2. Epigenetics
  3. Histone Methyltransferase
  4. EPZ011989

EPZ011989 is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ011989 shows robust methyl mark inhibition and anti-tumor activity. EPZ011989 can be used for the research of various cancers. EPZ011989 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

For research use only. We do not sell to patients.

EPZ011989 Chemical Structure

EPZ011989 Chemical Structure

CAS No. : 1598383-40-4

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10 mM * 1 mL in DMSO
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Based on 2 publication(s) in Google Scholar

Other Forms of EPZ011989:

EPZ011989 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

EPZ011989 is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ011989 shows robust methyl mark inhibition and anti-tumor activity. EPZ011989 can be used for the research of various cancers[1]. EPZ011989 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

EZH2

 

In Vitro

EPZ011989 inhibits mutant and wild-type EZH2 with an Ki value of <3 nM[1].
? EPZ011989 reduces cellular H3K27 methylation with an IC50 value of 94 nM[1].
? EPZ011989 (0-10 μM; 11 days) has anti-proliferation effect in WSU-DLCL2 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

EPZ011989 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: WSU-DLCL2 cells
Concentration: 0-10 μM
Incubation Time: 11 days
Result: Demonstrated an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM.
In Vivo

EPZ011989 (oral; 30-1000 mg/kg; single or bid; for 7 days or 21 days) can elicit robust methyl mark inhibition and antitumor activity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID mice[1]
Dosage: 125, 250, 500, and 1000 mg/kg
Administration: Oral; single, twice-daily (BID)for 7 days or twice-daily (BID)for 21 days
Result: Provided coverage over the LCC for 24 h (1000 mg/kg ), while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h.
Observed complete ablation of the methyl mark by the end of day 7.
Showed robust tumor growth inhibition, methyl mark reduction and extended total and free plasma exposure time.
Animal Model: Rat[1]
Dosage: 30, 100, and 300 mg/kg
Administration: Oral, single
Result:
dose (mg/kg) route t1/2 (h) tmax (h) Cmax (ng/mL) AUCinf (h*ng/mL) time above LCC (h)
30 p.o. 4.7 2 240 970 4
100 p.o. 3.9 2.7 1600 5600 8
300 p.o. 3.7 2.7 2900 10000 10
Molecular Weight

605.81

Formula

C35H51N5O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NCC1=C(C)C=C(C)NC1=O)C2=CC(C#CCN3CCOCC3)=CC(N(CC)[C@H]4CC[C@H](N(CCOC)C)CC4)=C2C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (165.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6507 mL 8.2534 mL 16.5068 mL
5 mM 0.3301 mL 1.6507 mL 3.3014 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.13 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.13 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.79%

SDS (392 KB)

COA (248 KB) LCMS (99 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6507 mL 8.2534 mL 16.5068 mL 41.2671 mL
5 mM 0.3301 mL 1.6507 mL 3.3014 mL 8.2534 mL
10 mM 0.1651 mL 0.8253 mL 1.6507 mL 4.1267 mL
15 mM 0.1100 mL 0.5502 mL 1.1005 mL 2.7511 mL
20 mM 0.0825 mL 0.4127 mL 0.8253 mL 2.0634 mL
25 mM 0.0660 mL 0.3301 mL 0.6603 mL 1.6507 mL
30 mM 0.0550 mL 0.2751 mL 0.5502 mL 1.3756 mL
40 mM 0.0413 mL 0.2063 mL 0.4127 mL 1.0317 mL
50 mM 0.0330 mL 0.1651 mL 0.3301 mL 0.8253 mL
60 mM 0.0275 mL 0.1376 mL 0.2751 mL 0.6878 mL
80 mM 0.0206 mL 0.1032 mL 0.2063 mL 0.5158 mL
100 mM 0.0165 mL 0.0825 mL 0.1651 mL 0.4127 mL
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EPZ011989 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EPZ0119891598383-40-4EPZ 011989EPZ-011989Histone MethyltransferaseoralZeste Homolog 2 (EZH2)metabolic stabilitymethylanti-tumorcancersInhibitorinhibitorinhibit

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