later exposed them to SGI-1027 ,which concentrations are ranging from 0 to 300 µmol/L. The solubility is determined by Nephalometry techniques immediately after dosing and before harvesting the cells at 24 h. Following the exposure period, the cells or their supernatant (culture medium) are analyzed for changes in cell proliferation (propidium iodide), membrane leakage (α-GST), mitochondrial function [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and cellular ATP], oxidative stress (intracellular GSH and 8-isoprostane), and apoptosis. Determine the half-maximal toxic concentration (TC50) from the dose-response curves. |
| Concentrations | ~300 μM |
| Incubation time | 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 461.52 |
| Formula | C27H23N7O |
| CAS Number | 1020149-73-8 |
| Solubility (25°C) | DMSO 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| Lomeguatrib
Lomeguatrib is a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase with IC50 of 5 nM. |
| SGI-110
SGI-110 (S-110) is a stable and potent inhibitor for DNA methylation, inhibits DNMT1 when SGI-110 is activated by phosphorylation and incorporated into DNA. |
| Zebularine
Zebularine is a DNA methylation inhibitor that forms a covalent complex with DNA methyltransferases, also inhibits cytidinedeaminase with Ki of 2 μM. |
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