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Zebularine is a DNA methylation inhibitor that forms a covalent complex with DNA methyltransferases, also inhibits cytidinedeaminase with Ki of 2 μM.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | male BALB/c nu/nu mice |
| Formulation | 0.45% saline |
| Dosages | 500 mg/kg, 1000 mg/kg |
| Administration | Intraperitoneal, oral |
| Molecular Weight | 228.2 |
| Formula | C9H12N2O5 |
| CAS Number | 3690-10-6 |
| Solubility (25°C) | DMSO 60 mg/mL Water 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] C B Yoo, et al. Zebularine: a new drug for epigenetic therapy
| Related DNA Methyltransferase Products |
|---|
| Decitabine
Decitabine (5-Aza-2'-deoxycytidine) is a potent inhibitor of DNA methylation for the treatment of myelodysplastic syndromes. |
| RG108
RG108 is a novel small-molecule inhibitors of DNA methyltransferases with IC50 of 115 nM. |
| Lomeguatrib
Lomeguatrib is a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase with IC50 of 5 nM. |
| SGI-1027
SGI-1027 is a DNMT inhibitor with IC50 of 6, 8, 7.5 μM for DNMT1, DNMT3A, and DNMT3B |
| 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. |
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