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Tazemetostat

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].

Product Specifications

CAS Number

[1403254-99-8]

Product Name Alternative

EPZ-6438; E-7438

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Histone Methyltransferase

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/EPZ-6438.html

Purity

99.93

Solubility

DMSO : 58.33 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

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

Molecular Formula

C34H44N4O4

Molecular Weight

572.74

Precautions

H302, H315, H319, H335

References & Citations

[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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

EZH2

Citation 01

Acta Pharmacol Sin. 2019 Dec;40 (12) :1587-1595.|Adv Funct Mater. 2024 Jun 20.|Apoptosis. 2020 Oct;25 (9-10) :697-714.|Biochem Pharmacol. 2026 Jan;243 (Pt 2) :117535.|Biochim Biophys Acta Mol Cell Res. 2026 Jan;1873 (1) :120076.|Biomaterials. 2023 Feb:293:121952.|bioRxiv. 2021 Feb 25.|bioRxiv. 2021 Jan 1.|bioRxiv. 2023 Jun 8:2023.06.06.543919.|biorxiv. 2024 Jun 08.|bioRxiv. 2024 September 11.|bioRxiv. 2025 February 12.|bioRxiv. 2025 Sep 9.|bioRxiv. April.|bioRxiv. May 31, 2022.|Cancer Lett. 2022 Jan 1:524:151-160.|Cancer Res. 2019 Oct 1;79 (19) :4814-4827.|Cancers (Basel) . 2023 Jun 3;15 (11) :3043.|Cancers (Basel) . 2024 Aug 7;16 (16) :2785.|Cell Death Dis. 2022 Feb 15;13 (2) :155.|Cell Death Dis. 2024 Nov 8;15 (11) :801.|Cell Death Dis. 2025 Apr 14;16 (1) :291.|Cell Mol Life Sci. 2024 Oct 5;81 (1) :417.|Cell Prolif. 2021 Jul;54 (7) :e13072.|Cell Rep. 2020 Jan 28;30 (4) :1223-1234.e8.|Cell Rep. 2024 Apr 23;43 (4) :114090.|Cell Rep. 2025 Jan 11;44 (1) :115171.|Cell Rep. 2019 Oct 8;29 (2) :249-257.e8. |Cell Rep. 2020 Jan 28;30 (4) :1223-1234.e8.|Cell Stem Cell. 2025 Apr 3;32 (4) :627-639.e8.|Clin Transl Med. 2024 Jun;14 (6) :e1692.|Elife. 2021 May 27;10:e67452.|EMBO Rep. 2020 Jun 4;21 (6) :e49708.|Epigenomics. 2025 Jan 29:1-10.|Eur J Cell Biol. 2022 May 20;101 (3) :151238.|Eur J Med Chem. 2023 Dec 5:261:115825.|Exp Eye Res. 2021 Jul:208:108611.|Exp Hematol Oncol. 2025 Jul 24;14 (1) :100.|Front Immunol. 2022 May 26:13:808347.|Genetics. 2025 Sep 3;231 (1) :iyaf133.|Heliyon. 2023 Oct 5;9 (10) :e20650.|Hum Cell. 2025 Jun 19;38 (4) :119.|Indiana University. 2024.|Int J Clin Oncol. 2019 Sep;24 (9) :1020-1029.|iScience. 2025 Nov 10;28 (12) :113977.|J Biol Chem. 2024 Sep 12:107765.|J Cell Mol Med. 2020 Mar;24 (6) :3336-3345.|J Cell Mol Med. 2020 Sep;24 (18) :10648-10662.|J Clin Invest. 2018 Jan 2;128 (1) :483-499. |J Med Chem. 2021 Oct 28;64 (20) :15170-15188.|Medicines (Basel) . 2019 Jun 27;6 (3) :71.|Mol Cell. 2022 Oct 20;82 (20) :3901-3918.e7.|Mol Oncol. 2018 Feb;12 (2) :180-195.|Mol Syst Biol. 2024 Jan;20 (1) :28-55.|Nat Commun. 2023 Jan 20;14 (1) :336.|Nat Commun. 2023 Jul 17;14 (1) :4259.|Nat Commun. 2019 Jul 1;10 (1) :2901. |Nat Med. 2017 Nov;23 (11) :1352-1361.|Nat Struct Mol Biol. 2018 Mar;25 (3) :225-232.|Nature. 2022 Apr;604 (7904) :160-166.|Neoplasia. 2025 Oct 27:70:101243.|NPJ Breast Cancer. 2023 Aug 11;9 (1) :66.|NPJ Precis Oncol. 2025 Mar 13;9 (1) :74.|Oncogene. 2021 Apr;40 (15) :2711-2724.|Oncotarget. 2016 Jul 19;7 (29) :46448-46465. |Patent. US20180263995A1.|Patent. US20240252638A1.|Patent. US20240390379A1.|Patent. US20250152731A1.|PLoS One. 2025 Feb 10;20 (2) :e0316716.|PLoS Pathog. 2020 Mar 24;16 (3) :e1008429.|Res Sq. 2025 Oct 6.|Research Square Preprint. 2024 Feb 7.|Sci Rep. 2020 Sep 16;10 (1) :15201.|Toxins. 2017 May 16;9 (5) . pii: E162.|Università degli Studi di CAGLIARI. Dipartimento di Scienze Biomediche. 2021 May.|University of Kentucky. 2023 Aug 20.|University of Kentucky. Toxicology and Cancer Biology. 2021 May.|University of Toronto. 2025.|Utrecht University. 2023 Feb.|Adv Sci (Weinh) . 2022 Dec;9 (34) :e2203088.|Utrecht University. 2025.

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