LLY-507,Protein-lysineMethyltransferaseSMYD2Inhibitor

Biological Activity:

LLY-507 is a potent, selective and cell permeable protein lysine methyltransferase SMYD2 inhibitor with IC50 <15 nM. It binds in the substrate peptide-binding pocket. It has >100-fold selectivity over other methyltransferases and other non-epigenetic targets. LLY-507 has been shown to inhibit p53K370 monomethylation in cells with an IC50 ~600 nM. It inhibited the proliferation of several esophageal, liver, and breast cancer cell lines in a dose-dependent manner. LLY-507 serves as a valuable chemical probe to aid in the dissection of SMYD2 function in cancer and other biological processes.

How to Use:

In vitro: LLY-507 was used at 10 µM final concentration in various in vitro assays.
In vivo: n/a

Reference:

• 1. Nguyen H, et al. LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2. (2015) J Biol Chem. 290(22):13641-53. 

产品留言

标题

联系人

联系电话

内容

验证码

点击换一张

注：1.可以使用快捷键Alt+S或Ctrl+Enter发送信息!
2.如有必要,请您留下您的详细联系方式!