Histone Methyltransferase

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  1. GSK126

    Catalog No. A11757
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    EZH2 inhibitor
    GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity, decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. Learn More
  2. OICR-9429

    Catalog No. A16641
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    Wdr5-MLL interaction antagonist
    OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction with IC50 of 5 uM. inhibit proliferation and induce differentiation . Learn More
  3. Entacapone

    Catalog No. A10355
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    COMT inhibitor
    Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment. Learn More
  4. SMYD3-IN-1

    Catalog No. A18572
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    SMYD3 inhibitor
    SMYD3-IN-1 (compound 29) is an irreversible and selective inhibitor of SMYD3 (SET and MYND domain containing 3), with an IC50 of 11.7 nM. Learn More
  5. CM-579

    Catalog No. A18692
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    G9a/DNMT inhibitor
    CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells. Learn More
  6. PF-06821497

    Catalog No. A21388
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    EZH2 inhibitor
    PF-06821497 (compound 23a) is a potent, selective and orally active Enhancer of Zeste Homolog 2 (EZH2) inhibitor, with a Ki value <0.1 nM against mutant Y641N EZH2. Exhibits robust tumor growth inhibition. Learn More
  7. CM-272

    Catalog No. A17173
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    G9a/DNMT inhibitor
    CM-272 is a reversible dual small molecule inhibitor against G9a and DNMTs in hematological malignancies. CAS: 1846570-31-7 (free base) 1846570-32-8 (TFA) Learn More
  8. EPZ011989

    Catalog No. A15544
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    EZH2 Inhibitor
    EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase. Learn More
  9. GSK503

    Catalog No. A15549
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    EZH2 Inhibitor
    GSK-503 is a potent EZH2 inhibitor with potential anticancer activity. Learn More
  10. Flopropione

    Catalog No. A16550
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    5-HT1A receptor antagonist/COMT inhibitor
    Flopropione is a 5-HT1A receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor. Learn More
  11. CPI-360

    Catalog No. A15908
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    EZH2 inhibitor
    CPI-360 is a selective EZH2 inhibitor with IC50 values of 0.5 and 2.5 nM for wild-type EZH2 and Y641N mutant EZH2, respectively. Learn More
  12. CPI-169

    Catalog No. A15920
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    EZH2 inhibitor
    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. Learn More
  13. CPUY074020

    Catalog No. A12190
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    G9a inhibitor
    CPUY074020 is a potent G9a inhibitor with an IC50 of 2.18 μM, and possesses anti-proliferative activity . Learn More
  14. OICR-0547

    Catalog No. A20877
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    Wdr5-MLL interaction antagonist
    OICR-0547 is a closely related derivative of OICR-9429. OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction, while OICR-0547 cannot bind to WDR5. Learn More
  15. Tolcapone

    Catalog No. A20966
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    COMT inhibitor
    Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor. Learn More
  16. MM-102 TFA

    Catalog No. A21941
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    WDR5/MLL interaction inhibitor
    MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide. Learn More
  17. MM-589 TFA

    Catalog No. A21892
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    WDR5 and MLL protein-protein interaction inhibitor
    MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. Learn More
  18. DZNep

    Catalog No. A11377
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    EZH2 Inhibitor
    3 Deazaneplanocin A (DZNep) is a cyclopentenyl analog of 3-deazaadenosine, originally synthesized as an inhibitor of S-adenosyl-L-homocysteine hydrolase. Learn More
  19. Entacapone sodium salt

    Catalog No. A21888
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    COMT inhibitor
    Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment. Learn More
  20. GSK2807 Trifluoroacetate

    Catalog No. A21731
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    SMYD3 inhibitor
    GSK2807 Trifluoroacetate is a potent, selective and SAM-competitive inhibitor of SMYD3, with a Ki of 14 nM and an IC50 of 130 nM. Learn More
  21. Tazemetostat hydrobromide

    Catalog No. A21759
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    EZH2 inhibitor
    Tazemetostat hydrobromide (EPZ-6438 hydrobromide) is a potent, selective and orally available EZH2 inhibitor. Learn More
  22. UNC-1999

    Catalog No. A13166
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    EZH2/EZH1 Inhibitor
    UNC1999 is the first orally bioavailable inhibitor that has high in vitro potency for wildtype and mutant EZH2 as well as EZH1. Learn More
  23. AZ505

    Catalog No. A13061
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    SMYD2 inhibitor
    AZ505 is a potent and highly selective inhibitor of the oncogenic protein SMYD2(IC50=0.12 μM) with potential anticancer activity, >600 fold than SMYD3(IC50>83.3 μM); DOT1L(IC50>83.3 μM);EZH2(IC50>83.3 μM). Learn More
  24. AZ505 ditrifluoroacetate

    Catalog No. A13169
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    SMYD2 inhibitor
    AZ505 ditrifluoroacetate is a potent and highly selective inhibitor of the oncogenic protein SMYD2(IC50=0.12 uM) with potential anticancer activity, >600 fold than SMYD3(IC50>83.3 uM); DOT1L(IC50>83.3 uM);EZH2(IC50>83.3 uM). Learn More
  25. CPI-1205

    Catalog No. A16357
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    EZH2 inhibitor
    CPI-1205 is a highly potent (biochemical IC50 = 0.002 μM, cellular EC50 = 0.032 μM) and selective inhibitor of EZH2. Learn More
  26. MI-503

    Catalog No. A20975
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    menin-mLL interaction inhibitor
    MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction. Learn More
    • New

