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Histone Methyltransferase

Histone methyltransferases (HMT) are histone-modifying enzymes , that catalyze the transfer of one, two, or three methyl groups to lysine and arginine residues of histone proteins. The attachment of methyl groups occurs predominantly at specific lysine or arginine residues on histones H3 and H4.

  • VTP50469
    T133362169916-18-9
    VTP50469 is a highly selective and orally active inhibitor of Menin-MLL interaction( Ki: 104 pM) and has potently anti-leukemia activity.
    • $177
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  • PF-06821497
    T124301844849-10-0
    PF-06821497 is a selective inhibitor of EZH2 with significant tumor growth inhibition.
    • $97
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    TargetMol | Inhibitor Hot
  • MM-102
    T63331417329-24-8
    MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.
    • $33
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    TargetMol | Inhibitor Hot
    TargetMol | Citations Cited
  • SNDX-5613
    T129432169919-21-3
    SNDX-5613 is a potent and specific inhibitor of Menin-MLL(Ki of 0.149 nM and a cell based IC50 of 10-20 nM). SNDX-5613 can be used for the research of MLL-rearranged (MLL-r) acute leukemias.
    • $67
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    TargetMol | Inhibitor Hot
  • MAK-683 hydrochloride
    T96812170606-94-5In house
    MAK683 hydrochloride is an inhibitor of embryonic ectoderm development (EED). MAK683 exhibits IC50s of 59, 26, 89 nM in EED Alphascreen binding, ELISA and LC-MS assay.
    • $195
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    TargetMol | Inhibitor Hot
  • Tazemetostat
    T17881403254-99-8
    Tazemetostat (EPZ6438) is a histone methyltransferase EZH2 inhibitor (IC50=11 nM) that is orally active, selective, and SAM-competitive. Tazemetostat exhibits antitumor activity and may be used for the treatment of epithelioid sarcoma/follicular lymphoma.
    • $59
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  • MRTX-1719
    T402542630904-45-7
    MRTX-1719 is a potent, first-in-class, selective inhibitor of the PRMT5/MTA complex, with an IC50 of less than 10 nM in PRMT5/MTA MTAP DEL SDMA cells.
    • $913
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    TargetMol | Inhibitor Hot
  • SETDB1-TTD-IN-1
    T97422755823-12-0In house
    SETDB1-TTD-IN-1 is a potent, selective and endogenous binder competitive inhibitor of SETDB1-TTD with a Kd of 88 nM.
    • $269
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    TargetMol | Inhibitor Hot
    TargetMol | Citations Cited
  • EZM 2302
    T56051628830-21-6
    EZM 2302 (GSK3359088) is a selective, and orally available arginine methyltransferase CARM1 inhibitor (IC50: 6 nM).
    • $68
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    TargetMol | Inhibitor Hot
  • Valemetostat
    T13279L1809336-39-7
    Valemetostat (DS-3201) is a first-in-class EZH1/2 dual inhibitor.
    • $96
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    TargetMol | Inhibitor Hot
  • (Iso)-MS4322
    T402332601727-80-2In house
    (Iso)-MS4322 ((Iso)-YS43-22) is a selective and potent protein arginine methyltransferase 5 (PRMT5) degrader with potential anticancer activity that effectively reduces PRMT5 protein levels in MCF-7 cells and inhibits the growth of a wide range of cancer cells.
    • $489 TargetMol
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  • EPZ015666
    T60761616391-65-1
    EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 enzymatic activity.
    • $42
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  • EPZ032597
    T700871887193-58-9In house
    EPZ032597 is a novel selective inhibitor of SMYD2 with an IC50 of 16 nM. EPZ032597 has anticancer activity and can be used to prevent and treat pancreatic cancer.
    • $350
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  • CPUY074020
    T10882902279-44-1In house
    CPUY074020 is a potent and orally bioavailable inhibitor of histone methyltransferase G9a (IC50: 2.18 μM) with anti-proliferative activity.
