A 366

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Cat.No. 5163 - A 366 | C19H27N3O2 | CAS No. 1527503-11-2
Description: Potent and selective G9a/GLP inhibitor
Chemical Name: 5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC50 = 3.3 nM). Exhibits >1000-fold selectivity for G9a/GLP over 21 other methyltransferases. Decreases levels of lysine 9 dimethylation on histone H3 (H3K9Me2) in PC3 cells.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the A 366 probe summary on the SGC website.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of A 366 is reviewed on the chemical probes website.

Compound Libraries

A 366 is also offered as part of the Tocriscreen Plus and Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 329.44
Formula C19H27N3O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1527503-11-2
PubChem ID 76285486
InChI Key BKCDJTRMYWSXMC-UHFFFAOYSA-N
Smiles COC1=C(OCCCN4CCCC4)C=C(N=C(N)C32CCC3)C2=C1

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
1eq. HCl 32.94 100
DMSO 32.94 100

Preparing Stock Solutions

The following data is based on the product molecular weight 329.44. 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 3.04 mL 15.18 mL 30.35 mL
5 mM 0.61 mL 3.04 mL 6.07 mL
10 mM 0.3 mL 1.52 mL 3.04 mL
50 mM 0.06 mL 0.3 mL 0.61 mL

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References

References are publications that support the biological activity of the product.

Sweis et al (2014) Discovery and development of potent and selective inhibitors of histone methyltransferase G9a. ACS Med.Chem.Lett. 5 205 PMID: 24900801


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View all G9a/GLP Inhibitors

Keywords: A 366, A 366 supplier, A366, G9a, histone, methyltransferases, potent, selective, lysine, GLP, sgc, Lysine, Methyltransferases, G9a/GLP, 5163, Tocris Bioscience

Citations for A 366

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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!

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Cancer

Cancer Research Product Guide

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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:

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  • Histone Demethylases
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Epigenetics in Cancer Poster

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