化合物LLY507 T6879

Product Introduction
Bioactivity


英文名: LLY-507

描述: LLY-507 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。

细胞实验: 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.

体外活性: 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 93 mg/mL (161.8 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 21 mg/mL (36.5 mM)


关键字: protein | inhibit | methyltransferase | methylation | breast | cancer | SMYD2 | p53 | Inhibitor | Histone Methyltransferase | LLY-507 | epigenetics

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相关库: Anti-Aging Compound Library | Inhibitor Library | Epigenetics Compound Library | Anti-Cancer Active Compound Library | Highly Selective Inhibitor Library | Reprogramming Compound Library | Stem Cell Differentiation Compound Library | NO PAINS Compound Library | Histone Modification Compound Library | Chromatin Modification Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途