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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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| (S)-GSK-3685032
(S)-GSK-3685032 is the inactive isomer of GSK-3685032.GSK-3685032 is a non-time-dependent, non-covalent, first-in-class, reversible selective inhibitor of DNMT1 with an IC50 value of 0.036 μM.GSK-3685032 induces DNA GSK-3685032 induces loss of DNA methylation, transcriptional activation and cancer cell growth inhibition. |
| (R)-GSK-3685032
(R)-GSK-3685032 is the R-isomer of GSK-3685032.GSK-3685032 is a non-time-dependent, non-covalent, first-in-class, reversible selective inhibitor of DNMT1 with an IC50 value of 0.036 μM.GSK-3685032 induces DNA GSK-3685032 induces loss of DNA methylation, transcriptional activation and cancer cell growth inhibition. |
| DNMT-IN-1
DNMT-IN-1 is a potent DNMT inhibitor with an EC50 value of 3.2 µM. |
| DNMT2-IN-1
DNMT2-IN-1 is a potent and selective DNMT2 (DNA methyltransferase 2) inhibitor with an IC50 value of 1.2 μM, and has the potential for mental and metabolic disorders or cancer research. |
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