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Biological Activity:

A-366 is a novel highly potent, selective and cell permeable G9a/GLP histone lysine methyltransferase inhibitor with an IC₅₀~3.3 nM. It has selectivity > 1000-fold over 21 other methyltransferases. A-366 has been shown to inhibit H3K9 methylation in prostate cancer PC3 cells with an IC₅₀ of 100 nM and exhibits minimal cellular toxicity compared with previous quinazoline-based probes, such as BIX-01294 and UNC0638.

How to Use:

In vitro:  A-366 was used at 1 µM in vitro and cellular assays.

In vivo: n/a

Reference:

1. 1. Sweis RF, et al. Discovery and development of potent and selective inhibitors of histone methyltransferase g9a. (2014) ACS Med Chem Lett. 5(2):205-9.
2. 2. http://www.thesgc.org/chemical-probes/A-366