Art. -Nr.: HY-13803

Tazemetostat

(Synonyms: EPZ-6438; E-7438)

96 Cited Publications

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Based on 96 publication(s) in Google Scholar

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 K_i 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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Reinheit: 99.93%
CAS. Nr.: 1403254-99-8
Formel: C₃₄H₄₄N₄O₄
Molecular Weight:572.74

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Tazemetostat Chemical Structure

CAS. Nr.: 1403254-99-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (96)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
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Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

EZH2

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	29.3 μM Compound: EPZ-6438	Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
A2780	IC₅₀	47 μM Compound: EPZ-6438	Antiproliferative activity against human A2780 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human A2780 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
A549	IC₅₀	>100 μM Compound: EPZ-6438	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
A549	IC₅₀	15.83 μM Compound: EPZ-6438	Antiproliferative activity against human A549 cells by MTT assay Antiproliferative activity against human A549 cells by MTT assay	[PMID: 38580135]
ASPC1	IC₅₀	>30 μM Compound: EPZ6438	Antiproliferative activity against human ASPC1 cells assessed as cell growth inhibition incubated for 6 days by MTS assay Antiproliferative activity against human ASPC1 cells assessed as cell growth inhibition incubated for 6 days by MTS assay	[PMID: 35500243]
Breast carcinoma cell	GI₅₀	>10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human 3D Triple-negative breast cancer cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human 3D Triple-negative breast cancer cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
BT-549	IC₅₀	>10 μM Compound: EPZ-6438	Anti-proliferative activity against human BT-549 cells assessed as cell growth inhibition measured after 5 days incubation by CCK-8 assay Anti-proliferative activity against human BT-549 cells assessed as cell growth inhibition measured after 5 days incubation by CCK-8 assay	[PMID: 38295690]
BT-549	IC₅₀	>40 μM Compound: Tazemetostat	Antiproliferative activity against human BT-549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human BT-549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
BT-549	IC₅₀	15.36 μM Compound: Taz	Synergistic cytotoxicity against human BT-549 cells incubated for 72 hrs in presence of Niraparib by MTT assay Synergistic cytotoxicity against human BT-549 cells incubated for 72 hrs in presence of Niraparib by MTT assay	[PMID: 38134746]
BT-549	IC₅₀	57.46 μM Compound: Taz	Cytotoxicity against human BT-549 cells incubated for 72 hrs by MTT assay Cytotoxicity against human BT-549 cells incubated for 72 hrs by MTT assay	[PMID: 38134746]
BT-549	IC₅₀	58.2 μM Compound: EPZ-6438	Antiproliferative activity against human BT-549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human BT-549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
CWR22R	GI₅₀	>30 μM Compound: EPZ; EPZ6438	Synergistic growth inhibition of human 22Rv1 cells incubated for 6 to 7 days in presence of ORY1001 by MTS assay Synergistic growth inhibition of human 22Rv1 cells incubated for 6 to 7 days in presence of ORY1001 by MTS assay	[PMID: 39196854]
CWR22R	GI₅₀	>30 μM Compound: EPZ; EPZ6438	Synergistic growth inhibition of human 22Rv1 cells incubated for 6 to 7 days in presence of TCP by MTS assay Synergistic growth inhibition of human 22Rv1 cells incubated for 6 to 7 days in presence of TCP by MTS assay	[PMID: 39196854]
CWR22R	GI₅₀	51.94 μM Compound: EPZ; EPZ6438	Growth inhibition of human 22Rv1 cells incubated for 6 to 7 days by MTS assay Growth inhibition of human 22Rv1 cells incubated for 6 to 7 days by MTS assay	[PMID: 39196854]
Daudi	GI₅₀	>10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human Daudi cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human Daudi cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
Daudi	GI₅₀	>10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human Daudi cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human Daudi cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
DB	IC₅₀	>3 μM Compound: 1; EPZ-6438	Antiproliferative activity against human DB cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay Antiproliferative activity against human DB cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay	[PMID: 37203326]
ES-2	IC₅₀	79 μM Compound: EPZ-6438	Antiproliferative activity against human ES2 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human ES2 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
Farage	GI₅₀	>10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human Farage cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human Farage cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
G-401	EC₅₀	0.2 μM Compound: 4; EPZ-6438; Tazemetostat	Inhibition of methyltransferase activity of EZH2 in human G401 cells assessed as H3K27 trimethylation after 4 hrs by ELISA Inhibition of methyltransferase activity of EZH2 in human G401 cells assessed as H3K27 trimethylation after 4 hrs by ELISA	[PMID: 26769278]
