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MAK683 Histone Methyltransferase inhibitor

Name: MAK683
Brand: Selleck Chemicals
SKU: S8983
Availability: InStock
Rating: 5 (7 reviews)

Cat.No.S8983

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

Chemical Structure

Molecular Weight: 376.39

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.86

Related Targets	HDAC JAK BET PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Other Histone Methyltransferase Inhibitors	Pinometostat (EPZ5676) 3-Deazaneplanocin A (DZNep) Hydrochloride BIX-01294 trihydrochloride EPZ004777 EPZ015666 (GSK3235025) UNC1999 EPZ005687 SGC 0946 MM-102 UNC0638

Solubility

In vitro
Batch:

DMSO : 12.5 mg/mL (33.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.300mg/ml (0.80mM)	Taking the 1 mL working solution as an example, add 50 μL of 6 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 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.150mg/ml (0.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 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.

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.

Chemical Information, Storage & Stability

Molecular Weight	376.39	Formula	C₂₀H₁₇FN₆O	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1951408-58-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	EED inhibitor-1			Smiles	CC1=C(C=CC=N1)C2=CN=C(N3C2=NN=C3)NCC4=C(C=CC5=C4CCO5)F

Mechanism of Action

Targets/IC₅₀/Ki	EED (ELISA assay) 26 nM EED (EED Alphascreen binding assay) 59 nM EED (LC-MS assay) 89 nM
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 this compound treatment in association with a higher CD38 expression is also identified.
References	[1] https://patents.google.com/patent/US20160176882A1/en [2] https://pubmed.ncbi.nlm.nih.gov/31816138/ [3] https://pubmed.ncbi.nlm.nih.gov/30755708/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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