Home Epigenetics Histone Methyltransferase inhibitor MAK683 For research use only.

MAK683

Synonyms: EED inhibitor-1

MAK683 (EED inhibitor-1, example 2) is an inhibitor of embryonic ectoderm development (EED). MAK683 exhibits IC50 of 59 nM, 89 nM and 26 nM in EED Alphascreen binding, LC-MS and ELISA assay, respectively.

MAK683 Chemical Structure

MAK683 Chemical Structure

CAS No. 1951408-58-4

Purity & Quality Control

Batch: S898301 DMSO]12.5 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.86%
99.86

MAK683 Related Products

Signaling Pathway

Histone Methyltransferase Signaling Pathways

Histone Methyltransferase Signaling Pathway

Biological Activity

Description MAK683 (EED inhibitor-1, example 2) is an inhibitor of embryonic ectoderm development (EED). MAK683 exhibits IC50 of 59 nM, 89 nM and 26 nM in EED Alphascreen binding, LC-MS and ELISA assay, respectively.
Targets
EED [1]
(ELISA assay)		 EED [1]
(EED Alphascreen binding assay)		 EED [1]
(LC-MS assay)
26 nM 59 nM 89 nM
In vitro
In vitro

MAK-683 binds to EED and disrupts the PRC2 complex. Cell viability is not significantly affected and the levels of H3K27me3 are decreased. A significant increase in the percentage of mature PCs after MAK-683 treatment in association with a higher CD38 expression is also identified.[3]
Cell Research Cell lines MBCs
Concentrations 2 µM
Incubation Time 4 days, 3 days
Method

MBCs are differentiated using a previously described culture protocol. All cultures are performed in Iscove modified Dulbecco medium, 10% FCS and 25–35% of Resto-6 cells supernatant. 1.5 × 105/ml purified peripheral blood MBCs are activated for 4 days by 10 µg/ml of phosphorothioate CpG oligodeoxynucleotides (ODN) 2006, 50 ng/ml histidine tagged soluble CD40 ligand (CD40L) and 5 µg/ml of an anti-poly-histidine mAb in the presence of 20 U/ml IL-2, 50 ng/ml IL-10, and 10 ng/ml IL-15. The next 3 days, PBs are generated by removing ODN and CD40L and changing the cytokine cocktail. From day 7 to day 10, PBs are differentiated into early PCs by adding 50 ng/ml IL-6, 10 ng/ml IL-15, 500 U/ml IFN-α. MAK-683 (2 µM) is added at the start of each step and its effects are evaluated by analyzing cell counts and phenotype at the end of each step.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02900651 Active not recruiting
Diffuse Large B-cell Lymphoma
Novartis Pharmaceuticals|Novartis
 October 3 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 376.39 Formula

C20H17FN6O
CAS No. 1951408-58-4 SDF --
Smiles CC1=C(C=CC=N1)C2=CN=C(N3C2=NN=C3)NCC4=C(C=CC5=C4CCO5)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 12.5 mg/mL ( (33.21 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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 MAK683 | MAK683 supplier | purchase MAK683 | MAK683 cost | MAK683 manufacturer | order MAK683 | MAK683 distributor