HCT-116	IC₅₀	>20 μM Compound: 5; EPZ6438	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36153841]
HeLa	IC₅₀	0.02 μM Compound: EPZ-6438	Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method	[PMID: 26189078]
HeLa	IC₅₀	27.69 μM Compound: EPZ-6438	Antiproliferative activity against human HeLa cells by MTT assay Antiproliferative activity against human HeLa cells by MTT assay	[PMID: 38580135]
HEY	IC₅₀	>100 μM Compound: EPZ-6438	Antiproliferative activity against human HEY cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human HEY cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
HK-2	IC₅₀	>40 μM Compound: Tazemetostat	Antiproliferative activity against human HK-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human HK-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
HL-60	IC₅₀	>20 μM Compound: 5; EPZ6438	Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36153841]
HL-60	IC₅₀	>40 μM Compound: Tazemetostat	Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
HT	IC₅₀	>3 μM Compound: 1; EPZ-6438	Antiproliferative activity against human HT cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay Antiproliferative activity against human HT cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay	[PMID: 37203326]
K562	IC₅₀	59.2 μM Compound: 2; EPZ-6438	Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 35569264]
KARPAS-422	GI₅₀	0.09 μM Compound: 1; EPZ-6438	Antiproliferative activity against human KARPAS-422 cells harboring EZH2 Y641N mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human KARPAS-422 cells harboring EZH2 Y641N mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
KARPAS-422	GI₅₀	0.39 μM Compound: 1; EPZ-6438	Antiproliferative activity against human KARPAS-422 cells expressing Y641N mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human KARPAS-422 cells expressing Y641N mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
KARPAS-422	IC₅₀	0.012 μM Compound: 5; EPZ-6438	Antiproliferative activity against human KARPAS422 cells harboring monoallelic Y641N EZH2 mutation assessed as reduction in cell viability measured every 3 to 4 days up to 14 days by Beckman Coulter-based method Antiproliferative activity against human KARPAS422 cells harboring monoallelic Y641N EZH2 mutation assessed as reduction in cell viability measured every 3 to 4 days up to 14 days by Beckman Coulter-based method	[PMID: 28092155]
KARPAS-422	IC₅₀	0.294 μM Compound: 1; EPZ-6438	Antiproliferative activity against human KARPAS-422 cells expressing EZH2 Y641N mutant assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay Antiproliferative activity against human KARPAS-422 cells expressing EZH2 Y641N mutant assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay	[PMID: 37203326]
KARPAS-422	IC₅₀	3.86 nM Compound: 1; EPZ-6438	Antiproliferative activity against human KARPAS-422 cells harboring EZH2 Y641N mutant Antiproliferative activity against human KARPAS-422 cells harboring EZH2 Y641N mutant	[PMID: 37956762]
KARPAS-422	IC₅₀	35.01 nM Compound: 1; EPZ-6438	Antiproliferative activity against human KARPAS-422 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 method Antiproliferative activity against human KARPAS-422 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 method	[PMID: 38640588]
KMS-11	IC₅₀	>20 μM Compound: EPZ6438	Antiproliferative activity against human KMS-11 cells assessed as inhibition of cell growth incubated for 6 days by CCK-8 assay Antiproliferative activity against human KMS-11 cells assessed as inhibition of cell growth incubated for 6 days by CCK-8 assay	[PMID: 36642961]
L02	IC₅₀	>40 μM Compound: Tazemetostat	Antiproliferative activity against human L02 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human L02 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
LNCaP	GI₅₀	12 μM Compound: EPZ; EPZ6438	Synergistic growth inhibition of human LNCaP cells incubated for 6 to 7 days in presence of ORY1001 by MTS assay Synergistic growth inhibition of human LNCaP cells incubated for 6 to 7 days in presence of ORY1001 by MTS assay	[PMID: 39196854]
LNCaP	GI₅₀	13 μM Compound: EPZ; EPZ6438	Synergistic growth inhibition of human LNCaP cells incubated for 6 to 7 days in presence of TCP by MTS assay Synergistic growth inhibition of human LNCaP cells incubated for 6 to 7 days in presence of TCP by MTS assay	[PMID: 39196854]
LNCaP	GI₅₀	19.5 μM Compound: EPZ; EPZ6438	Growth inhibition of human LNCaP cells incubated for 6 to 7 days by MTS assay Growth inhibition of human LNCaP cells incubated for 6 to 7 days by MTS assay	[PMID: 39196854]
MCF-10A	IC₅₀	>40 μM Compound: Tazemetostat	Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MCF-10A	IC₅₀	>40 μM Compound: Taz	Cytotoxicity against human MCF-10A cells incubated for 72 hrs by MTT assay Cytotoxicity against human MCF-10A cells incubated for 72 hrs by MTT assay	[PMID: 38134746]
MCF-10A	IC₅₀	>40 μM Compound: Taz	Synergistic cytotoxicity against human MCF-10A cells incubated for 72 hrs in presence of Niraparib by MTT assay Synergistic cytotoxicity against human MCF-10A cells incubated for 72 hrs in presence of Niraparib by MTT assay	[PMID: 38134746]
MCF-10A	IC₅₀	>50 μM Compound: Taz	Antiproliferative activity against human MCF-10A cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF-10A cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 34455779]
