LLY507 是一种有效的、细胞活性的、特异性的蛋白质赖氨酸甲基转移酶 SMYD2 抑制剂。它是一种化学探针，用于解析 SMYD2 在癌症和其他生物过程中的功能。它有抑制 SMYD2 甲基化 p53 肽的能力，IC50小于 15 nM。

LLY-507 effectively inhibits the ability of SMYD2 to methylate p53 peptide (IC50<15 nM). LLY-507 is able to potently inhibit the methylation of the H4 peptide by the SMYD2 enzyme (IC50: 31 nM). It has 100-fold selectivity for SMYD2 than 24 other protein or DNA methyltransferases including related family members SMYD3 and SUVH420H1/SUV420H2. LLY-507 inactive (>20 μM) against three cytochrome P450 enzymes, 14 nuclear hormone receptors, 35 G protein-coupled receptors, and 454 kinases. LLY-507 dose-dependently inhibits the proliferation of several liver, esophageal, and breast cancer cell lines.

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

LLY-507 effectively inhibits the ability of SMYD2 to methylate p53 peptide (IC50<15 nm). lly-507 is able to potently inhibit the methylation of h4 peptide by smyd2 enzyme (ic50: 31 it has 100-fold selectivity for than 24 other protein or dna methyltransferases including related family members smyd3 and suvh420h1 suv420h2. inactive (>20 μM) against three cytochrome P450 enzymes, 14 nuclear hormone receptors, 35 G protein-coupled receptors, and 454 kinases. LLY-507 dose-dependently inhibits the proliferation of several liver, esophageal, and breast cancer cell lines.

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.

1793053-37-8

C36H42N6O

574.773

LLY 507;LLY507

DMSO:93 mg/mL (161.8 mM)
H2O:<1 mgml
Ethanol:21 mg/mL (36.5 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years