A selective

LLY-507 – 5 mg

Brand:
Cayman
CAS:
1793053-37-8
Storage:
-20
UN-No:
Non-Hazardous - /

SMYD2 is a lysine N-methyltransferase that methylates both histones and non-histone proteins, including p53 and retinoblastoma-associated protein.{21355,23894} LLY-507 is a cell-active, small molecule inhibitor of SMYD2 (IC50 = 15 nM).{16441} It has been shown to inhibit p53 lysine370 monomethylation in KYSE-150 esophageal squamous cell carcinoma cells stably expressing SMYD2 with an IC50 value of 0.6 µM.{16441} LLY-507 is >100-fold selective for SMYD2 over a panel of 27 protein methyltransferases and non-methyltransferase targets.{16441} See the Structural Genomics Consortium (SGC) website for more information.  

 

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Description

A selective, cell-active, small molecule inhibitor of SMYD2 (IC50 = 15 nM); inhibits p53 lysine370 monomethylation in KYSE-150 esophageal squamous cell carcinoma cells stably expressing SMYD2 with an IC50 value of 0.6 µM

Formal name: 5-cyano-2′-[4-[2-(3-methyl-1H-indol-1-yl)ethyl]-1-piperazinyl]-N-[3-(1-pyrrolidinyl)propyl]-[1,1′-biphenyl]-3-carboxamide

Synonyms: 

Molecular weight: 574.8

CAS: 1793053-37-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Demethylases||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Methylation

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