产品详情
简单介绍：
GSK591(EPZ015866),PRMT5Inhibitor
详情介绍：
Product Information
| Molecular Weight: | 380.48 |
| Formula: | C22H28N4O2 |
| Purity: | ≥98% |
| CAS#: | 1616391-87-7 |
| Solubility: | DMSO and EtOH up to 100 mM |
| Chemical Name: | (S)-2-(cyclobutylamino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)isonicotinamide |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
GSK591 (EPZ015866) is a potent and selective Protein arginine methyltransferase-5 (PRMT5) Inhibitor with IC50 of 11 nM. It is selective for PRMT5 (up to 50 micromolar) relative to a panel of methyltransferases. It potently inhibits the PRMT5/MEP50 complex from methylating (histone) H4. In Z-138 cells, GSK591 inhibits the symmetric arginine methylation of SmD3 with EC50 of 56 nM. Further, GSK591 is selective for PRMT5 (up to 50 micromolar) relative to a panel of methyltransferases
How to Use:
In vitro: GSK591 was used at 1-10 µM final concentration in various in vitro assays.
In vivo: n/a
Reference:
- 1. Duncan KW, et al. Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666. (2015) ACS Med Chem Lett. 7(2):162-6.
- 2. http://www.thesgc.org/chemical-probes/GSK591
Products are for research use only. Not for human use.
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