Product 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].
Applications: Cancer-programmed cell death
Formula: C34H44N4O4
Citations: 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 Death Dis. 2024 Nov 8;15(11):801./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./Patent. US20240390379A1./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.
References: [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.
CAS Number: 1403254-99-8
Molecular Weight: 572.74
Compound Purity: 99.93
Research Area: Cancer
Solubility: 0.1 M HCL : 14.29 mg/mL (ultrasonic;adjust pH to 5 with HCl)/DMSO : 31.25 mg/mL (ultrasonic;warming;heat to 60°C)
Target: Apoptosis;Histone Methyltransferase
English
Deutsch