MCF7	IC₅₀	>100 μM Compound: EPZ-6438	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
MCF7	IC₅₀	>40 μM Compound: Tazemetostat	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MCF7	IC₅₀	>50 μM Compound: Taz	Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 34455779]
MCF7	IC₅₀	>50 μM Compound: 6; EPZ-6438	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 35531606]
MDA-MB-231	GI₅₀	>10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human MDA-MB-231 cells expressing EZH2 assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human MDA-MB-231 cells expressing EZH2 assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
MDA-MB-231	IC₅₀	>20 μM Compound: 5; EPZ6438	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36153841]
MDA-MB-231	IC₅₀	>40 μM Compound: Tazemetostat	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MDA-MB-231	IC₅₀	11.07 μM Compound: Taz	Synergistic cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs in presence of Niraparib by MTT assay Synergistic cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs in presence of Niraparib by MTT assay	[PMID: 38134746]
MDA-MB-231	IC₅₀	44.45 μM Compound: Taz	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 34455779]
MDA-MB-231	IC₅₀	52.72 μM Compound: Taz	Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay	[PMID: 38134746]
MDA-MB-468	GI₅₀	>10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human MDA-MB-468 cells expressing EZH2 assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human MDA-MB-468 cells expressing EZH2 assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
MDA-MB-468	IC₅₀	>2.5 μM Compound: EPZ-6438	Anti-proliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 5 days incubation by CCK-8 assay Anti-proliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 5 days incubation by CCK-8 assay	[PMID: 38295690]
MDA-MB-468	IC₅₀	>40 μM Compound: Tazemetostat	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MDA-MB-468	IC₅₀	46.67 μM Compound: 6; EPZ-6438	Antiproliferative activity against human MDA-MB-468 cells Antiproliferative activity against human MDA-MB-468 cells	[PMID: 35531606]
MDA-MB-468	IC₅₀	46.76 μM Compound: Taz	Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 34455779]
Medulloblastoma cell	IC₅₀	8.74 μM Compound: Chemical Probe: EPZ6438	Antiproliferative activity in Ptch1-deficient mouse medulloblastoma cell after 48 hrs by CCK-8 assay Antiproliferative activity in Ptch1-deficient mouse medulloblastoma cell after 48 hrs by CCK-8 assay	[PMID: 32579914]
MV4-11	IC₅₀	>20 μM Compound: 5; EPZ6438	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36153841]
MV4-11	IC₅₀	>40 μM Compound: Tazemetostat	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MV4-11	IC₅₀	22.38 μM Compound: EPZ-6438	Antiproliferative activity against human MV4-11 cells Antiproliferative activity against human MV4-11 cells	[PMID: 31959420]
NCI-H1703	IC₅₀	>100 μM Compound: EPZ-6438	Antiproliferative activity against human NCI-H1703 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1703 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
OAW-42	IC₅₀	>100 μM Compound: EPZ-6438	Antiproliferative activity against human OAW-42 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human OAW-42 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
OPM-2	IC₅₀	>3 μM Compound: 1; EPZ-6438	Antiproliferative activity against human OPM-2 cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay Antiproliferative activity against human OPM-2 cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay	[PMID: 37203326]
OVCAR-3	IC₅₀	>100 μM Compound: EPZ-6438	Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
PA-1	IC₅₀	46.6 μM Compound: EPZ-6438	Antiproliferative activity against human PA-1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human PA-1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
PC-3	GI₅₀	>30 μM Compound: EPZ; EPZ6438	Growth inhibition of human PC-3 cells incubated for 6 to 7 days by MTS assay Growth inhibition of human PC-3 cells incubated for 6 to 7 days by MTS assay	[PMID: 39196854]
PC-3	GI₅₀	>30 μM Compound: EPZ; EPZ6438	Synergistic growth inhibition of human PC-3 cells incubated for 6 to 7 days in presence of ORY1001 by MTS assay Synergistic growth inhibition of human PC-3 cells incubated for 6 to 7 days in presence of ORY1001 by MTS assay	[PMID: 39196854]
PC-3	GI₅₀	>30 μM Compound: EPZ; EPZ6438	Synergistic growth inhibition of human PC-3 cells incubated for 6 to 7 days in presence of TCP by MTS assay Synergistic growth inhibition of human PC-3 cells incubated for 6 to 7 days in presence of TCP by MTS assay	[PMID: 39196854]
Pfeiffer	GI₅₀	0.002 μM Compound: 1; EPZ-6438	Antiproliferative activity against human Pfeiffer cells harboring EZH2 A677G mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human Pfeiffer cells harboring EZH2 A677G mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
Pfeiffer	GI₅₀	0.01 μM Compound: 1; EPZ-6438	Antiproliferative activity against human Pfeiffer cells expressing A677G mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human Pfeiffer cells expressing A677G mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
Pfeiffer	IC₅₀	0.034 μM Compound: 1; EPZ-6438	Antiproliferative activity against human Pfeiffer cells expressing EZH2 Y641N mutant assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay Antiproliferative activity against human Pfeiffer cells expressing EZH2 Y641N mutant assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay	[PMID: 37203326]
Pfeiffer	IC₅₀	2.26 nM Compound: 1; EPZ-6438	Antiproliferative activity against human Pfeiffer cells harboring EZH2 A677G mutant Antiproliferative activity against human Pfeiffer cells harboring EZH2 A677G mutant	[PMID: 37956762]
Pfeiffer	IC₅₀	38 nM Compound: EPZ-6438	Cytotoxicity against human Pfeiffer cells assessed as decrease in cell viability after 5 days by CellTiter-Glo reagent based luminescence assay Cytotoxicity against human Pfeiffer cells assessed as decrease in cell viability after 5 days by CellTiter-Glo reagent based luminescence assay	[PMID: 29456795]
Raji	GI₅₀	>10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human Raji cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human Raji cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
Raji	GI₅₀	>10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human Raji cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human Raji cells assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
RD	CC₅₀	244.78 μM Compound: Tazemetostat	Cytotoxicity against human RD cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human RD cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 37021456]
SK-BR-3	IC₅₀	67.1 μM Compound: EPZ-6438	Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
SK-OV-3	IC₅₀	89.8 μM Compound: EPZ-6438	Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
SUD4	GI₅₀	>10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human SU-DHL-4 cells expressing Y641S mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human SU-DHL-4 cells expressing Y641S mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
SUD4	GI₅₀	3.39 μM Compound: 1; EPZ-6438	Antiproliferative activity against human SU-DHL-4 cells harboring EZH2 Y641S mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human SU-DHL-4 cells harboring EZH2 Y641S mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
SUD4	IC₅₀	14.34 μM Compound: EPZ-6438	Antiproliferative activity against over expressing E2H2 human SUDHL4 cells Antiproliferative activity against over expressing E2H2 human SUDHL4 cells	[PMID: 31959420]
SU-DHL10	IC₅₀	>20 μM Compound: 5; EPZ6438	Antiproliferative activity against human SU-DHL-10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human SU-DHL-10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36153841]
SU-DHL-2	IC₅₀	>3 μM Compound: 1; EPZ-6438	Antiproliferative activity against human SUDHL2 cells expressing EZH2 mutant assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay Antiproliferative activity against human SUDHL2 cells expressing EZH2 mutant assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay	[PMID: 37203326]
SU-DHL-6	GI₅₀	>10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human SU-DHL-6 cells expressing Y641N mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human SU-DHL-6 cells expressing Y641N mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
SU-DHL-6	GI₅₀	1.05 μM Compound: 1; EPZ-6438	Antiproliferative activity against human SU-DHL-6 cells harboring EZH2 Y641N mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human SU-DHL-6 cells harboring EZH2 Y641N mutant assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
SU-DHL-6	IC₅₀	21.95 μM Compound: EPZ-6438	Antiproliferative activity against human SU-DHL-6 cells Antiproliferative activity against human SU-DHL-6 cells	[PMID: 38056296]
SW982	CC₅₀	116.43 μM Compound: Tazemetostat	Cytotoxicity against human SW982 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human SW982 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 37021456]
U2932	GI₅₀	>10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human U2932 cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay Antiproliferative activity against human U2932 cells expressing wild type EZH2 assessed as inhibition of cell growth measured after 6 days by CellTiter-Glo luminescent assay	[PMID: 34664960]
U2932	IC₅₀	>3 μM Compound: 1; EPZ-6438	Antiproliferative activity against human U2932 cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay Antiproliferative activity against human U2932 cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay	[PMID: 37203326]
WSUDLCL2	GI₅₀	>10 μM Compound: 1; EPZ-6438	Antiproliferative activity against human WSUDLCL2 cells expressing Y641F mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay Antiproliferative activity against human WSUDLCL2 cells expressing Y641F mutant assessed as cell growth inhibition incubated for 5 days by CellTiter-Glo assay	[PMID: 37826933]
WSUDLCL2	IC₅₀	>3 μM Compound: 1; EPZ-6438	Antiproliferative activity against human WSUDLCL2 cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay Antiproliferative activity against human WSUDLCL2 cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay	[PMID: 37203326]
WSUDLCL2	IC₅₀	6.44 nM Compound: 1; EPZ-6438	Antiproliferative activity against human WSUDLCL2 cells harboring EZH2 Y641F mutant Antiproliferative activity against human WSUDLCL2 cells harboring EZH2 Y641F mutant	[PMID: 37956762]

