A 366

Cat. No. 5163

A 366 C19H27N3O2 [1527503-11-2]

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Chemical Name: 5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine

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.

Technical Data

M.Wt:
329.44
Formula:
C19H27N3O2
Solubility:
Soluble to 100 mM in 1eq. HCl and to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
1527503-11-2

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 Data Sheet

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: A 366, supplier, A366, G9a, histone, methyltransferases, potent, selective, lysine, GLP, sgc, Tocris Bioscience, Lysine Methyltransferase Inhibitor products

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