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SGI 1027

Cat. No. 5155 Submit a Review Datasheet / COA / SDS
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Description: DNA methyltransferase inhibitor
Chemical Name: N-[4-[(2-Amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)benzamide
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature (4)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for SGI 1027

SGI 1027 is a 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.

Technical Data for SGI 1027

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for SGI 1027

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 23.08 50

Preparing Stock Solutions for SGI 1027

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.

Select a batch to recalculate based on the batch molecular weight:
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

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References for SGI 1027

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

Citations for SGI 1027

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Literature in this Area

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