LLY-507

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Chemical Structure| 1793053-37-8 同义名 : -
CAS号 : 1793053-37-8
货号 : A434113
分子式 : C36H42N6O
纯度 : 99%+
分子量 : 574.758
MDL号 : MFCD28902312
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 14 mg/mL(24.36 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.74mL

0.35mL

0.17mL

8.70mL

1.74mL

0.87mL

17.40mL

3.48mL

1.74mL
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.