Histone Methyltransferase

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  1. EZH2 Inhibitor

    3 Deazaneplanocin A (DZNep) is a cyclopentenyl analog of 3-deazaadenosine, originally synthesized as an inhibitor of S-adenosyl-L-homocysteine hydrolase.
  2. 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.
  3. 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.
  4. G9a/GLP HMT inhibitor

    BIX 01294 is a G9a-like protein and G9a histone lysine methyltransferase inhibitor.
  5. G9a inhibitor

    CPUY074020 is a potent G9a inhibitor with an IC50 of 2.18 μM, and possesses anti-proliferative activity .
  6. CARM1 inhibitor

    SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 50 nM.
  7. EZH2 inhibitor

    EPZ005687 is a potent inhibitor of EZH2 (K(i) of 24 nM)
  8. Dot1L inhibitor

    Dot1L-IN-1 is a highly potent, selective and structurally novel Dot1L inhibitor with a Ki of 2 pM.
  9. 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.
  10. 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.
  11. DOT1L Inhibitor

    EPZ-5676 is a small molecule inhibitor of histone methyltransferase with potential antineoplastic activity.
  12. 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.
  13. 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.
  14. DOT1L inhibitor

    SGC 0946 is a potent DOT1L methyltransferase inhibitor that blocks H3K79 methylation in A431 cells and MCF10A cells.
  15. 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.
  16. 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.
  17. PRC2 antagonist

    A-395 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.
  18. 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).
  19. 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).
  20. 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.
  21. 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).
  22. 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).
  23. 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.
  24. G9a HMTase inhibitor

    UNC0321 is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date
  25. 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.
  26. EZH1/EZH2 inhibitor

    UNC 2400, a close analogue of UNC1999, is a negative control of UNC1999 that inhibits EZH2 and EZH1.
  27. G9a/GLP inhibitor

    UNC 0638 is a selective inhibitor of G9a and GLP histone lysine methyltransferases.
  28. 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.
  29. 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.
  30. menin-MLL interaction inhibitor

    MI-3 is a potent menin-MLL interaction inhibitor with IC50 of 648 nM.
  31. MLL1 inhibitor

    MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 uM.
  32. 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.
  33. G9a inhibitor

    BRD4770 is a novel histone methyltransferase inhibitor.
  34. G9a inhibitor

    UNC0224 is a potent and selective G9a inhibitor with IC50 of 15 nM in in the G9a Thioglo assay.
  35. 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.
  36. 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.
  37. EZH2 Inhibitor

    GSK-503 is a potent EZH2 inhibitor with potential anticancer activity.
  38. SMYD2 inhibitor

    LLY-507 is a cell-active, small molecule inhibitor of SMYD2 with IC50 of= 15 nM.
  39. 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.
  40. 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.
  41. 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).
  42. G9a/GLP inhibitor

    A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 value of 3.3 nM.
  43. EZH2 inhibitor

    Lirametostat (CPI-1205) is a highly potent (biochemical IC50 = 0.002 μM, cellular EC50 = 0.032 μM) and selective inhibitor of EZH2.

  44. SMYD3/ MEKK2 inhibitor

    EPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ki=1.2 and 1.1 nM respectively.
  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.
  46. 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 .
  47. 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.
  48. EED PPI inhibitor

    MAK-683 is a potent inhibitor of embryonic ectoderm development protein (EED) and allosteric inhibitor of polycomb repressive complex 2 (PRC2), with potential antineoplastic activity.
  49. EZH2 inhibitor

    PF-06726304 is a potent and SAM-competitive EZH2 (Enhancer of Zeste Homolog 2) lysine methyltransferase inhibitor.
  50. EZH2 inhibitor

    JQEZ5 is a potent and selective SAM-competitive EZH2 lysine methyltransferase inhibitor with IC50 value of 11 nM.

Items 1-50 of 85

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