|5-氰基-2'-(4-(2-(3-甲基-1H-吲哚-1-基)乙基)哌嗪-1-基)-N-(3-(吡咯烷-1-基)丙基)-[1,1'-联苯] -3-酰胺|CsnPharm

CAS No.: 1793053-37-8

LLY-507 Catalog No. CSN18032

Synonyms: LLY-507

LLY-507 is a potent and selective protein-lysine methyltransferase SMYD2 inhibitor with IC50 <15 nM, which can inhibit p53K370 monomethylation in cells with an IC50 ~600 nM.

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400-920-2911

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技术信息

生物活性

描述LLY-507 is a potent and selective SMYD2 inhibitor with IC50 value <15nM, >100-fold selective for SMYD2 over a broad range of methyltransferase and non-methyltransferase targets. LLY-507 inhibited SMYD2-induced p53 methylation in U2OS cells with an IC50 of 0.6μM. Inhibition of SMYD2 by LLY-507 did not significantly affect cellular global histone methylation levels for SMYD2 targeted a very small subset of histones at specific chromatin loci and/or non-histone substrates. LLY-507 inhibited the proliferation of several esophageal, liver, and breast cancer cell lines in a dose-dependent manner, with IC50 values<10μM post 3 days or 7 days^[2].
作用机制LLY-507 binds in the substrate peptide binding pocket.^[2]
参考文献

[1] Nguyen H, Allali-Hassani A, et al. LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2. J Biol Chem. 2015 May 29;290(22):13641-53.
[2] Nguyen H, Allali-Hassani A, Antonysamy S, Chang S, Chen LH, Curtis C, Emtage S, Fan L, Gheyi T, Li F, Liu S, Martin JR, Mendel D, Olsen JB, Pelletier L, Shatseva T, Wu S, Zhang FF, Arrowsmith CH, Brown PJ, Campbell RM, Garcia BA, Barsyte-Lovejoy D, Mader M, Vedadi M. LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2. J Biol Chem. 2015 May 29;290(22):13641-53. doi: 10.1074/jbc.M114.626861. Epub 2015 Mar 30. PMID: 25825497; PMCID: PMC4447944.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7399 mL
- 8.6993 mL
- 17.3986 mL
- 5 mM
- 0.3480 mL
- 1.7399 mL
- 3.4797 mL
- 10 mM
- 0.1740 mL
- 0.8699 mL
- 1.7399 mL

技术信息

CAS号

1793053-37-8

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C36H42N6O

运输

蓝冰

分子量

574.76

别名

LLY-507

溶解度

DMSO	25.0 mg/mL (43.5 mM)
Water	insoluble

动物实验配方

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