    • $117
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  • (S)-HH2853
    T731152202678-05-3In house
    (S)-HH2853 is a potent dual inhibitor of EZH1 and EZH2, inhibiting EZH2_Y641F with an IC50 of <100 nM.(S)-HH2853 has potential antitumor activity and can be used in the study of autoimmune diseases.
    • $333 TargetMol
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  • (R)-HH2853
    T731162202678-06-4In house
    (R)-HH2853 is a potent EZH2 inhibitor with an IC50 <100 nM for EZH2-Y641F.(R)-HH2853 has anticancer and antitumor activity and can be used in autoimmune diseases.
    • $333 TargetMol
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  • MS0124
    T281121197196-63-6In house
    MS0124 is a potent and selective G9A-like protein (GLP) inhibitor with IC50 values of 13±4 nM and 440±63 nM, respectively.
    • $329
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  • LEM-14-1189
    T729792987501-17-5In house
    Lem-14-1189, a LEM-14 derivative, is a potent NSD inhibitor of the nuclear receptor binding SET domain, and has inhibitory effects on NSD1, NSD2, and NSD3, with IC50 of 418 μM, 111 μM, and 60 μM, respectively. LEM-14-1189 has potential anticancer activity and can be used to study multiple myeloma (MM) and diseases of the blood system.
    • $350
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  • WDR5-47
    T676971422389-91-0
    WDR5-47 is a potent small molecule to disturb the interaction of MLL1-WDR5 with IC50 value of 0.3μM.
    • $195
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  • MS8511 HCl
    T63351L In house
    MS8511 HCl is a selective and potent covalent inhibitor of G9a/GLP that acts by targeting cysteine residues in the substrate binding site. MS8511 has anticancer activity and antiproliferative activity and reduces intracellular H3K9me2 levels.MS8511 can be used to study a wide range of cancers including brain, breast, and ovarian cancers .
    • $195
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  • OTS186935 FA
    T12344L1 In house
    OTS186935 FA is a protein methyltransferase SUV39H2 inhibitor.OTS186935 FA inhibits tumor growth in MDA-MB-231 breast cancer cells and A549 lung cancer cells.
    • $98
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  • UNC3866 TFA(1872382-47-2 free base)
    T4021L1872382-48-3
    UNC3866 TFA is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen.
    • $53
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  • CM-579
    T10840L1846570-40-8In house
    CM-579 is a dual inhibitor of G9a and DNMT( IC50:16 nM, 32 nM for G9a and DNMT). It has potent in vitro cellular activity in a wide range of cancer cells.
    • $50
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  • PRMT6-IN-3
    T731852890765-10-1
    PRMT6-IN-3 is a selective PRMT6 inhibitor with an IC50 value of 192 nM.PRMT6-IN-3 has anticancer activity and induces apoptosis in cancer cells.
    • $83
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  • ZLD1039
    T292311826865-46-6In house
    ZLD1039 is a potent, orally bioavailable EZH2 (Enhancer of Zeste Homolog 2) inhibitor with high selectivity. It demonstrates strong, concentration-dependent inhibition of both wild-type and mutant (Y641F and A677G) PRC2 (Polycomb Repressive Complex 2) enzymatic activities, exhibiting IC50 values of 5.6, 15, and 4.0 nM, respectively. Additionally, ZLD1039 effectively suppresses breast tumor growth and metastasis.
    • $30
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  • Sinefungin
    T1688658944-73-3In house
    Sinefungin (Adenosyl-Ornithine) is an effective inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication. Sinefungin is a SET7/9 inhibitor and ameliorates renal fibrosis by inhibiting H3K4 methylation.
    • $129
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  • MAK683
    T152011951408-58-4In house
    MAK683 is an inhibitor of embryonic ectoderm development (EED) (IC50s: 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay).
    • $48
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  • CPI-360
    T68101802175-06-9In house
    CPI-360 is a small molecule EZH2 inhibitor (IC50: 0.002 μM, EC50: 0.080 μM) that shows antitumor activity in an EZH200-dependent tumor xenograft model.
