1. Signaling Pathways
  2. Epigenetics
  3. Histone Methyltransferase
  4. EZH2 Isoform

EZH2

 

EZH2 Related Products (35):

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-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-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-156292
    IHMT-EZH2-426
    Inhibitor
    IHMT-EZH2-426 (compound 38) is a potent and covalent EZH2 degrader with IC50s of 1.3 nM, 1.2 nM, and 1.7-3.5 nM against EZH2 wild-type, EZH2-A687V, and EZH2-Y641F/Y641N/Y641S, respectively. IHMT-EZH2-426 exhibits potent antiproliferation effects against both B-cell lymphoma and triple negative breast cancer (TNBC) cell lines by reducing the levels of H3K27me3 and EZH2.
  • HY-161083
    PARP/EZH2-IN-2
    Inhibitor
    PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC50 values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy.
  • 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 99.00%
    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 98.05%
    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-147090
    Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH
    Degrader 98.24%
    Tazemetostat de(methylene morpholine)-O-C3-O-C-COOH (Compound 21b) is an EZH2 degrader and can be used for the research of lymphoma.
  • 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.
  • 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.
Cat. No. Product Name / Synonyms Application Reactivity