LLY-507 

LLY-507 is a potent and selective inhibitor of protein-lysine methyltransferase SMYD2. LLY-507 potently inhibits the ability of SMYD2 to methylate p53 peptide with an IC₅₀ <15 nM. LLY-507 serves as a valuable chemical probe to aid in the dissection of SMYD2 function in cancer and other biological processes^[1].

LLY-507 is >100-fold selective for SMYD2 over 21 other methyltransferases including SMYD3^[1].
LLY-507 binds to the substrate channel of SMYD2 and supports the selectivity of its inhibition^[1].
LY-507 is able to potently inhibit the methylation of H4 peptide by SMYD2 enzyme with an IC₅₀ of 31 nM^[1].
LLY-507 (0.03-20 μM; 28 hours) inhibits SMYD2-mediated methylation of p53 Lys³⁷⁰ in U2OS cells, with an IC₅₀ of 0.6 μM^[1].
LLY-507 (0-20 μM; 3-7 days) inhibits the proliferation of several ESCC, HCC, and breast cancer cell lines^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

574.76

C₃₆H₄₂N₆O

1793053-37-8

Solid

White to off-white

O=C(C1=CC(C2=CC=CC=C2N3CCN(CCN4C=C(C)C5=C4C=CC=C5)CC3)=CC(C#N)=C1)NCCCN6CCCC6

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

• [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.  [Content Brief]