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.

Cell Proliferation Assay^[1]

Cell Line:

Wild-type and mutant lymphoma cell lines
Concentration:

0.49-7.6 μM
Incubation Time:

11 days
Result:

Inhibited DOHH-2 cell (EZH2 wild-type; IC₅₀=1.7 μM), Farage cell (EZH2 wild-type; IC₅₀=99 nM), OCI-LY19 cell (EZH2 wild-type; IC₅₀=6.2 μM), Toledo cell (EZH2 wild-type; IC₅₀=7.6 μM), KARPAS-422 (EZH2 Y646N; IC₅₀=1.8 nM), Pfeiffer (EZH2 A682G; IC₅₀=0.49 nM), RL cell line (EZH2 Y646N; IC₅₀=5.8 μM), SU-DHL-10 (EZH2 Y646F; IC₅₀=5.8 nM), SU-DHL-6 (EZH2 Y646N; IC₅₀=4.7 nM), WSU-DLCL2 (EZH2 Y646F; IC₅₀=8.6 nM) proliferation.

In Vivo

Tazemetostat (EPZ-6438; 250 or 500 mg/kg twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors^[1].

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

Animal Model:

SCID mice bearing s.c. G401 xenografts^[1]
Dosage:

125 mg/kg, 250 mg/kg and 500 mg/kg
Administration:

Oral administration; twice daily; 28 days
Result:

Eliminated the fast-growing G401 tumors.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1403254-99-8
Appearance Solid
Molecular Weight 572.74
Formel C₃₄H₄₄N₄O₄
Color White to light yellow
SMILES

O=C(C1=CC(C2=CC=C(CN3CCOCC3)C=C2)=CC(N(CC)C4CCOCC4)=C1C)NCC5=C(C)C=C(C)NC5=O
Synonyms

EPZ-6438; E-7438
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (96)

All WB

Sort by:

Journal Impact Factor

Nat Med

Targeting glioma stem cells through combined BMI1 and EZH2 inhibition. [Abstract]

2017 Nov;23(11):1352-1361. PMID: 29035367
Nature

Targeting Xist with compounds that disrupt RNA structure and X inactivation. [Abstract]

2022 Apr;604(7904):160-166. PMID: 35355011
Cell

p53 safeguards chemical reprogramming of human somatic cells toward pluripotency. [Abstract]

2026 Jun 11;189(12):3541-3552.e18. PMID: 41999746
Cell Stem Cell

Inhibition of PRC2 enables self-renewal of blastoid-competent naive pluripotent stem cells from chimpanzee. [Abstract]

2025 Apr 3;32(4):627-639.e8. PMID: 40015279
Cell Mol Immunol

EZH2 and intracellular Ca2+ signals interdependently coordinate alloreactive and CAR-T-cell responses. [Abstract]

2026 Jul;23(7):840-854. PMID: 42020715
Adv Funct Mater

2024 Jun 20.
Mol Cell

Histone methylation antagonism drives tumor immune evasion in squamous cell carcinomas. [Abstract]

2022 Oct 20;82(20):3901-3918.e7. PMID: 36206767
Cancer Res

Pathogenic Epigenetic Consequences of Genetic Alterations in IDH-Wild-Type Diffuse Astrocytic Gliomas. [Abstract]

2019 Oct 1;79(19):4814-4827. PMID: 31431463
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

Context-defined cancer co-dependency mapping identifies a functional interplay between PRC2 and MLL-MEN1 complex in lymphoma. [Abstract]

2023 Jul 17;14(1):4259. PMID: 37460547
Nat Commun

Polycomb deficiency drives a FOXP2-high aggressive state targetable by epigenetic inhibitors. [Abstract]

2023 Jan 20;14(1):336. PMID: 36670102
Nat Commun

An ErbB2/c-Src axis links bioenergetics with PRC2 translation to drive epigenetic reprogramming and mammary tumorigenesis. [Abstract]

2019 Jul 1;10(1):2901. PMID: 31263101
Adv Sci (Weinh)

Allosteric Inhibition of Polycomb Repressive Complex 2 by an EZH2-Selective Small Molecule Inhibitor. [Abstract]

2026 Jun 18:e76025. PMID: 42314051
Adv Sci (Weinh)

PRC2.1 Coordinates Peri-Nucleolar H3K27me3-Enriched Heterochromatin Organization and NPM1 Pentamerization to Maintain Nucleolar Integrity. [Abstract]

2026 Jun 16:e19359. PMID: 42299771
J Clin Invest

Shifts in podocyte histone H3K27me3 regulate mouse and human glomerular disease. [Abstract]

2018 Jan 2;128(1):483-499. PMID: 29227285

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.
Exp Hematol Oncol

Targeted degradation of sICOSL reverses cytotoxic T cells dysfunction. [Abstract]

2025 Jul 24;14(1):100. PMID: 40708008
Biomaterials

Epigenetic reprogramming of carrier free photodynamic modulator to activate tumor immunotherapy by EZH2 inhibition. [Abstract]

2023 Feb:293:121952. PMID: 36502580
Metabolism

Liver cancer chronically exposed to palmitate acquires ferroptosis resistance via the downregulation of glutamine-driven hepcidin expression. [Abstract]

2025 Dec 17:176:156469. PMID: 41418943
Cancer Lett

EZH2 inhibition confers PIK3CA-driven lung tumors enhanced sensitivity to PI3K inhibition. [Abstract]

