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LLY-507

CAS No. : 1793053-37-8

產(chǎn)品活性：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.

研究領(lǐng)域：Epigenetics

作用靶點(diǎn)：Histone Methyltransferase

In Vitro: LLY-507 is >100-fold selective for SMYD2 over 21 other methyltransferases including SMYD3.
LLY-507 binds to the substrate channel of SMYD2 and supports the selectivity of its inhibition.
LY-507 is able to potently inhibit the methylation of H4 peptide by SMYD2 enzyme with an IC₅₀ of 31 nM.
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.
LLY-507 (0-20 μM; 3-7 days) inhibits the proliferation of several ESCC, HCC, and breast cancer cell lines.

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