LLY507 |
Catalog No.GC16261 |
LLY507 es un inhibidor potente y selectivo de la proteína-lisina metiltransferasa SMYD2. LLY507 inhibe potentemente la capacidad de SMYD2 para metilar el péptido p53 con una IC50 \u003c15 nM. LLY507 sirve como una valiosa sonda química para ayudar en la disección de la función SMYD2 en el cáncer y otros procesos biológicos.
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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