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

EZH2 Inhibitor

EZH2 Inhibitors (38):

Cat. No. Product Name Effect Purity
  • 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-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-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-13500
    GSK343
    		Inhibitor 99.88%
    GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.
  • HY-15646
    UNC1999
    		Inhibitor 99.83%
    UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH2/1 with IC50s of <10 nM and 45 nM, repectively.
  • HY-162384
    EPIC-0628
    		Inhibitor
    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 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.
  • HY-148333
    MS177
    		Inhibitor 98.00%
    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-133129
    MS1943
    		Inhibitor 98.02%
    MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines. MS1943 effectively blocks proliferation of multiple TNBC and other cancer cell lines.
  • 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-147525
    PROTAC EZH2 Degrader-1
    		Inhibitor 98.55%
    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-12856
    GSK503
    		Inhibitor 99.52%
    GSK503 is a potent and specific inhibitor of EZH2 methyltransferase with Kiapp values of 3 to 27 nM.
  • HY-100846
    JQEZ5
    		Inhibitor 98.08%
    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-15555
    EPZ005687
    		Inhibitor 99.79%
    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-N5024
    Gambogenic acid
    		Inhibitor 99.94%
    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-103682
    PF-06726304
    		Inhibitor 98.37%
    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-15573
    EI1
    		Inhibitor 99.78%
    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-101508
    GNA002
    		Inhibitor 98.02%
    GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes.
  • HY-A0298
    EZH2-IN-2
    		Inhibitor 99.40%
    EZH2-IN-2 is a EZH2 inhibitor extracted from patent WO2018133795A1, Compound Example 69, with an IC50 of 64 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity.
  • HY-136188
    UNC2399
    		Inhibitor 99.62%
    UNC2399, a biotinylated UNC1999, is a selective EZH2 inhibitor, maintaining high in vitro potency for EZH2, with an IC50 of 17 nM.
  • HY-119198
    NSC745885
    		Inhibitor ≥98.0%
    NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers.