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LLY507 目录号 GC16261

SMYD2 inhibitor

规格 价格 库存 购买数量
10mg
¥1,344.00
现货
50mg
¥4,694.00
现货
500mg
¥20,475.00
现货
1g
¥29,925.00
现货

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 1793053-37-8 SDF
别名 N/A
化学名 5-cyano-2'-(4-(2-(3-methyl-1H-indol-1-yl)ethyl)piperazin-1-yl)-N-(3-(pyrrolidin-1-yl)propyl)-[1,1'-biphenyl]-3-carboxamide
Canonical SMILES N#CC1=CC(C(NCCCN2CCCC2)=O)=CC(C3=CC=CC=C3N4CCN(CC4)CCN5C=C(C6=C5C=CC=C6)C)=C1
分子式 C36H42N6O 分子量 574.76
溶解度 ≥ 57.5mg/mL in DMSO 储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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产品描述

IC50: < 15 nM

LLY-507 is a potent inhibitor of SMYD2.

SMYD2, a lysine methyltransferase, catalyzes the monomethylation of several protein substrates including p53. SMYD2 is reported to be overexpressed in a significant percentage of esophageal squamous primary carcinomas, and such overexpression related with poor patient survival.

In vitro: LLY-507 has been identified as a cell-active, potent small molecule inhibitor of SMYD2. LLY-507 was found to be >100-fold selective for SMYD2 over a broad range of methyltransferase and non-methyltransferase targets. The crystal structure of SMYD2 in complex with LLY-507 showed it bound in the substrate peptide binding pocket. LLY-507 was active in cells as demonstrated by the reduction of SMYD2-induced monomethylation of p53 Lys(370) at submicromolar concentrations. Furthermore, MS-based proteomics indicated that cellular histone methylation levels were not affected by SMYD2 inhibition with LLY-507 significantly, and subcellular fractionation studies showed that SMYD2 was primarily cytoplasmic, indicating that SMYD2 targeted a small subset of histones. Moreover, LLY-507 was able to inhibit the proliferation of several liver, esophageal, as well as breast cancer cell lines in a dose-dependent manner [1].

In vivo: So far, there is no animal data reported.

Clinical trial: Up to now, LLY-507 is still in the preclinical development stage.

Reference:
[1] Nguyen H, et al.  LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2. J Biol Chem. 2015 May 29;290(22):13641-13653.