SGI 1027

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Cat.No. 5155 - SGI 1027 | C27H23N7O | CAS No. 1020149-73-8
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
Literature

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.

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

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Reconstitution Calculator

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Dilution Calculator

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Product Datasheets

Safety Datasheet

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


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

Citations for SGI 1027

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Epigenetics

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

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:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases

Pathways for SGI 1027

Protocols

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