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EPZ011989

Name: EPZ011989
Brand: TargetMol
SKU: T2435
Price: 31 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2435Cas No. 1598383-40-4

EPZ011989 is a effective, specific orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 Y646 and EZH2 wt; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.

EPZ011989

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Purity: 99.45%

Catalog No. T2435Cas No. 1598383-40-4

EPZ011989 is a effective, specific orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 Y646 and EZH2 wt; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$31	In Stock	In Stock
10 mg	$46	In Stock	In Stock
25 mg	$79	In Stock	In Stock
50 mg	$128	In Stock	In Stock
100 mg	$229	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:99.45%

Color:White

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COA HNMR LCMS

Product Introduction

EPZ011989 AI Summary

EPZ011989 exhibits diverse bioactivities and pharmacological profiles. It shows no significant inhibition of human cytochrome P450 (CYP) enzyme activities, with an IC50 value greater than 100,000 nM. The compound demonstrates antiviral activity against SARS-CoV-2, inhibiting virus-induced cytotoxicity in Caco-2 cells at 10 µM after 48 hours with a 3.08% inhibition rate, and in VERO-6 cells with inhibition percentages ranging from 0.01% to 0.07% at the same concentration and duration. Additionally, it inhibits SARS-CoV-2 3CL-Pro protease at 20 µM, with inhibition percentages of 7.2% and 9.802%. In enzymatic assays of human HDAC6, the compound demonstrates -8.25% inhibition with a commercial peptide substrate and 5.05% inhibition with a custom peptide substrate. Furthermore, EPZ011989 is a potent inhibitor of EZH2 Y641F mutant with an IC50 of 15.0 nM, inhibits EZH2 leading to a reduction in H3K27me3 levels with an IC50 of 110.0 nM, exhibits antiproliferative activity against human WSUDLCL2 cells with an IC50 of 385.0 nM, and shows a Ki value of less than 3.0 nM for EZH2 inhibition..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	EPZ011989 is a effective, specific orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 Y646 and EZH2 wt; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.
Targets&IC50	EZH2:<3 nM(Ki), EZH1:103 nM

Chemical Properties

Molecular Weight	605.81
Formula	C₃₅H₅₁N₅O₄
Cas No.	1598383-40-4
Smiles	CCN([C@H]1CC[C@@H](CC1)N(C)CCOC)c1cc(cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C)C#CCN1CCOCC1
Relative Density.	1.17 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 3.8 mg/mL (6.27 mM), Sonication is recommended.

Ethanol: 100 mg/mL (165.07 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (1.65 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/Ethanol

	1mg	5mg	10mg	50mg
1 mM	1.6507 mL	8.2534 mL	16.5068 mL	82.5341 mL
5 mM	0.3301 mL	1.6507 mL	3.3014 mL	16.5068 mL

Ethanol

	1mg	5mg	10mg	50mg
10 mM	0.1651 mL	0.8253 mL	1.6507 mL	8.2534 mL
20 mM	0.0825 mL	0.4127 mL	0.8253 mL	4.1267 mL
50 mM	0.0330 mL	0.1651 mL	0.3301 mL	1.6507 mL
100 mM	0.0165 mL	0.0825 mL	0.1651 mL	0.8253 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