SGI 1027

Cat. No. 5155

SGI 1027 C27H23N7O [1020149-73-8]

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Chemical Name: N-[4-[(2-Amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)benzamide

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.

Technical Data

M.Wt:
461.52
Formula:
C27H23N7O
Solubility:
Soluble to 50 mM in DMSO
Purity:
>99 %
Storage:
Store at -20°C
CAS No:
1020149-73-8

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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.

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.

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Keywords: SGI 1027, supplier, SGI1027, DNA, methyltransferase, inhibitors, inhibits, DNMT, TSGs, tumour, suppressor, genes, CpG, island, hypermethylation, Tocris Bioscience, DNA Methyltransferase Inhibitor products

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