Tazemetostat (EPZ-6438)

For research use only.

Catalog No.S7128 Synonyms: E7438

75 publications

Tazemetostat (EPZ-6438) Chemical Structure

CAS No. 1403254-99-8

Tazemetostat (EPZ-6438, E7438) 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.

Selleck's Tazemetostat (EPZ-6438) has been cited by 75 publications

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description Tazemetostat (EPZ-6438, E7438) 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.
EZH2 [1]
(Cell-free assay)
2.5 nM(Ki)
In vitro

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. [1] The antiproliferative effect of EPZ-6438 is enhanced by either prednisolone or dexamethasone in several EZH2 mutant lymphoma cell lines. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HeLa cells M4LrcmZ2dmO2aX;uJIF{e2G7 NVHSd2JnPzJiaB?= Mmf6TY5pcWKrdHnvckBw\iCHWliyJIlvKGi3bXHuJGhmVGFiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJGg{UzJ5bXWzJIxmfmWuczDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCHTFnTRUBu\XSqb3SsJGlEPTB;MD6wNkDPxE1w NWfVUnBMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xPFkxPzhpPkK2NVg6ODd6PD;hQi=>
Sf9 NELYcGdHfW6ldHnvckBie3OjeR?= NUnSe5FCOiCq NUe2ZmlJUW6qaXLpeIlwdiCxZjDoeY1idiCQLYTldo1qdmGuIFjpd{11[WepZXSgSXpJOi:obHHnMZRi\2enZDDFSWQwW1WcMUKvRWVDWDJxUlLBVFQ5KEF4N{fHJI12fGGwdDCoNkB1dyCnbnSgdoV{cWS3ZYOpJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6|ZXP0JINmdGy|IIXzbY5oKGirc4TvcoUhUDNiKEGgeI8hPTBicnXzbYR2\XNrLVfHT{BieyC|dXLzeJJifGViYX\0[ZIhOiCqcoOgbY4heHKnc3XuZ4Uhd2ZiU1HNJIJ6KG[uLDDJR|UxKD1iMD6wNFQh|ryPLh?= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR3Nke5OUc,Ojl2NU[3PVU9N2F-
KARPAS422 NGHGco9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NGj5NHo{KHSxIESg[IF6eyC3cDD0c{AyPCCmYYnz MofPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNQWLQRXM1OjJiY3XscJMhcGG{Yn;ybY5oKG2xbn;hcIxmdGmlIGm2OFFPKEWcSEKgcZV1[XSrb36gZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KG2nYYP1doVlKGW4ZYL5JFMhfG9iNDDkZZl{KHWyIITvJFE1KGSjeYOgZpkhSmWla33hckBEd3WudHXyMYJie2WmIH3leIhw\CxiSVO1NEA:KDBwMEGyJO69VS5? NUjpd2pzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiwPVIyPTVpPkK4NFkzOTV3PD;hQi=>
Pfeiffer NU\1c4dpS3m2b4TvfIlkcXS7IHHzd4F6 NVXufW9RPSCmYYnz M1q5PWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBn\WmoZnXyJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEWg[IF6eyCkeTDD[YxtXGm2ZYKtS4xwKHKnYXflcpQh[mG|ZXSgcJVucW6nc3PlcoNmKGG|c3H5MEBKSzVyIE2gNE4xOzhizszNMi=> MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR3Nke5OUc,Ojl2NU[3PVU9N2F-
G401 NIrpdlBHfW6ldHnvckBie3OjeR?= NIHTelQ1QCCq M1fsZ2lvcGmkaYTpc44hd2ZiRVXEJIlvKGi3bXHuJGc1ODFiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJIdtd2KjbDDIN2szP22nMzDs[ZZmdCCjZoTldkA1QCCqcoOgZpkhTUyLU1GsJGlEPTBiPTCwMlA1KM7:TT6= NECzO3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEC5NlE2PSd-MkiwPVIyPTV:L3G+
G401 NXTOR|doTnWwY4Tpc44h[XO|YYm= Mn32OEBp NWTEZ4xoUW6qaXLpeIlwdiCxZjDt[ZRpgWy2cnHud4ZmemG|ZTDhZ5Rqfmm2eTDv[kBGYkh{IHnuJIh2dWGwIFe0NFEh[2WubIOgZZN{\XO|ZXSgZZMhUDONMkegeJJqdWW2aInsZZRqd25iYX\0[ZIhPCCqcoOgZpkhTUyLU1GsJGVEPTBiPTCwMlIh|ryPLh?= NWqzTopORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3OlkzPzhpPkK2O|Y6Ojd6PD;hQi=>
Pfeiffer NUPYV29YSW62aYT1cY9zKGG|c3H5 NYG4UppvOTByIH3nM4to NF\WSXozOCCmYYnz MkfHRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUH\lbYZn\XJiY3XscJMhgGWwb3fyZYZ1\WRiaX6gZZRpgW2rYzDueYRmKG2xdYPlJIF{e2W|c3XkJIF{KHS3bX;yJIdzd3e2aDDpcohq[mm2aX;uJIF1KDFyMDDt[{9s\yxicH:gdYQh[WSvaX7pd5RmemWmIH\vdkAzOCCmYYnzJI1m[XO3cnXkJJR4cWOnIIDldkB4\WWt NIjSXFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUS1Olc6PSd-Mkm0OVY4QTV:L3G+

