A 366
Chemical Name: 5'-Methoxy-6'-[3-(1-pyrrolidinyl)propoxy]spiro[cyclobutane-1,3'-[3H]indol]-2'-amine
Purity: ≥98%
Biological Activity
A 366 is a 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.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
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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A chemical biology toolbox to study protein methyltransferases and epigenetic signaling.
Scheer et al.
Nat.Commun., 2019;10:19 -
Discovery and development of potent and selective inhibitors of histone methyltransferase G9a.
Sweis et al.
ACS Med.Chem.Lett., 2014;5:205
Product Datasheets
Citation for A 366
The citations listed below are publications that use Tocris products. Selected citations for A 366 include:
1 Citation: Showing 1 - 1
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Pharmacological Targeting of STK19 Inhibits Oncogenic NRAS-Driven Melanomagenesis.
Authors: Xin Et al.
Cell 2019;176:1113-1127.e16
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