DNA methyltransferase inhibitor. Inhibits the mammalian DNA methyltransferases DNMT3B, DNMT3A and DNMT1 (IC50 values are 7.5, 8 and 12.5 μM with Poly(dl-dC) as the substrate). Reactivates silenced tumor suppressor genes by reducing CpG island hypermethylation.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 461.52. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||4.33 mL||21.67 mL||43.34 mL|
|2.5 mM||0.87 mL||4.33 mL||8.67 mL|
|5 mM||0.43 mL||2.17 mL||4.33 mL|
|25 mM||0.09 mL||0.43 mL||0.87 mL|
References are publications that support the biological activity of the product.
Datta et al (2009) A new class of quinoline-based DNA hypomethylating agents reactivates tumor suppressor genes by blocking DNA methyltransferase 1 activity and inducing its degradation. Cancer Res. 69 4277 PMID: 19417133
García-Domínguez et al (2013) Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line. Bioorg.Med.Chem.Lett. 23 1631 PMID: 23402879
If you know of a relevant reference for SGI 1027, please let us know.
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Keywords: SGI 1027, SGI 1027 supplier, SGI1027, DNA, methyltransferase, inhibitors, inhibits, DNMT, TSGs, tumour, suppressor, genes, CpG, island, hypermethylation, Methyltransferases, 5155, Tocris Bioscience
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics Research Bulletin
Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:
- DNA Methyltransferases
- Histone Deacetylases
- Histone Demethylases
- Histone Methyltransferases