Tazémétostat (EPZ-6438) est un inhibiteur puissant, sélectif de EZH2 et disponible par voie orale. Tazémétostat (EPZ-6438) inhibe l'activité du complexe répressif humain 2 polycomb (PRC2) contenant du type sauvage EZH2 avec une valeur Ki de 2,5 nM. Tazémétostat (EPZ-6438) inhibe EZH2 avec des IC50 de 11 et 16 nM dans le dosage des peptides et le dosage des nucléosomes, respectivement. Tazémétostat (EPZ-6438) inhibe l'EZH2 de rat avec un IC50 de 4 nM. Tazémétostat (EPZ-6438) inhibe également EZH1 avec un IC50 de 392 nM.
Tazemetostat (EPZ-6438) ist ein wirksamer, selektiver und oral verfügbarer EZH2-Inhibitor. Tazemetostat (EPZ-6438) hemmt die Aktivität des humanen Polycomb-repressiven Komplexes 2 (PRC2), der Wildtyp-EZH2 mit einem Ki-Wert von 2,5 nM enthält. Tazemetostat (EPZ-6438) hemmt EZH2 mit IC50 -Werten von 11 und 16 nM im Peptidassay bzw. im Nucleosomentest. Tazemetostat (EPZ-6438) hemmt Ratten-EZH2 mit einem IC50 von 4 nM. Tazemetostat (EPZ-6438) hemmt auch EZH1 mit einem IC50 von 392 nM.
Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells.
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Tazemetostat Chemical Structure
CAS No. : 1403254-99-8
This product is a controlled substance and not for sale in your territory.
Western blots of extracts from E14 mESCs treated with 10 μM. EPZ6438 EZH2 inhibitor for 7 d and sampled at time points following inhibitor washout. Blots are probed with the indicated antibodies.
Tazemetostat purchased from MedChemExpress. Usage Cited in:
J Clin Invest. 2018 Jan 2;128(1):483-499.
[Abstract]
Immunoblotting for N1-ICD (n=3) in mouse podocytes exposed to 10 μM EPZ-6438 for 48 hours.
Tazemetostat purchased from MedChemExpress. Usage Cited in:
Toxins (Basel). 2017 May 16;9(5). pii: E162.
[Abstract]
Cells are treated with LeTx in the presence or absence of GSK-J4 or EPZ-6438 for 48 h. H3K27me3 level is analyzed by Western blotting.
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Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells[1].
IC50 & Target[1]
EZH2
In Vitro
Tazemetostat (EPZ-6438) inhibits multi wild-type and mutant lymphoma cell lines proliferation with IC50s of 0.49 nM-7.6 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Room temperature in continental US; may vary elsewhere.
Storage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
1 year
-20°C
6 months
Solvent & Solubility
In Vitro:
DMSO : 31.25 mg/mL (54.56 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
0.1 M HCL : 14.29 mg/mL (24.95 mM; ultrasonic and adjust pH to 5 with HCl)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
1.7460 mL
8.7300 mL
17.4599 mL
5 mM
0.3492 mL
1.7460 mL
3.4920 mL
10 mM
0.1746 mL
0.8730 mL
1.7460 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (4.36 mM); Clear solution
Protocol 2
Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.36 mM); Clear solution
Protocol 3
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 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 4
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 mg/mL) to 900 μLCorn oil, and mix evenly.
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time. 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: 0.5% CMC-Na/0.1% Tween-80 in Saline water
Solubility: 50 mg/mL (87.30 mM); Suspended solution; Need ultrasonic
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.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
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.
[1]. Knutson SK, et, al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferaseEZH2. Proc Natl Acad Sci U S A. 2013 May 7;110(19):7922-7.
[Content Brief]
[1]. Knutson SK, et, al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferaseEZH2. Proc Natl Acad Sci U S A. 2013 May 7;110(19):7922-7.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
0.1 M HCL / DMSO
1 mM
1.7460 mL
8.7300 mL
17.4599 mL
43.6498 mL
5 mM
0.3492 mL
1.7460 mL
3.4920 mL
8.7300 mL
10 mM
0.1746 mL
0.8730 mL
1.7460 mL
4.3650 mL
15 mM
0.1164 mL
0.5820 mL
1.1640 mL
2.9100 mL
20 mM
0.0873 mL
0.4365 mL
0.8730 mL
2.1825 mL
DMSO
25 mM
0.0698 mL
0.3492 mL
0.6984 mL
1.7460 mL
30 mM
0.0582 mL
0.2910 mL
0.5820 mL
1.4550 mL
40 mM
0.0436 mL
0.2182 mL
0.4365 mL
1.0912 mL
50 mM
0.0349 mL
0.1746 mL
0.3492 mL
0.8730 mL
Tazemetostat Related Classifications
EpigeneticsApoptosis
Histone MethyltransferaseApoptosis
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.
