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UNC0646

Name: UNC0646
Brand: TargetMol
SKU: TQ0232
Price: 58 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. TQ0232Cas No. 1320288-17-2

Alias UNC 0646

UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases G9a and GLP (IC50s: 6 nM/15 nM for G9a/GLP). UNC0646(UNC 0646) potently blocks G9a/GLP methyltransferase activity in cells (IC50: 10 nM in MCF7 cells) and exhibits low cellular toxicity (EC50: 4.7 μM in MCF7 cells).

UNC0646

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Catalog No. TQ0232Alias UNC 0646Cas No. 1320288-17-2

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$58	In Stock	In Stock
10 mg	$103	In Stock	In Stock
25 mg	$192	In Stock	In Stock
50 mg	$342	Inquiry	Inquiry
100 mg	$497	Inquiry	Inquiry
1 mL x 10 mM (in DMSO)	$88	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:>99.99%

Appearance:Solid

Color:White

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COA

Product Introduction

UNC0646 AI Summary

UNC0646 exhibits bioactivities encompassing significant inhibition of the enzyme G9a, with IC50 values ranging from 6.0 nM to 86.0 nM in various cell lines. It demonstrates moderate cytotoxicity against several human cell lines, with EC50 values ranging from 2800.0 nM to 12000.0 nM after 48 hours. Its selectivity is indicated by varying EC50 to IC50 ratios across different cell lines. The compound exhibits negligible or weak inhibition against other enzymes such as GLP, PRMT3, SETD7, SUV39H2, and SETD8. In the context of antiviral activity, UNC0646 inhibits SARS-CoV-2-induced cytotoxicity in Caco-2 cells at a concentration of 10 µM, displaying a modest inhibition of 2.23%. It shows inhibition of SARS-CoV-2 3CL-Pro protease at 20 µM with inhibition percentages of 2.65% and 7.307%. In VERO-6 cells, the compound demonstrates inhibition percentages against SARS-CoV-2 ranging from 46.28% to 93.73%, and a selectivity index between 0.56 to 2.74. The IC50 values for inhibiting virus-induced cytotoxicity vary between 12030.0 nM and greater than 33000.0 nM, while the toxicity CC50 values against VERO-E6 cells range from greater than 33000.0 nM to 18620.0 nM. Furthermore, UNC0646 shows inhibition of human HDAC6 enzyme, with 27.78% inhibition for a commercial peptide substrate assay and 8.06% for a custom peptide substrate assay. It also displays bioactivity in inhibiting SARS-CoV-2-induced cytopathy with an IC50 value of 17.22 µM, assessed via fluorescence imaging four days post-infection of EGFP-labeled Green monkey Vero cells. Additionally, it exhibits cytotoxicity against human HepG2 cells with an IC50 value of 6600.0 nM as determined by the CellTiter-Glo luminescent cell viability assay..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases G9a and GLP (IC50s: 6 nM/15 nM for G9a/GLP). UNC0646(UNC 0646) potently blocks G9a/GLP methyltransferase activity in cells (IC50: 10 nM in MCF7 cells) and exhibits low cellular toxicity (EC50: 4.7 μM in MCF7 cells).
Targets&IC50	G9a:6 nM, GLP:15 nM
Synonyms	UNC 0646

Chemical Properties

Molecular Weight	621.9
Formula	C₃₆H₅₉N₇O₂
Cas No.	1320288-17-2
Smiles	COc1cc2c(NC3CCN(CC3)C3CCCCC3)nc(nc2cc1OCCCN1CCCCC1)N1CCCN(CC1)C(C)C
Relative Density.	1.128 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 30 mg/mL (48.24 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (6.43 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.6080 mL	8.0399 mL	16.0798 mL	80.3988 mL
5 mM	0.3216 mL	1.6080 mL	3.2160 mL	16.0798 mL
10 mM	0.1608 mL	0.8040 mL	1.6080 mL	8.0399 mL
20 mM	0.0804 mL	0.4020 mL	0.8040 mL	4.0199 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc