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EZH2 Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
E4850 Tazemetostat hydrobromide Tazemetostat hydrobromide (EPZ-6438 hydrobromide) is a potent, selective, and orally available inhibitor of EZH2. It inhibits EZH2 with IC50 values of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide also inhibits EZH1 with an IC50 of 392 nM.
S8702 EBI-2511 EBI-2511 is a highly potent and orally active EZH2 inhibitor with an IC50 of 4 nM for EZH2(A667G).
S7165 UNC1999 UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets. This compound is a potent autophagy inducer. It specifically suppresses H3K27me3/2 and induces a range of anti-leukemia effects including anti-proliferation, differentiation, and apoptosis.
Cell Stem Cell, 2025, S1934-5909(25)00041-4
Cell Rep, 2025, 44(5):115673
bioRxiv, 2025, 2025.05.22.655558
Verified customer review of UNC1999
S7004 EPZ005687 EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM in a cell-free assay, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
Genome Biol, 2025, 26(1):307
Commun Biol, 2024, 7(1):1535
J Exp Clin Cancer Res, 2023, 42(1):320
Verified customer review of EPZ005687
S7805 EPZ011989 EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM.
Cancers (Basel), 2024, 16(3):569.
Cancers (Basel), 2024, 16(3)569
Sci Adv, 2024, 10(13):eadk4423
S7804 GSK503 GSK503 is a potent and specific EZH2 methyltransferase inhibitor.
JCI Insight, 2025, e177545
Int J Mol Sci, 2023, 24(10)8603
Cancer Res, 2022, CAN-22-0736
Verified customer review of GSK503
S7616 CPI-169 CPI-169 is a potent, and selective EZH2 inhibitor with IC50 of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.
J Exp Clin Cancer Res, 2023, 42(1):96
Nat Commun, 2022, 13(1):6226
Cell Chem Biol, 2021, S2451-9456(21)00213-0
S7611 EI1 EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
NPJ Precis Oncol, 2025, 9(1):7
Cancer Res, 2018, 78(20):5731-5740
Elife, 2018, 7e35368
Verified customer review of EI1
S9031 Gambogenic acid Gambogenic Acid, identified from Gamboge, is an inhibitor of the FGFR signaling pathway in non-small-cell lung cancer (NSCLC) and exhibits anti-tumor effects. This compound is also an effective inhibitor of EZH2 that specifically and covalently binds to Cys668 within the EZH2-SET domain, and triggers EZH2 ubiquitination.
Cancer Biol Ther, 2024, 25(1):2427374
Chem Biol Interact, 2023, 382:110602
Oncotarget, 2021, 12(6):549-561
S8494 PF-06726304 PF-06726304 is a selective EZH2 inhibitor with Ki values of 0.7 nM and 3 nM for WT EZH2 and Y641N respectively; this compound also inhibits H3K27me3 with the IC50 value of 15 nM.
NPJ Precis Oncol, 2025, 9(1):7
Nat Commun, 2023, 10.1038/s41467-023-42930-y
Elife, 2021, 10e65654
S8607 JQ-EZ-05 (JQEZ5) JQ-EZ-05 (JQEZ5) is a specific and reversible EZH1/2 inhibitor.
Nat Chem Biol, 2019, 15(4):391-400
S8918 MS1943 MS1943 is an orally bioavailable EZH2 selective degrader that effectively reduces EZH2 levels in cells with IC50 of 120 nM for inhibiting EZH2 methyltransferase activity.
Nat Commun, 2024, 15(1):9755
E1163 MS177 MS177 is an EZH2-targeting PRTOAC degrader and a potent inhibitor of enzymatic EZH2, that effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukemia cell growth inhibition, apoptosis, and cell cycle progression arrest.
S1803 5-Boc-amino-pentanoic acid 5-Boc-amino-pentanoic acid (Boc-5-aminovaleric acid, Boc-NH-C4-acid, Boc-5-Ava-OH) is a PROTAC linker that belongs to a Alkyl/ether linker. Boc-NH-C4-acid is applicable to the synthesis of PROTAC1, and specifically degrades EED, EZH2, and SUZ12 in the PRC2 Complex.