    BCI-121

    Catalog No. A17065
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    SMYD3 inhibitor
    BCI-121 is an SMYD3 inhibitor. It acts by impairing cancer cell growth. Learn More
  27. EPZ031686

    Catalog No. A16375
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    SMYD3/ MEKK2 inhibitor
    EPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ki=1.2 and 1.1 nM respectively. Learn More
  28. BIX-01338 hydrate

    Catalog No. A21812
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    histone lysine methyltransferase inhibitor
    BIX-01338 hydrate is a histone lysine methyltransferase inhibitor. Learn More
  29. JQEZ5

    Catalog No. A16961
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    EZH2 inhibitor
    JQEZ5 is a potent and selective SAM-competitive EZH2 lysine methyltransferase inhibitor with IC50 value of 11 nM. Learn More
  30. PF-06726304

    Catalog No. A16937
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    EZH2 inhibitor
    PF-06726304 is a potent and SAM-competitive EZH2 (Enhancer of Zeste Homolog 2) lysine methyltransferase inhibitor. Learn More
  31. GNA002

    Catalog No. A13266
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    covalent EZH2 inhibitor
    GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. Learn More
  32. JNJ-64619178

    Catalog No. A16861
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    Histone Methyltransferase inhibitor
    JNJ-64619178 is a PRMT5 inhibitor with high selectivity and potency (subnanomolar range, PRMT5-MEP-50 IC50=0.14 nM) under different in vitro and cellular conditions, paired with favorable pharmacokinetics and safety properties. Learn More
  33. BAY-598

    Catalog No. A17012
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    SMYD2 inhibitor
    BAY-598 is a potent, peptide-competitive chemical probe for SMYD2. CAS: 1906919-67-2 (S-isomer) 1906920-28-2 (BAY598 R-isomer) 1906920-07-7 (BAY598 recamic mixture) Learn More
  34. EI1

    Catalog No. A12711
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    EZH2 inhibitor
    EI1 is a potent and selective small molecule inhibitor of EZH2 with IC50 values of 15 nM and 13 nM for wild type EZH2 and EZH2 Y641F mutant, respectively. Learn More
  35. UNC 2400

    Catalog No. A13282
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    EZH1/EZH2 inhibitor
    UNC 2400, a close analogue of UNC1999, is a negative control of UNC1999 that inhibits EZH2 and EZH1. Learn More
  36. MI-3

    Catalog No. A14218
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    menin-MLL interaction inhibitor
    MI-3 is a potent menin-MLL interaction inhibitor with IC50 of 648 nM. Learn More
  37. UNC 0638

    Catalog No. A13690
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    G9a/GLP inhibitor
    UNC 0638 is a selective inhibitor of G9a and GLP histone lysine methyltransferases. Learn More
  38. SGC 0946

    Catalog No. A12941
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    DOT1L inhibitor
    SGC 0946 is a potent DOT1L methyltransferase inhibitor that blocks H3K79 methylation in A431 cells and MCF10A cells. Learn More
  39. EPZ004777

    Catalog No. A12983
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    DOT1L inhibitor
    EPZ004777 is a potent, selective inhibitor of DOT1L. EPZ004777 selectively inhibits cellular H3K79 methylation and inhibits expression of key MLL fusion target genes. Learn More
  40. EPZ-6438 (Tazemetostat)

    Catalog No. A12712
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    EZH2 inhibitor
    EPZ-6438 is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. It induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells. Learn More
  41. UNC0321

    Catalog No. A13200
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    G9a HMTase inhibitor
    UNC0321 is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date Learn More
  42. Opicapone (BIA 9-1067)

    Catalog No. A13110
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    COMT inhibitor
    opicapone is a novel catechol-O-methyltransferase inhibitor Learn More
  43. GSK343

    Catalog No. A13114
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    EZH2 inhibitor
    GSK343 is a potent histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor (IC= 4 nM). Diplays 1000-fold selectivity for other HMTs except EZH1 (60-fold selectivity). GSK343 inhibits H3K27 methylation in HCC1806 cells with an IC of <200nM (measured by immunofluorescence). Learn More
  44. UNC0631

    Catalog No. A13195
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    G9a inhibitor
    UNC-0631 is a novel G9a inhibitor with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity. Learn More
  45. UNC0646

    Catalog No. A13194
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    G9a/GLP HMTase inhibitor
    UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases, G9a and GLP (IC50 values are 6 nM and 15 nM for G9a and GLP, respectively). Learn More
  46. Chaetocin

    Catalog No. A12812
    SUV39H HMT Inhibitor
    Chaetocin is a histone methyltransferase SUV39H1 inhibitor (IC50 = 0.8 μM). Induces apoptosis in myeloma cell lines in vitro; exhibits antiproliferative activity in a mouse myeloma model in vivo. Learn More
  47. EPZ-5676 (Pinometostat)

    Catalog No. A12735
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    DOT1L Inhibitor‎
    EPZ-5676 is a small molecule inhibitor of histone methyltransferase with potential antineoplastic activity. Learn More
  48. PFI-2

    Catalog No. A14216
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    SETD7 inhibitor
    PFI-2 is a potent, selective, and cell-active lysine methyltransferase SETD7 inhibitor with Ki (app) and IC50 of 0.33 nM and 2 nM, 1000-fold selectivity over other methyltransferases and other non-epigenetic targets. Learn More
  49. MM-102

    Catalog No. A14315
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    MLL1 inhibitor
    MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 uM. Learn More

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