2022 Jan 1:524:151-160. PMID: 34655667
Nat Struct Mol Biol

Accurate H3K27 methylation can be established de novo by SUZ12-directed PRC2. [Abstract]

2018 Mar;25(3):225-232. PMID: 29483650

Tazemetostat purchased from MedChemExpress. Usage Cited in: Nat Struct Mol Biol. 2018 Mar;25(3):225-232. [Abstract]

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.
Cell Death Dis

Multi-omics analyses identify EZH2 as a central driver in rhabdomyosarcoma radioresistance and highlight Tazemetostat as an effective radiosensitizer in vitro and in vivo. [Abstract]

2026 Jun 1. PMID: 42225614
Cell Death Dis

Targeting EZH2-driven cholesterol metabolic vulnerability through Napabucasin suppresses ovarian cancer metastasis. [Abstract]

2026 Jun 27;17(1):603. PMID: 42373608
Cell Death Dis

NRF1 predominantly causes EZH2 overexpression in cancer cells. [Abstract]

2026 May 16. PMID: 42140904
Cell Death Dis

A targetable antioxidant defense mechanism to EZH2 inhibitors enhances tumor cell vulnerability to ferroptosis. [Abstract]

2025 Apr 14;16(1):291. PMID: 40229247
Cell Death Dis

Integration of epigenomic and transcriptomic profiling uncovers EZH2 target genes linked to cysteine metabolism in hepatocellular carcinoma. [Abstract]

2024 Nov 8;15(11):801. PMID: 39516467
Cell Death Dis

Induction of senescence-associated secretory phenotype underlies the therapeutic efficacy of PRC2 inhibition in cancer. [Abstract]

2022 Feb 15;13(2):155. PMID: 35169119

Tazemetostat purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Feb 15;13(2):155. [Abstract]

EED226 (0.04-10 μM; 72 h) dose-dependently inhibited cellular H3K27me3 in HeLa cells.
Acta Pharmacol Sin

AZD9291 inactivates the PRC2 complex to mediate tumor growth inhibition. [Abstract]

2019 Dec;40(12):1587-1595. PMID: 31171828
Apoptosis

Valproic acid upregulates the expression of the p75NTR/sortilin receptor complex to induce neuronal apoptosis. [Abstract]

2020 Oct;25(9-10):697-714. PMID: 32712736
NPJ Precis Oncol

Lethal co-expression intolerance underlies the mutually exclusive expression of ASCL1 and NEUROD1 in SCLC cells. [Abstract]

2025 Mar 13;9(1):74. PMID: 40082639
J Orthop Translat

2026 Jan 22.
Neoplasia

Cholesterol biosynthesis as a drug-induced vulnerability in diffuse large B cell lymphoma insensitive to EZH2 inhibition. [Abstract]

2025 Oct 27:70:101243. PMID: 41151153
Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
NPJ Breast Cancer

Epigenetically upregulating TROP2 and SLFN11 enhances therapeutic efficacy of TROP2 antibody drug conjugate sacitizumab govitecan. [Abstract]

2023 Aug 11;9(1):66. PMID: 37567892
Cell Mol Gastroenterol Hepatol

Pbrm1 Loss Induces a Permissive Chromatin State for Cholangiocytic Differentiation and Cholangiocarcinoma Formation. [Abstract]

2026 Jan 7:101720. PMID: 41513002
Oncogene

BRD4 inhibition sensitizes cervical cancer to radiotherapy by attenuating DNA repair. [Abstract]

2021 Apr;40(15):2711-2724. PMID: 33712705
Cell Rep

miR-449a/miR-340 reprogram cell identity and metabolism in fusion-negative rhabdomyosarcoma. [Abstract]

2025 Jan 11;44(1):115171. PMID: 39799567
Cell Rep

Nucleation and spreading maintain Polycomb domains every cell cycle. [Abstract]

2024 Apr 23;43(4):114090. PMID: 38607915
Cell Rep

Reduction of Global H3K27me3 Enhances HER2/ErbB2 Targeted Therapy. [Abstract]

2019 Oct 8;29(2):249-257.e8. PMID: 31597089
Cell Rep

Domain Model Explains Propagation Dynamics and Stability of Histone H3K27 and H3K36 Methylation Landscapes. [Abstract]

2020 Jan 28;30(4):1223-1234.e8. PMID: 31995760
Clin Transl Med

Inhibition of HDAC2 sensitises antitumour therapy by promoting NLRP3/GSDMD-mediated pyroptosis in colorectal cancer. [Abstract]

2024 Jun;14(6):e1692. PMID: 38804602
J Med Chem

Discovery of IHMT-EZH2-115 as a Potent and Selective Enhancer of Zeste Homolog 2 (EZH2) Inhibitor for the Treatment of B-Cell Lymphomas. [Abstract]

