Description
| Molecular Weight: | 574.76 |
| Formula: | C36H42N6O |
| Purity: | ≥98% |
| CAS#: | 1793053-37-8 |
| Solubility: | DMSO up to 50 mM |
| Chemical Name: | 5-cyano-2'-(4-(2-(3-methyl-1H-indol-1-yl)ethyl)piperazin-1-yl)-N-(3-(pyrrolidin-1-yl)propyl)-[1,1'-biphenyl]-3-carboxamide |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
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.
Products are for research use only. Not for human use.
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