2. Signaling Pathways
  3. Epigenetics
  4. Histone Methyltransferase
  5. EZH2 Isoform
  6. EZH2 Inhibitor

EZH2 Inhibitor

EZH2 Inhibitors (58):

Cat. No. Product Name Effect Purity
  • HY-13803
    Tazemetostat
    		Inhibitor 99.93%
    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.
  • HY-13470
    GSK126
    		Inhibitor 99.98%
    GSK126 (GSK2816126A) is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC50 of 9.9 nM.
  • HY-13500
    GSK343
    		Inhibitor 99.85%
    GSK343, a chemical probe, is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.
  • HY-10442
    3-Deazaneplanocin A
    		Inhibitor 99.97%
    3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity.
  • HY-12186
    3-Deazaneplanocin A hydrochloride
    		Inhibitor 99.98%
    3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A hydrochloride also has anti-orthopoxvirus and anti-variola activities.
  • HY-15646
    UNC1999
    		Inhibitor 99.87%
    UNC1999, a chemical probe, is a SAM-competitive, potent and selective inhibitor of EZH2/1 with IC50s of <10 nM and 45 nM, repectively.
  • HY-133129
    MS1943
    		Inhibitor 98.92%
    MS1943 is an orally active selective HyT degrader of EZH2 that effectively reduces EZH2 levels in cells. MS1943 has anticancer activity and exhibits cytotoxic effects in a variety of TNBC cells while sparing normal cells. In addition, MS1943 maintains high potency (IC50=120 nM) in inhibiting EZH2 methyltransferase activity and is highly selective for EZH2. (Structure Note: RED, EZH2 ligand (HY-148458); Blue, Hyt (HY-W001578)).
  • HY-148333
    MS177
    		Inhibitor 99.55%
    MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12 nM). MS177 effectively depletes both canonical EZH2-PRC2 and noncanonical EZH2-cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest.
  • HY-101512
    A-395
    		Inhibitor 99.12%
    A-395, a chemical probe, is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM.
  • HY-145602
    Tulmimetostat
    		Inhibitor 99.79%
    Tulmimetostat (CPI-0209) is an orally active EZH1/EZH2 inhibitor that targets and inhibits the EZH2 enzyme.Tulmimetostat has antitumor activity and is used in a variety of solid tumor studies.
  • HY-147525
    PROTAC EZH2 Degrader-1
    		Inhibitor 99.44%
    PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC50 of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes.
  • HY-162250
    MS8847
    		Inhibitor 99.78%
    MS8847 is a PROTAC degrader and antiproliferative agent targeting EZH2 (DC50=34.4 nM in EOL-1 MLL-rAML cells). MS8847 recruits the E3 ligase von Hippel-Lindau (VHL) to mediate the degradation of EZH2 via the ubiquitin-proteasome system. MS8847 induces antiproliferative effects in MLL-rearranged acute myeloid leukemia cells and inhibits the growth of triple-negative breast cancer cell lines or 3D triple-negative breast cancer models. MS8847 is applicable to research related to MLL-rearranged acute myeloid leukemia and triple-negative breast cancer.
  • HY-103682
    PF-06726304
    		Inhibitor 99.71%
    PF-06726304 is a potent and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 displays robust antitumor growth activity.
  • HY-N5024
    Gambogenic acid
    		Inhibitor 99.91%
    Gambogenic acid is an active ingredient that can be isolated from gamboge. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination. Gambogenic acid can be used for the research of cancer.
  • HY-16986
    EPZ011989
    		Inhibitor 98.79%
    EPZ011989 is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ011989 shows robust methyl mark inhibition and anti-tumor activity. EPZ011989 can be used for the research of various cancers. EPZ011989 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-15555
    EPZ005687
    		Inhibitor 99.46%
    EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, and has 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
  • HY-100846
    JQEZ5
    		Inhibitor 98.14%
    JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitively inhibits polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM. JQEZ5 has anti-tumor effects.
  • HY-12856
    GSK503
    		Inhibitor 99.52%
    GSK503 is a potent and specific inhibitor of EZH2 methyltransferase with Kiapp values of 3 to 27 nM.
  • HY-15573
    EI1
    		Inhibitor 98.84%
    EI1 (KB-145943) is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
  • HY-162384
    EPIC-0628
    		Inhibitor 98.93%
    EPIC-0628 is an inhibitor of the HOTAIR-EZH2 interaction and promotes ATF3 expression. The long noncoding RNA HOTAIR has been found to regulate glioblastoma (GBM) progression and mediate DNA damage repair (DDR) by interacting with the catalytic subunit EZH2 of PRC2. EPIC-0628 also inhibits the ATF3-p38-E2F1 DDR pathway to inhibit the HR pathway and upregulates CDKN1A (p21) expression, causing cell cycle arrest. EPIC-0628 also synergizes with Temozolomide (TMZ) (HY-17364) to enhance its in vivo potency.