Name: LLY507
Price: 325.00 USD

- Overview
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    Background
    
    IC50: < 15 nMLLY-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.
- Properties
  - Alternative 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
    
    CAS Number
    
    1793053-37-8
    
    Molecular Formula
    
    C36H42N6O
    
    Molecular Weight
    
    574.76
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥57.5 mg/mL in DMSO; insoluble in H2O; ≥54.7 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

LLY507

LLY507

Background

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