Catalog No.S7128 Synonyms: E7438
Molecular Weight(MW): 572.74
Tazemetostat (EPZ-6438) is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.
Cited by 15 Publications
5 Customer Reviews
EZH2i-induced H3K27ac level change in cancer cells. Cells were treated with 1 mM EPZ-6438 and 1 mM GSK126 for 6 days, respectively. H3K27ac was detected by immunoblotting. Lysates from each cell line were blotted individually. EPZ: EPZ-6438.
Cell, 2018, 175(1):186-199. Tazemetostat (EPZ-6438) purchased from Selleck.
Global H3K27me3 status was also assessed by flow cytometry. Results are median values of the H3K27me3 staining index in CD138 viable PC. * indicates a significant difference compared to control cells using a Wilcoxon test for pairs (P ≤ 0.05).
Clin Epigenetics, 2018, 10(1):121. Tazemetostat (EPZ-6438) purchased from Selleck.
EZH2 inhibition does not affect pediatric high-grade glioma cell growth in vitro. (a-c) Relative cell viability of pediatric high-grade glioma cell lines were subjected to MTT cell viability assays 72 h after incubation with increasing concentrations of Tazemetostat (EPZ-6438) as indicated. Graphs show the mean of 3 independent biological replicates with the respective SEM, * p < 0.05.
Klin Padiatr, 2016, 228(3):113-117.. Tazemetostat (EPZ-6438) purchased from Selleck.
Purity & Quality Control
Choose Selective Histone Methyltransferase Inhibitors
|Description||Tazemetostat (EPZ-6438) is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.|
|Features||Orally bioavailable EZH2-selective inhibitor for both wild-type and mutant. Currently being tested in Phase II clinical trials for treatment of Diffuse Large B Cell Lymphoma.|
EPZ-6438 concentration-dependently reduces global H3K27Me3 levels in wild-type or SMARCB1 mutant cells, and induces strong antiproliferative effects with IC50 ranging from 32 nM to 1000 nM in SMARCB1-deleted MRT cell lines. EPZ-6438 induces gene expression of neuronal differentiation and cell cycle inhibition, while inhibtis expression of Hedgehog pathway genes, MYC and EZH2.  The antiproliferative effect of EPZ-6438 is enhanced by either prednisolone or dexamethasone in several EZH2 mutant lymphoma cell lines. 
|In vivo||In SCID mice bearing s.c. G401 xenografts, EPZ-6438 induces tumor stasis during the administration period and produces a significant tumor growth delay with minimal effect on body weight. |
Biochemical Methods:EPZ-6438 is incubated for 30 min with 40 μL per well of 5 nM PRC2 (final assay concentration in 50 μL is 4 nM ) in 1X assay buffer (20 mM Bicine [pH 7.6], 0.002% Tween-20, 0.005% Bovine Skin Gelatin and 0.5 mM DTT). 10 μL per well of substrate mix comprising assay buffer 3 H-SAM, unlabeled SAM, and peptide representing histone H3 residues 21-44 containing C-terminal biotin (appended to a C-terminal amide-capped lysine) are added to initiate the reaction (both substrates are present in the final reaction mixture at their respective Km values, an assay format referred to as ‘‘balanced conditions’’. The final concentrations of substrates and methylation state of the substrate peptide are indicated for each enzyme Reactions are incubated for 90 min at room temperature and quenched with 10 μL per well of 600 μM unlabeled SAM, Then transferred to a 384-well flashplate and washed after 30 min.
|In vitro||DMSO||5 mg/mL warmed (8.72 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Frequently Asked Questions
Could you please help test the formulation of S7128 for in vivo studies?
We've tried some vehicles for S7128 EPZ-6438, and found it can be dissolved in 2% DMSO+30% PEG 300+5% Tween+ddH2O at 5 mg/ml as a clear solution. S7128 dissolved in 5% DMSO+0.5% CMC Na at 15 mg/ml is a suspension for oral gavage.