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot

PubMed: 26360609     

C-E. Measure of target engagement by CETSA. HEK293 cells stably expressing EZH2 WT or mutants were incubated with DMSO or incremental dose of EPZ-6438 for 3 hr and heated at 52°C. Nucleoplasmic lysates were analyzed by immunoblot for EZH2 level.


PubMed: 29670078     

U2OS were treated with increasing concentrations of the EZH2 inhibitor EPZ-6438 for 4 days. Nuclear protein extracts were used for western blot detection of H3K27me3. Actin was used as loading control. (Graph) Quantification is shown.

26360609 29670078

PubMed: 29670078     

Representative images of the average number of colocalizations of RAP1 (green) and HP1 (red) in U2OS treated with vehicle or with EZH2 inhibitor. Arrowheads indicate colocalization events. Scale bar, 10 μm.

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. [1]


Kinase Assay:[1]
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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.
Cell Research:[1]
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  • Cell lines: Mutant cell lines (G401, A204, G402, KYM-1), Wild type cell line (RD, 293, SJCRH30)
  • Concentrations: ~10 μM
  • Incubation Time: 7 days
  • Method: For the adherent cell line proliferation assays, plating densities for each cell line are determined based on growth curves (measured by ATP content) and density over a 7-d time course. On the day before compound treatment, cells are plated in either 96-well plates in triplicate (for the day 0–7 time course) or 6-well plates (for replating on day 7 for the remainder of the time course). On day 0, cells are either untreated, DMSO-treated, or treated with EPZ-6438 starting at 10 µM and decreasing in either threefold or fourfold dilutions. Plates are read on day 0, day 4, and day 7 using Cell Titer Glo, with compound/media being replenished on day 4. On day 7, the six-well plates are trypsinized, centrifuged, and resuspended in fresh media for counting by Vi-Cell. Cells from each treatment are replated at the original density in 96-well plates in triplicate. Cells are allowed to adhere to the plate overnight, and cells are treated as on day 0. On days 7, 11, and 14, plates are read using Cell Titer Glo, with compound/media being replenished on day 11. Averages of triplicates are used to plot proliferation over the time course, and calculate IC50 values. For cell cycle and apoptosis, G401 and RD cells are plated in 15-cm dishes in duplicate at a density of 1 × 106 cells per plate. Cells are incubated with EPZ-6438 at 1 µM, in a total of 25 mL, over a course of 14 d, with cells being split back to original plating density on day 4, 7, and 11. Cell cycle analysis and TUNEL assay are performed using a Guava flow cytometer, following the manufacturer’s protocol.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: SCID mice bearing s.c. G401 xenografts.
  • Dosages: ~500 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 5 mg/mL warmed (8.72 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+50% 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.

Chemical Information

Molecular Weight 572.74


CAS No. 1403254-99-8
Storage powder
in solvent
Synonyms E7438

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    Could you please help test the formulation of S7128 for in vivo studies?

  • Answer:

    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.

Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID