Description
Details
3-Deazaneplanocin A (DZNep) acts as an epigenetic modifier that inhibits histone methyltransferases and decreases global DNA methylation. It is a competitive inhibitor of S-adenosylhomocysteine hydrolase (Ki = 50 pM). It has been specifically shown to inhibit EZH2 protein expression which reduces the trimethylation of lysine 27 on histone H3. When used in combination with other compounds, DZNep can enable chemical reprogramming of mouse embryonic fibroblasts to iPSCs by increasing Oct4 expression.
Details
Details
Molecular Weight | 262.26 |
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Molecular Formula | C12H14N4O3 |
Chemical Name | (1S,2R,5R)-5-(4-aminoimidazo[4,5-c]pyridin-1-yl)-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol |
CAS Number | 102052-95-9 |
PubChem Identifier | 73087 |
Appearance | Colorless liquid |
Purity | >97% by HPLC analysis |
Size | 400 μL, 10 mM in DMSO |
Alternative Names | DZNep |
Storage and Stability | Store at -20°C. Stable for 6 months when stored as directed. Avoid repeated freeze-thaw cycles. |
References | Hou, P., et al. (2013) Pluripotent stem cells induced from mouse somatic cells by small-molecule compounds. Science 341(6146): 651-654. PMID: 23868920. Miranda, T.B., et al. (2009) DZNep is a global histone methylation inhibitor that reactivates developmental genes not silenced by DNA methylation. Mol Cancer Ther 8(6): 1579-1588. PMID: 19509260. Tan, J., et al. (2007) Pharmacologic disruption of Polycomb-repressive complex 2-mediated gene repression selectively induces apoptosis in cancer cells. Genes Dev 21(9): 1050-1063. PMID: 17437993. Tseng, C.K., et al. (1989) Synthesis of 3-deazaneplanocin A, a powerful inhibitor of S-adenosylhomocysteine hydrolase with potent and selective in vitro and in vivo antiviral activities. J Med Chem 32(7): 1442-1446. PMID: 2544721. |
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