产品详情
简单介绍:
A-366,G9a/GLPHMTaseInhibitor
详情介绍:
Product Information
Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Purity: | ≥98% |
CAS#: | 1527503-11-2 |
Solubility: | DMSO up to 100 mM |
Chemical Name: | 5'-methoxy-6'-(3-(pyrrolidin-1-yl)propoxy)spiro[cyclobutane-1,3'-indol]-2'-amine |
Molecular Weight: | 329.44 |
Formula: | C19H27N3O2 |
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. 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. http://www.thesgc.org/chemical-probes/A-366
Products are for research use only. Not for human use.
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