Antibodies
Zebularine
- 貨號 Cat. No.
- S7113
- 規格 Size
- 10mM/1mL~50mg
- 品牌 Brand
- Selleckchem
Description
Zebularine
Catalog No.S7113
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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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | 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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| Targets | DNA methyltransferase | cytidine deaminase | ||||
| IC50 | 2 μM (Ki)[2] | |||||
| In vitro | Zebularine is a cytidine analogue containing a 2-(1H)-pyrimidinone ring, originally synthesized as a cytidine deaminase inhibitor. [2] Zebularine is shown to form a tight, covalent complex with bacterial methyltransferases. [1] In N. crassa, zebularine inhibits DNA methylation and reactivates a gene previously silenced by methylation. Zebularine is a global inhibitor of DNA methylation, similar to 5-Aza-CR, rather than a selective inhibitor. Zebularine induces the myogenic phenotype in 10T1/2 cells, which is a phenomenon unique to DNA methylation inhibitors. Zebularine reactivates a silenced p16 gene and demethylates its promoter region in T24 bladder carcinoma cells. Zebularine is only slightly cytotoxic to T24 cells. [3] Zebularine is preferentially incorporated into DNA and exhibits greater cell growth inhibition and gene expression in cancer cell lines compared to normal fibroblasts. In addition, zebularine preferentially depletes DNA methyltransferase 1 (DNMT1) and induces expression of cancer-related antigen genes in cancer cells relative to normal fibroblasts. [4] | |||||
| In vivo | Zebularine is only slightly cytotoxic to tumor-bearing mice (average maximal weight change in mice treated with 1000 mg/kg zebularine = 11% [95% CI = 4% to 19%]). Compared with those in control mice, tumor volumes are statistically significantly reduced in mice treated with high-dose zebularine administered by intraperitoneal injection or by oral gavage. [3] | |||||
| Features | Very stable with half-life of ~44 h at 37°C in PBS at pH 1.0 and approx. 508 h at pH 7. | |||||
Protocol(Only for Reference)
Animal Study: [3]
| Animal Models | male BALB/c nu/nu mice |
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| Dosages | 500 mg/kg, 1000 mg/kg |
| Administration | Intraperitoneal, oral |
| Solubility | Saline, 30 mg/mL |
References
Chemical Information
| Molecular Weight (MW) | 228.2 |
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| Formula | C9H12N2O5 |
| CAS No. | 3690-10-6 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 46 mg/mL (201 mM) |
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| Water | 46 mg/mL (201 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | Saline, | 30 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 2(1H)-Pyrimidinone, 1-β-D-ribofuranosyl- |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.2282 | 2.282 | 4.564 | 6.846 |
