Tazemetostat

• UNSPSC Description:

  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].

• Target Antigen:

  Apoptosis; Histone Methyltransferase

• Type:

  Reference compound

• Related Pathways:

  Apoptosis;Epigenetics

• Field of Research:

  Cancer

• Assay Protocol:

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

• 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 Weight:

  572.74

• 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.Acta Pharmacol Sin. 2019 Dec;40(12):1587-1595. |Adv Funct Mater. 2024 Jun 20.|Apoptosis. 2020 Oct;25(9-10):697-714.|Biomaterials. 2022 Dec 7;293:121952.|bioRxiv. 2021 Feb 25.|bioRxiv. 2021 Jan 1.|bioRxiv. 2023 Jun 8.|biorxiv. 2024 Jun 08.|bioRxiv. 2024 September 11.|bioRxiv. April.|bioRxiv. May 31, 2022.|Cancer Lett. 2021 Oct 13;S0304-3835(21)00520-6.|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 Mol Life Sci. 2024 Oct 5;81(1):417.|Cell Prolif. 2021 May 24;e13072.|Cell Rep. 2020 Jan 28;30(4):1223-1234.e8.|Cell Rep. 2024 Apr 23;43(4):114090.|Cell Rep. 2019 Oct 8;29(2):249-257.e8. |Cell Rep. 2020 Jan 28;30(4):1223-1234.e8.|Clin Transl Med. 2024 Jun;14(6):e1692.|Elife. 2021 May 27;10:e67452.|EMBO Rep. 2020 Jun 4;21(6):e49708.|Eur J Cell Biol. 2022 May 20;101(3):151238.|Eur J Med Chem. 2023 Oct 2, 115825.|Exp Eye Res. 2021 May 13;108611.|Front Immunol. 26 May 2022.|Heliyon. 2023 Oct 3.|Int J Clin Oncol. 2019 Sep;24(9):1020-1029. |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 19.|Medicines (Basel). 2019 Jun 27;6(3):71. |Mol Cell. 2022 Sep 29;S1097-2765(22)00896-6.|Mol Oncol. 2018 Feb;12(2):180-195.|Mol Syst Biol. 2023 Dec 18.|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.|NPJ Breast Cancer. 2023 Aug 11;9(1):66.|Oncogene. 2021 Apr;40(15):2711-2724.|Oncotarget. 2016 Jul 19;7(29):46448-46465. |Patent. US20180263995A1.|Patent. US20240252638A1.|PLoS Pathog. 2020 Mar 24;16(3):e1008429.|Research Square Preprint. 2024 Feb 7.|Sci Rep. 2020 Sep 16;10(1):15201.|Toxins (Basel). 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.|Utrecht University. 2023 Feb.|Adv Sci (Weinh). 2022 Oct 18;e2203088.

• Shipping Conditions:

  Room Temperature

• CAS Number:

  1403254-99-8