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UNC0646 Histone Methyltransferase inhibitor

Name: UNC0646
Brand: Selleck Chemicals
SKU: S7020
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S7020

UNC0646 is a selective histone lysine methyltransferase (HMTase) inhibitor for G9a and GLP with IC50 of 6 nM and 15 nM , respectively, with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity.

Chemical Structure

Molecular Weight: 621.9

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Quality Control

Batch: S702001 Ethanol]50 mg/mL]false]DMSO]33 mg/mL]false]Water]Insoluble]false Purity: 99.82%

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

99.82

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

Solubility

In vitro
Batch:

Ethanol : 50 mg/mL

DMSO : 33 mg/mL (53.06 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 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.	0.35mg/ml (0.56mM)	Taking the 1 mL working solution as an example, add 50 μL of 7 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.	0.35mg/ml (0.56mM)	Taking the 1 mL working solution as an example, add 50 μL of 7 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	621.9	Formula	C₃₆H₅₉N₇O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1320288-17-2	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	G9a (Cell-free assay) 6 nM GLP (Cell-free assay) 15 nM
In vitro	UNC0646 is a novel G9a inhibitor with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity. This compound has high in vitro potency versus G9a and improved lipophilicity, are highly potent (IC50 < 0.06 μM) in reducing H3K9me2 levels in MDA-MB-231 cells and has low cell toxicity.
In vivo	Due to its water insolubility, the in vivo efficacy of UNC0646 is not satisfactory. Nanodiamonds (NDs) are utilized as a drug delivery platform to improve in vivo delivery of this small-molecule inhibitor. ND-this compound complexes can be rapidly synthesized by physical adsorption, meanwhile possessing favorable drug delivery properties and is able to improve the dispersibility of this chemical in water, therefore making it amenable for intravenous administration. The release profile of this compound from NDUNC0646 is demonstrated to be pH-responsive. Moreover, ND-this chemical maintains the biological functionality of this inhibitor, with higher efficacy in reducing H3K9 methylation as well as enhanced invasion suppressive effects. Most importantly, increased in vivo efficacy is demonstrated using an orthotopic Hepatocellular carcinoma (HCC) mouse model, which paves the way of translating this small-molecule inhibitor toward HCC treatment.
References	[1] https://pubmed.ncbi.nlm.nih.gov/21780790/ [2] https://pubmed.ncbi.nlm.nih.gov/31718136/

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