LLY507 |
Catalog No.GC16261 |
LLY507 est un inhibiteur puissant et sélectif de la protéine-lysine méthyltransférase SMYD2. LLY507 inhibe puissamment la capacité de SMYD2 à méthyler le peptide p53 avec une IC50 \u003c15 nM. LLY507 sert de sonde chimique précieuse pour aider à la dissection de la fonction SMYD2 dans le cancer et d'autres processus biologiques.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1793053-37-8
Sample solution is provided at 25 µL, 10mM.
IC50: < 15 nM
LLY-507 is a potent inhibitor of SMYD2.
SMYD2, a lysine methyltransferase, catalyzes the monomethylation of several protein substrates including p53. SMYD2 is reported to be overexpressed in a significant percentage of esophageal squamous primary carcinomas, and such overexpression related with poor patient survival.
In vitro: LLY-507 has been identified as a cell-active, potent small molecule inhibitor of SMYD2. LLY-507 was found to be >100-fold selective for SMYD2 over a broad range of methyltransferase and non-methyltransferase targets. The crystal structure of SMYD2 in complex with LLY-507 showed it bound in the substrate peptide binding pocket. LLY-507 was active in cells as demonstrated by the reduction of SMYD2-induced monomethylation of p53 Lys(370) at submicromolar concentrations. Furthermore, MS-based proteomics indicated that cellular histone methylation levels were not affected by SMYD2 inhibition with LLY-507 significantly, and subcellular fractionation studies showed that SMYD2 was primarily cytoplasmic, indicating that SMYD2 targeted a small subset of histones. Moreover, LLY-507 was able to inhibit the proliferation of several liver, esophageal, as well as breast cancer cell lines in a dose-dependent manner [1].
In vivo: So far, there is no animal data reported.
Clinical trial: Up to now, LLY-507 is still in the preclinical development stage.
Reference:
[1] Nguyen H, et al. LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2. J Biol Chem. 2015 May 29;290(22):13641-13653.
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