    • $76
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  • CMP-5
    T10850880813-42-3In house
    CMP-5 is a PRMT5 inhibitor with antiviral activity, inhibits PRMT5 methyltransferase activity, and can be used in the study of SARS virus infection.
    • $39
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  • DW14800
    T111312243709-60-4In house
    DW14800 is an inhibitor of PRMT5 (IC50 = 17 nM), enhances the transcription of HNF4α, and reduces the level of H4R3me2s.
    • $89
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  • GSK3368715
    T115001629013-22-4In house
    GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity.
    • $2,720
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  • GSK3326595
    T57451616392-22-3In house
    GSK3326595 (EPZ015938) is an inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50:6.2 nM.).
    • $39
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  • Tazemetostat hydrobromide
    T170021467052-75-0In house
    Tazemetostat hydrobromide (E-7438 hydrobromide) is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 (Ki: 2.5 nM). Tazemetostat hydrobromide also inhibits EZH1 (IC50: 392 nM).
    • $36
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  • A-366
    T36241527503-11-2
    A-366 is a highly selective peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP, respectively.It is more than 1,000-fold selective for G9a and GLP over the other 21 methyltransferases. It is an inhibitor of the Spindlin1-H3K4me3 interaction with an IC50 of 182.6 nM.It exhibits high affinity for human H3R with a Ki value of 17 nM, and shows subtype selectivity between subgroups of the histaminergic and dopaminergic receptor families.
    • $30
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  • GSK591
    T68531616391-87-7
    GSK591 (GSK3203591), Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM).
    • $41
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  • UNC1999
    T30571431612-23-5
    UNC1999 is a orally bioavailable, effective and specific inhibitor of EZH2 (IC50=2 nM) and EZH1 (IC50=45).
    • $31
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  • Menin-MLL inhibitor MI-2
    T26491271738-62-5
    Menin-MLL inhibitor MI-2 (MI2) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.
    • $41
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  • BIX-01294 trihydrochloride
    T19591392399-03-9
    BIX-01294 trihydrochloride is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.
    • $37
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  • Pinometostat
    T30991380288-87-8
    Pinometostat (EPZ-5676) has been used in trials studying the treatment of Leukemia, Acute Leukemias, Acute Myeloid Leukemia, Myelodysplastic Syndrome, and Acute Lymphocytic Leukemia, among others.
    • $34
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  • Gambogenic acid
    T8201173932-75-7
    Gambogenic acid is a natural product,is an effective inhibitor of EZH2,with anticancer activity.
    • $94
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  • GSK343
    T60591346704-33-3
    GSK343, a specific and effective EZH2 inhibitor (IC50=4 nM), exhibits 60 fold specificity activity against EZH1, and >1000 fold specificity activity against other histone methyltransferases.
    • $54
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  • SGC0946
    T30821561178-17-3
    SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.
    • $41
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  • UNC0638
    T32571255580-76-7
    UNC0638 is an inhibitor of β-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.
    • $54
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  • EPZ004777
    T30811338466-77-5
    EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
    • $33
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  • OICR-9429
    T69161801787-56-3
    OICR-9429 is a potent antagonist of the interaction that WDR5 effect with peptide regions of MLL and Histone 3. It reduces the viability of acute myeloid leukemia cells in vitro.
    • $31
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  • AMI-1
    T235220324-87-2
    AMI-1 is an effective and selective Histone Methyltransferase (HMT) inhibitor (IC50: 3.0/8.8 μM, for yeast Hmt1p, and human PRMT1).
    • $43
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  • EPZ011989
    T24351598383-40-4
    EPZ011989 is a effective, specific orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 Y646 and EZH2 wt; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.
    • $35
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  • GSK126
    T20791346574-57-9
    GSK126 (GSK2816126A) is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 nM).
    • $37
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  • EPZ005687
    T19051396772-26-1
    EPZ005687 is a potent and selective inhibitor of EZH2.
    • $53
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  • AZ505 ditrifluoroacetate
    T104271035227-44-1
    AZ505 ditrifluoroacetate is an effective and selective SMYD2 inhibitor (IC50: 0.12 μM).
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