2021 Oct 28;64(20):15170-15188. PMID: 34664960
Elife

SIRT1 regulates sphingolipid metabolism and neural differentiation of mouse embryonic stem cells through c-Myc-SMPDL3B. [Abstract]

2021 May 27:10:e67452. PMID: 34042046
Cell Mol Life Sci

KLF15 suppresses stemness of pancreatic cancer by decreasing USP21-mediated Nanog stability. [Abstract]

2024 Oct 5;81(1):417. PMID: 39367978
EMBO Rep

IκBα deficiency imposes a fetal phenotype to intestinal stem cells. [Abstract]

2020 Jun 4;21(6):e49708. PMID: 32270911
Eur J Med Chem

Discovery of dihydropyridinone derivative as a covalent EZH2 degrader. [Abstract]

2023 Dec 5:261:115825. PMID: 37826933
Front Immunol

The Chemokine Receptor CCR8 Is a Target of Chimeric Antigen T Cells for Treating T Cell Malignancies. [Abstract]

2022 May 26:13:808347. PMID: 35693763
Biochem Pharmacol

Opposing outcomes of short- and long-term epigenetic therapy in breast cancer: Implications for chemotherapy response. [Abstract]

2026 Jan;243(Pt 2):117535. PMID: 41213410
Cell Prolif

EZH2-mediated inhibition of KLF14 expression promotes HSCs activation and liver fibrosis by downregulating PPARγ. [Abstract]

2021 Jul;54(7):e13072. PMID: 34031939

Tazemetostat purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2021 Jul;54(7):e13072. [Abstract]

The HSCs shown were treated with DNMT inhibitors (5-azacytidine, 2 μmol/L), G9a inhibitors (UNC0642, 2 μmol/L), and pan-HDAC inhibitor Givinostat (ITF-2357, 100 nmol/L) for 48 hours, or with EZH2 inhibitors (EPZ-6438, 10 μmol/L) for 72 hours. KLF14 expression was detected by Western blotting.
Genetics

Analysis of a BCOR internal tandem duplication in mouse embryonic stem cell to neuronal precursor differentiation. [Abstract]

2025 Sep 3;231(1):iyaf133. PMID: 40646718
Int J Mol Sci

Biological Evaluation of a Novel Compound with Predicted EZH2 and EED Binding Against Human Malignant Melanoma Cells. [Abstract]

2026 Mar 13;27(6):2647. PMID: 41898517
PLoS Pathog

BRD4 inhibition exerts anti-viral activity through DNA damage-dependent innate immune responses. [Abstract]

2020 Mar 24;16(3):e1008429. PMID: 32208449
Mol Oncol

Dual inhibition of DNMTs and EZH2 can overcome both intrinsic and acquired resistance of myeloma cells to IMiDs in a cereblon-independent manner. [Abstract]

2018 Feb;12(2):180-195. PMID: 29130642
Cancers (Basel)

Evaluation of Combined Chemotherapy and Genomic-Driven Targeted Therapy in Patient-Derived Xenografts Identifies New Therapeutic Approaches in Squamous Non-Small-Cell Lung Cancer Patients. [Abstract]

2024 Aug 7;16(16):2785. PMID: 39199558
Cancers (Basel)

SAM-Competitive EZH2-Inhibitors Induce Platinum Resistance by EZH2-Independent Induction of ABC-Transporters. [Abstract]

2023 Jun 3;15(11):3043. PMID: 37297005
Eur J Cell Biol

The PRC2 molecule EED is a target of epigenetic therapy for neuroblastoma. [Abstract]

2022 May 20;101(3):151238. PMID: 35636260
FASEB J

H3K27me3 Modified FBXO10 Promotes Golgi Stress to Accelerate Traumatic Brain Injury via Activation of the RAS/ERK Axis. [Abstract]

2026 Apr 30;40(8):e71791. PMID: 41999223
J Cell Mol Med

Curcumin inhibits the growth of triple-negative breast cancer cells by silencing EZH2 and restoring DLC1 expression. [Abstract]

2020 Sep;24(18):10648-10662. PMID: 32725802
J Cell Mol Med

Combined tazemetostat and MAPKi enhances differentiation of papillary thyroid cancer cells harbouring BRAFV600E by synergistically decreasing global trimethylation of H3K27. [Abstract]

2020 Mar;24(6):3336-3345. PMID: 31970877
iScience

CD2 costimulation strength: A key regulator of T cell function and anti-tumor immunity that is epigenetically regulated. [Abstract]

2025 Nov 10;28(12):113977. PMID: 41377664
Toxins

HDAC8 Prevents Anthrax Lethal Toxin-induced Cell Cycle Arrest through Silencing PTEN in Human Monocytic THP-1 Cells. [Abstract]

2017 May 16;9(5). pii: E162. PMID: 28509866

Tazemetostat purchased from MedChemExpress. Usage Cited in: Toxins. 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.
J Biol Chem

PPARγ and C/EBPα enable adipocyte differentiation upon inhibition of histone methyltransferase PRC2 in malignant tumors. [Abstract]

