Biological Activity
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.
Compound Libraries
SGI 1027 is also offered as part of the Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 461.52 |
| Formula | C27H23N7O |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1020149-73-8 |
| PubChem ID | 24858111 |
| InChI Key | QSYLKMKIVWJAAK-UHFFFAOYSA-N |
| Smiles | O=C(NC4=CC=C(NC5=NC(N)=NC(C)=C5)C=C4)C(C=C3)=CC=C3NC2=CC=NC1=CC=CC=C12 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 23.08 | 50 |
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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.17 mL | 10.83 mL | 21.67 mL |
| 5 mM | 0.43 mL | 2.17 mL | 4.33 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.17 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
Molarity Calculator
Reconstitution Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: SGI 1027, supplier, SGI1027, DNA, methyltransferase, inhibitors, inhibits, DNMT, TSGs, tumour, suppressor, genes, CpG, island, hypermethylation, DNA, Methyltransferases, DNA, Methyltransferases, Tocris Bioscience
