Choose Your Country or Region

LLY-507

Name: LLY-507
Brand: Selleck Chemicals
SKU: S7575
Rating: 5 (6 reviews)

Catalog No.S7575 Purity:99.78%

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

LLY-507 Chemical Structure

CAS No. 1793053-37-8

Purity & Quality Control

Batch: Purity: 99.78%

99.78

LLY-507 Related Products

Related Targets	Menin-MLL interaction WDR5-MLL interaction	Click to Expand
Related Products	GSK126 DZNeP (3-deazaneplanocin A) HCl GSK343 Pinometostat (EPZ5676) BIX 01294 EPZ004777 EPZ015666 (GSK3235025) UNC1999 Chaetocin EPZ005687 Pemrametostat (GSK3326595) SGC 0946 MM-102 UNC0638 EPZ011989 UNC0642 OICR-9429 UNC0379 GSK591 Lirametostat (CPI-1205) MI-2 (Menin-MLL Inhibitor) CPI-169 MI-503 MS023 A-196 GSK503 AMI-1 PFI-2 HCl SGC707 A-366 MI-3 (Menin-MLL Inhibitor) BRD4770 Onametostat (JNJ-64619178) WDR5-0103 EI1 UNC3866 EPZ020411 2HCl MI-463 HLCL-61 HCL MAK683 MI-136 MS049 SAH (S-Adenosyl-L-homocysteine) PF-06726304 CPI-360 JQ-EZ-05 (JQEZ5) SGC2085	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Highly Selective Inhibitor Library	Click to Expand

Signaling Pathway

Histone Methyltransferase Signaling Pathway

Biological Activity

Description

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

Targets

SMYD2 ^[1]

In vitro
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].
Cell Research	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.

References

[1] Nguyen H, et al. J Biol Chem. 2015, 290(22):13641-53.

Chemical Information & Solubility

Molecular Weight	574.76	Formula	C₃₆H₄₂N₆O
CAS No.	1793053-37-8	SDF	Download LLY-507 SDF
Smiles	CC1=CN(C2=CC=CC=C12)CCN3CCN(CC3)C4=CC=CC=C4C5=CC(=CC(=C5)C#N)C(=O)NCCCN6CCCC6
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 30 mg/mL ( (52.19 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 22 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	10% DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O	2.0mg/ml (3.48mM)	Taking the 1 mL working solution as an example, add 100 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.	In vivo Formulation Calculator
Clear solution	5% DMSO 1 95% corn oil	1.65mg/ml (2.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml (8.70mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.

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

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):