2024 Sep 12:107765. PMID: 39276936
Sci Rep

A membrane transporter determines the spectrum of activity of a potent platinum-acridine hybrid anticancer agent. [Abstract]

2020 Sep 16;10(1):15201. PMID: 32939009
Biochim Biophys Acta Mol Cell Res

EZH2-mediated hypermethylation of H3K27me3 downregulates claudin-4 and upregulates the Wnt/β-catenin signaling pathway in hepatocellular carcinoma metastasis. [Abstract]

2026 Jan;1873(1):120076. PMID: 41187860
Heliyon

Derepressing of STAT3 and USP7 contributes to resistance of DLBCL to EZH2 inhibition. [Abstract]

2023 Oct 5;9(10):e20650. PMID: 37829803
Hum Cell

EZH2 regulates tumor-associated macrophages by the KDM6A-mediated inflammatory response in HPV16-positive cervical cancer. [Abstract]

2025 Jun 19;38(4):119. PMID: 40536676
Int J Clin Oncol

Cell-type-specific sensitivity of bortezomib in the methotrexate-resistant primary central nervous system lymphoma cells. [Abstract]

2019 Sep;24(9):1020-1029. PMID: 30993483
Exp Eye Res

Inhibition of enhancer of zeste homolog 2 prevents corneal myofibroblast transformation in vitro. [Abstract]

2021 Jul:208:108611. PMID: 33992624
Epigenomics

EZH2 inhibition enhances the activity of Carboplatin in aggressive-variant prostate cancer cell lines. [Abstract]

2025 Jan 29:1-10. PMID: 39878501
PLoS One

MAP1LC3C repression reduces CIITA- and HLA class II expression in non-small cell lung cancer. [Abstract]

2025 Feb 10;20(2):e0316716. PMID: 39928678
bioRxiv

Spatially-Resolved Multiomic Atlas of Leiomyosarcoma Identifies Two Clinically Relevant Epigenetically-Driven Cell States. [Abstract]

2026 May 26:2026.05.22.726988. PMID: 42244620
bioRxiv

Radiation synergizes with BET inhibition to stimulate durable, systemic anti-tumor immunity in murine cancer models. [Abstract]

2026 Feb 18:2026.02.16.706212. PMID: 41757027
Indiana University

2026.
bioRxiv

2026 Feb 25.
bioRxiv

Multiplexed measurements of protein-protein interactions and protein abundance across cellular conditions using Prod&PQ-seq. [Abstract]

2026 Jan 14:2026.01.01.697286. PMID: 41509405
Res Sq

2025 Oct 6.
bioRxiv

2025 Sep 9.
Patent

US20250152731A1.
University of Toronto

2025.
bioRxiv

2025 February 12.
Patent

US20240390379A1.
Patent

US20240252638A1.
bioRxiv

2024 September 11.
Indiana University

2024.
biorxiv

2024 Jun 08.
Research Square Preprint

2024 Feb 7.
University of Kentucky

2023 Aug 20.
bioRxiv

EZH2 inhibition promotes tumor immunogenicity in lung squamous cell carcinomas. [Abstract]

2023 Jun 8:2023.06.06.543919. PMID: 37333199
bioRxiv

May 31, 2022.
Utrecht University

2023 Feb.
University of Kentucky

2021 May.
Università degli Studi di CAGLIARI

2021 May.
bioRxiv

2021 Jan 1.
Medicines (Basel)

Effect of Sulforaphane and 5-Aza-2'-Deoxycytidine on Melanoma Cell Growth. [Abstract]

2019 Jun 27;6(3):71. PMID: 31252639
bioRxiv

April.
Patent

US20180263995A1.
Oncotarget

Androgen receptor mitigates postoperative disease progression of hepatocellular carcinoma by suppressing CD90+ populations and cell migration and by promoting anoikis in circulating tumor cells. [Abstract]

2016 Jul 19;7(29):46448-46465. PMID: 27340775

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 58.33 mg/mL (101.84 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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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

Solubility: ≥ 2.08 mg/mL (3.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO 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.

Protocol 4

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

Solubility: ≥ 2.08 mg/mL (3.63 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.63 mM); Clear solution

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 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

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Data Sheet (279 KB)
SDS (393 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
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
	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
	60 mM	0.0291 mL	0.1455 mL	0.2910 mL	0.7275 mL
	80 mM	0.0218 mL	0.1091 mL	0.2182 mL	0.5456 mL
	100 mM	0.0175 mL	0.0873 mL	0.1746 mL	0.4365 mL

Keywords

Tazemetostat

96 Cited Publications

100 mg Angebot einholen

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Tazemetostat

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

FDA-Approved Drug Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Chemical Probe Library

FDA Approved & Pharmacopeial Drug Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Rare Diseases Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Anti-Cancer Approved Drug Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

RNA Binding Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Tazemetostat

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (96)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tazemetostat Related Classifications

HY-13803 Related Classifications