Zebularine 3690-10-6

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Molecular Weight:

228.2 Zebularine is a DNA methylation inhibitor that forms a covalent complex with DNA methyltransferases, also inhibits cytidinedeaminase with Ki of 2 μM.






Biological Activity


Zebularine is a cytidine analogue containing a 2-(1H)-pyrimidinone ring,
originally synthesized as a cytidine deaminase inhibitor. Zebularine is shown to form a tight, covalent complex with bacterial methyltransferases. 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. 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.


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.

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Product Categories : Epigenetics > DNA Methyltransferase Inhibitor