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
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.

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

Safety Datasheet

References

References are publications that support the products' biological activity.

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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Keywords: A366 G9a histone methyltransferases potent selective lysine GLP sgc Lysine Methyltransferases

Citations for A 366

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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.

Pathways for A 366

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