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 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] C B Yoo, et al. Zebularine: a new drug for epigenetic therapy
| Related DNA Methyltransferase Products |
|---|
| (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. |
| Guadecitabine
Guadecitabine (SGI-110) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS). |
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