LLY-507

Catalog No.S7575

For research use only.

LLY-507 is a cell-active, potent, and selective inhibitor of protein-lysine Methyltransferase SMYD2.

LLY-507 Chemical Structure

CAS No. 1793053-37-8

Selleck's LLY-507 has been cited by 5 Publications

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description LLY-507 is a cell-active, potent, and selective inhibitor of protein-lysine Methyltransferase SMYD2.
Targets
SMYD2 [1]
()
In vitro

LLY-507 potently inhibits the ability of SMYD2 to methylate p53 peptide with an IC50 <15 nM. LLY-507 is able to potently inhibit the methylation of H4 peptide by SMYD2 enzyme with an IC50 of 31 nM. It has 100-fold selectivity for SMYD2 over 24 other protein or DNA methyltransferases including related family members SMYD3, SUVH420H1, and SUV420H2. LLY-507 inactives (>20 μM) against 454 kinases, 35 G protein-coupled receptors, 14 nuclear hormone receptors, and three cytochrome P450 enzymes. LLY-507 inhibits the proliferation of several esophageal, liver, and breast cancer cell lines in a dose-dependent manner[1].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: HEK293 cells
  • Concentrations: 0-2.5 μM
  • Incubation Time: 28 h
  • Method:

    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 radioimmunoprecipitation assay (RIPA) buffer. Cell lysates are subject to 10% SDS-PAGE and transferred to a PVDF membrane.

Solubility (25°C)

In vitro

DMSO 100 mg/mL warmed
(173.98 mM)
Water Insoluble
Ethanol '22 mg/mL

Chemical Information

Molecular Weight 574.76
Formula

C36H42N6O

CAS No. 1793053-37-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CN(C2=CC=CC=C12)CCN3CCN(CC3)C4=CC=CC=C4C5=CC(=CC(=C5)C#N)C(=O)NCCCN6CCCC6

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy LLY-507 | LLY-507 supplier | purchase LLY-507 | LLY-507 cost | LLY-507 manufacturer | order LLY-507 | LLY-507 distributor