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GSK591(EPZ015866),PRMT5Inhibitor

品牌：Xcessbio

貨號(hào)：M60321-2s

規(guī)格：2 mg solid

貨期：

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GSK591(EPZ015866),PRMT5Inhibitor

商品詳情參考文獻(xiàn) 相關(guān)資料

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: 4^oC 1 year. DMSO: 4^oC 3 month; -20^oC 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

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