Histone Methyltransferase

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  1. GSK126

    Catalog No. A11757
    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. CPI-360

    Catalog No. A15908
    EZH1 inhibitor
    CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases. Learn More
  3. EPZ011989

    Catalog No. A15544
    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
  4. CPI-169

    Catalog No. A15920
    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
  5. GSK503

    Catalog No. A15549
    EZH2 Inhibitor
    GSK-503 is a potent EZH2 inhibitor with potential anticancer activity. Learn More
  6. UNC-1999

    Catalog No. A13166
    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
  7. DZNep

    Catalog No. A11377
    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
    • New


    Catalog No. A17065
    SMYD3 inhibitor
    BCI-121 is an SMYD3 inhibitor. It acts by impairing cancer cell growth. Learn More
  8. PF-06726304

    Catalog No. A16937
    EZH2 inhibitor
    PF-06726304 is a potent and SAM-competitive EZH2 (Enhancer of Zeste Homolog 2) lysine methyltransferase inhibitor. Learn More
  9. JNJ-64619178

    Catalog No. A16861
    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
  10. BAY-598

    Catalog No. A17012
    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
  11. Menin-MLL interaction inhibitor
    MI-2 (Menin-MLL inhibitor 2) specifically binds to Menin and inhibits Menin??s interaction with MLL fusion proteins in cells. It can effectively reverse MLL fusion protein?Cmediated leukemic transformation by downregulating the expression of target genes downstream of MLL fusion protein oncogenic activity. MI-2 is a new tool for better understanding MLL-mediated leukemogenesis and represents a new approach for studying the role of Menin as an oncogenic cofactor of MLL fusion proteins. Learn More
  12. LLY-507

    Catalog No. A15813
    SMYD2 inhibitor
    LLY-507 is a cell-active, small molecule inhibitor of SMYD2 with IC50 of= 15 nM. Learn More
  13. UNC0638

    Catalog No. A12947
    G9a/GLP HMTase inhibitor
    UNC0638 is an inhibitor of protein lysine methyltransferases G9a(IC50<15 nM) and GLP(IC50=19 nM) with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets. Learn More
  14. UNC0642

    Catalog No. A15487
    G9a/GLP inhibitor
    UNC0642 is a potent and selective G9a and GLP histone lysine methyltransferase inhibitor (IC50 < 2.5 nM). It reduces H3K9 dimethylation levels in MDA-MB-231 cells (IC50 = 110 nM). Displays modest brain penetration in vivo. Learn More
  15. WDR5-0103

    Catalog No. A15928
    WDR5 antagonist
    WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM), inhibiting the catalytic activity of the MLL core complex in vitro (IC50 = 39 M). Learn More
  16. A-366

    Catalog No. A15969
    G9a/GLP inhibitor
    A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 value of 3.3 nM. Learn More
  17. UNC3866

    Catalog No. A11599
    CBX4 /CBX7 chromodomains antagonist
    UNC3866 is a potent antagonist of CBX4 and CBX7 chromodomains with a Kd of ~100 nM for each, and is 6- to 18-fold selective as compared to seven other CBX and CDY chromodomains. Learn More
  18. UNC 2400

    Catalog No. A13282
    EZH1/EZH2 inhibitor
    UNC 2400, a close analogue of UNC1999, is a negative control of UNC1999 that inhibits EZH2 and EZH1. Learn More
  19. JQEZ5

    Catalog No. A16961
    EZH2 inhibitor
    JQEZ5 is a potent and selective SAM-competitive EZH2 lysine methyltransferase inhibitor with IC50 value of 11 nM. Learn More
  20. AZ505

    Catalog No. A13061
    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
  21. AZ505 ditrifluoroacetate

    Catalog No. A13169
    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
  22. CPI-1205

    Catalog No. A16357
    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
  23. EPZ031686

    Catalog No. A16375
    SMYD3/ MEKK2 inhibitor
    EPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ki=1.2 and 1.1 nM respectively. Learn More
  24. EI1

    Catalog No. A12711
    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
  25. MM-102

    Catalog No. A14315
    MLL1 inhibitor
    MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 uM. Learn More
  26. UNC0321

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

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

    Catalog No. A13114
    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
  29. UNC0631

    Catalog No. A13195
    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
  30. UNC0646

    Catalog No. A13194
    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
  31. 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
  32. EPZ-5676 (Pinometostat)

    Catalog No. A12735
    DOT1L Inhibitor‎
    EPZ-5676 is a small molecule inhibitor of histone methyltransferase with potential antineoplastic activity. Learn More
  33. BIX 01294

    Catalog No. A11763
    G9a/GLP HMT inhibitor
    BIX 01294 is a G9a-like protein and G9a histone lysine methyltransferase inhibitor. Learn More
  34. EPZ-6438 (Tazemetostat)

    Catalog No. A12712
    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
  35. EPZ004777

    Catalog No. A12983
    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
  36. UNC 0224

    Catalog No. A15388
    G9a inhibitor
    UNC0224 is a potent and selective G9a inhibitor with IC50 of 15 nM in in the G9a Thioglo assay. Learn More
  37. BRD4770

    Catalog No. A14401
    G9a inhibitor
    BRD4770 is a novel histone methyltransferase inhibitor. Learn More
  38. EZH2 inhibitor
    3-deazaneplanocin A, also known as DZNep, is a well-known histone methyltransferase inhibitor, which disrupts polycomb-repressive complex 2 (PRC2), and induces apoptosis, while inhibiting proliferation and metastasis, in cancer cells, including acute myeloid leukemia, breast cancer and glioblastoma. Learn More
  39. UNC0379

    Catalog No. A14320
    SETD8 HMTase inhibitor
    UNC0379 is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8. Its affinity to SETD8 was confirmed by ITC (isothermal titration calorimetry) and SPR (surface plasmon resonance) studies. Learn More
  40. PFI-2

    Catalog No. A14216
    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
  41. MI-3

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

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

    Catalog No. A12941
    DOT1L inhibitor
    SGC 0946 is a potent DOT1L methyltransferase inhibitor that blocks H3K79 methylation in A431 cells and MCF10A cells. Learn More
  44. EPZ005687

    Catalog No. A12439
    EZH2 inhibitor
    EPZ005687 is a potent inhibitor of EZH2 (K(i) of 24 nM) Learn More
  45. Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase in human erythrocytes, also used as an antimalarial and anti-inflammatory agent. Learn More

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