Home Methylation PRMT inhibitor LLY-283 For research use only.

LLY-283

LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. LLY-283 shows antitumor activity.

LLY-283 Chemical Structure

LLY-283 Chemical Structure

CAS No. 2040291-27-6

Purity & Quality Control

LLY-283 Related Products

Biological Activity

Description LLY-283 is a novel and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 nM and 25 nM, respectively. LLY-283 shows antitumor activity.
Targets
PRMT5 [1]
(Cell-free assay)		 PRMT5 [1]
(Cell-based assay)
22 nM 25 nM
In vitro
In vitro

LLY-283 inhibits PRMT5 enzymatic activity in vitro and in cells with IC50 of 22 ± 3 and 25 ± 1 nM, respectively. LLY-283 directly binds to and occupies the SAM pocket. LLY-283 is a low nanomolar enzymatic inhibitor of the PRMT5:MEP50 complex in biochemical assays and is selective for PRMT5 over other methyltransferases including related family members.[1]
Cell Research Cell lines Sf9 cells, A375 tumor cells, MCF7 cells
Concentrations 1 µM, 10 µM
Incubation Time 48 h
Method

PRMT5 cellular assay. MCF7 cells are grown in DMEM supplemented with 10% FBS, penicillin (100 units/ml) and streptomycin (100 µg/ml). 40% confluent cells are treated with different concentrations of LLY-283 or DMSO control for 48 h. The levels of SmBB' and symmetrically dimethylated SmBB' are analyzed in westernblot.
In Vivo
In vivo LLY-283 shows antitumor activity in mouse xenografts when dosed orally and can serves as an excellent probe molecule for understanding the biological function of PRMT5 in normal and cancer cells. LLY-283 can be used as an in vivo tool compound to evaluate the pharmacology of PRMT5 inhibition.[1]
Animal Research Animal Models SCID mice with A375 derived xenografts
Dosages 20 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 342.35 Formula

C17H18N4O4
CAS No. 2040291-27-6 SDF --
Smiles C1=CC=C(C=C1)C(C2C(C(C(O2)N3C=CC4=C(N=CN=C43)N)O)O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 68 mg/mL ( (198.62 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 5 mg/mL

Ethanol : 3 mg/mL


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

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-283 | LLY-283 supplier | purchase LLY-283 | LLY-283 cost | LLY-283 manufacturer | order LLY-283 | LLY-283 distributor