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:
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