LLY-507
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货号：A434113
LLY-507 是一种高效和选择性的蛋白-赖氨酸甲基转移酶 SMYD2 抑制剂，IC50 小于 15 nM，可在细胞中抑制 p53K370 甲基化，IC50 约为 600 nM。
LLY-507 化学结构
LLY-507 3D分子结构
规格
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会员价
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数量
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现货
1周
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+
LLY-507 纯度/质量文件 产品仅供科研
货号：A434113
标准纯度：
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产品说明书
全球学术期刊中引用的产品
• Adv. Funct. Mater. , 2025, 2500696. Ambeed. • J. Am. Chem. Soc. , 2025. Ambeed. • Sci. Adv. , 2025, 11(13): eadr0006. Ambeed. • ACS Appl. Mater. Interfaces , 2025, 17(12): 18046-18058. Ambeed. • Food Res. Int. , 2025, 116191. Ambeed. 更多 >
LLY-507 质控信息
BRD4770
✔
99%+
UNC1999
+++
EZH1, IC50: 45 nM
EZH2, IC50: 2 nM
99%+
EPZ005687
++
98+%
EPZ015666
+++
99%+
3-Deazaneplanocin A HCl
++++
S-adenosylhomocysteine hydrolase, Ki: 50 pM
99%+
Tazemetostat
+++
EZH2, Ki: 2.5 nM
EZH2, IC50: 11 nM
98%
GSK126
++
99%+
MI-3
+
98%
MM-102
++
99%
EI1
++
Ezh2 (wild-type), IC50: 15 nM
EZH2 (Y641F), IC50: 13 nM
99% (HPLC)
SGC0946
++++
99%+
PFI-2 HCl
++++
SETD7, IC50: 2 nM
SETD7, Ki: 0.33 nM
99%+
Pinometostat
++++
99%+
EPZ004777
+++
99%+
Entacapone
++
95%
UNC0379
+
99%+
Menin-MLL inhibitor MI-2
+
98%
GSK343
+++
EZH1, IC50: 240 nM
EZH2, IC50: 4 nM
99%+
BIX-01294 3HCl
+
99%+
展开
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
LLY-507 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]
LLY-507 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.
LLY-507 实验方案
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存储液制备
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
LLY-507 技术信息
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