LLY-507 is an effective, cell-active, and specific inhibitor of protein-lysine Methyltransferase SMYD2.

SMYD2:15 nM.

LLY-507有效抑制SMYD2对p53肽的甲基化能力（IC50<15 nM）。此外，LLY-507能强效抑制SMYD2酶对H4肽的甲基化（IC50：31 nM），并对SMYD2具有100倍的选择性，相比于其他24种蛋白质或DNA甲基转移酶，包括相关家族成员SMYD3及SUVH420H1/SUV420H2。LLY-507对三种细胞色素P450酶无活性（>20 μM），对14种核激素受体、35种G蛋白偶联受体和454种激酶同样无活性。LLY-507剂量依赖性地抑制多种肝癌、食道癌和乳腺癌细胞系的增殖。

To examine the methylation status of p53 in HEK293 cells treated with LLY-507 by Western blotting, 2 × 105 cells are seeded in 6-well plates in triplicate and co-transfected with FLAG-tagged p53 and FLAG-tagged SMYD2 using Lipofectamine? 2000. The day after transfection, cells are treated with 0-2.5 μM LLY-507 for 28 h, then collected, and lysed in RIPA buffer. Cell lysates are subject to 10% SDS-PAGE and transferred to a PVDF membrane.