Histone Methyltransferase

Choose Selective Histone Methyltransferase Inhibitors

Histone Methyltransferase Signaling Pathway Map

Histone Methyltransferase Signaling Pathways

Histone Methyltransferase Products

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  • Histone Methyltransferase Inhibitors (55)
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  • Histone Methyltransferase Antagonists (3)
  • New Histone Methyltransferase Products
Catalog No. Product Name Information Product Use Citations Product Validations
S3147 Entacapone Entacapone (OR-611) inhibits catechol-O-methyltransferase(COMT) with IC50 of 151 nM. Entacapone can be used for the research of Parkinson's disease. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.
bioRxiv, 2021, 10.1101/2021.03.22.436393
S4021 Tolcapone Tolcapone (Ro 40-7592) is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM.
Viruses, 2021, 13(8)1533
S4589 Amodiaquine dihydrochloride dihydrate Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase with estimated Ki of 18.6 nM. It is also used as an antimalarial and anti-inflammatory agent.
Nat Biomed Eng, 2021, 10.1038/s41551-021-00718-9
J Med Chem, 2020, 31
bioRxiv, 2020, 10.1101/2020.04.13.039917
S5445 AMI-1 (free acid) AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.
S7004 EPZ005687 EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM in a cell-free assay, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
Cancer Cell, 2021, 39(3):407-422.e13
Cancer Biol Ther, 2021, 22(4):333-344
Nat Commun, 2020, 11(1):604
S7020 UNC0646 UNC0646 is a selective histone lysine methyltransferase (HMTase) inhibitor for G9a and GLP with IC50 of 6 nM and 15 nM , respectively, with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity.
S7061 GSK126 GSK126 (GSK2816126A, GSK2816126) is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases.
Nat Commun, 2022, 13(1):12
Cell, 2021, 184(25):6119-6137.e26
Sci Adv, 2021, 7(15)eabe2261
S7062 Pinometostat (EPZ5676) Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM in a cell-free assay, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor. Phase 1.
Nat Biotechnol, 2021, 10.1038/s41587-021-00837-3
Proc Natl Acad Sci U S A, 2021, 118(29)e2104013118
EMBO Rep, 2021, 22(2):e51184
S7079 SGC 0946 SGC 0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM in a cell-free assay, is inactive against a panel of 12 PMTs and DNMT1.
Transpl Int, 2020, 33(2):229-243
Cancer Cell, 2019, 36(2):179-193
Cell, 2019, 36(2):179-193
S7120 3-deazaneplanocin A (DZNeP) HCl 3-deazaneplanocin A HCl (DZNeP, NSC 617989), an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM in a cell-free assay.
Nat Cell Biol, 2021, 23(4):341-354
Theranostics, 2021, 11(1):361-378
J Pathol, 2021, 10.1002/path.5657
S7128 Tazemetostat (EPZ-6438) Tazemetostat (EPZ-6438, E7438) is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.
Nat Commun, 2022, 13(1):12
Cell, 2021, 184(25):6119-6137.e26
Nat Cell Biol, 2021, 23(4):341-354
S7164 GSK343 GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases. GSK343 induces autophagy.
J Immunol, 2022, 208(2):347-357
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
S7165 UNC1999 UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets. UNC1999 is a potent autophagy inducer. UNC1999 specifically suppresses H3K27me3/2 and induces a range of anti-leukemia effects including anti-proliferation, differentiation, and apoptosis.
J Immunol, 2022, 208(2):347-357
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
S7230 UNC0642 UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels.
Blood, 2021, blood.2020009195
Blood, 2021, 138(9):790-805
Cell Death Dis, 2021, 12(6):570
S7265 MM-102 MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM in a cell-free assay.
J Cell Mol Med, 2020, 10.1111/jcmm.16030
Mol Carcinog, 2020, 10.1002/mc.23147
Front Genet, 2020, 11:80
S7294 PFI-2 HCl 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.
Brain Behav Immun, 2019, 82:382-395
Cancer Res, 2018, 78(20):5731-5740
Cell Death Dis, 2018,
S7353 EPZ004777 EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM in a cell-free assay and demonstrates >1,200-fold selectivity for DOT1L over all other tested PMTs. EPZ004777 induces apoptosis.
Proc Natl Acad Sci U S A, 2021, 118(29)e2104013118
Nat Chem Biol, 2020, 10.1038/s41589-020-0618-6
Cancer Cell, 2019, 35(5):752-766
S7570 UNC0379 UNC0379 is a selective, substrate competitive inhibitor of N-lysine methyltransferase SETD8 with IC50 of 7.9 μM, high selectivity over 15 other methyltransferases.
Acta Biochim Biophys Sin (Shanghai), 2021, gmab140
J Biol Chem, 2020, 10.1074/jbc.RA119.010951
Biochim Biophys Acta Gene Regul Mech, 2019, 1862(2):173-183
S7572 A-366 A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 of 3.3nM, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases.
Nat Med, 2019, 25(7):1073-1081
Genome Res, 2019, 29(10):1659-1672
Cancer Res, 2018, 78(20):5731-5740
S7575 LLY-507 LLY-507 is a cell-active, potent, and selective inhibitor of protein-lysine Methyltransferase SMYD2.
Oncol Lett, 2020, 20(5):153
J Immunother Cancer, 2019, 7(1):277
Biochem Biophys Res Commun, 2019, 513(2):340-346
S7591 BRD4770 BRD4770 is a histone methyltransferase G9a inhibitor with IC50 of 6.3 μM, and induces cell senescence.
Cancer Res, 2018, 78(20):5731-5740
Hum Pathol, 2018, 72:117-126
S7611 EI1 EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
Cancer Res, 2018, 78(20):5731-5740
Mol Cancer, 2017, 10.1186/s12943-016-0575-6
Virology, 2017, 506:34-44
S7616 CPI-169 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.
Cell Chem Biol, 2021, S2451-9456(21)00213-0
Cancer Sci, 2020, 112(1):133-143
J Clin Invest, 2020, 134217
S7618 MI-2 (Menin-MLL Inhibitor) MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.
J Immunol, 2021, ji1901348
Cell Rep, 2019, 26(2):415-428
Endocrinology, 2019, 10.1210/en.2019-00274
S7619 MI-3 (Menin-MLL Inhibitor) MI-3 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 648 nM.
Nature, 2021, 10.1038/s41586-021-04116-8
Clin Epigenetics, 2019, 11(1):137
Cancer Res, 2018, 78(20):5731-5740
S7656 CPI-360 CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.
Cancer Res, 2018, 78(20):5731-5740
S7748 EPZ015666 (GSK3235025) EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.
Sci Adv, 2021, 7(13)eabc1834
Front Immunol, 2021, 12:695947
Ann Transl Med, 2021, 9(9):755
S7804 GSK503 GSK503 is a potent and specific EZH2 methyltransferase inhibitor.
Cancer Cell, 2019, 36(4):385-401
Cancer Res, 2018, 78(20):5731-5740
J Pathol, 2018, 245(4):433-444
S7805 EPZ011989 EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM.
Mol Cancer Ther, 2021, 20(3):541-552
Cancer Lett, 2020, S0304-3835(20)30632-7
Cancer Cell, 2019, 36(4):385-401
S7815 MI-136 MI-136 can specifically inhibit the menin-MLL interaction. It inhibits DHT-induced expression of androgen receptor (AR) target genes.
J Med Chem, 2020, 31
S7816 MI-463 MI-463 is a potent inhibitor of Menin-MLL interaction with an IC50 value of 15.3 nM.
Front Oncol, 2020, 10:524922
S7817 MI-503 MI-503 is a potent and selective Menin-MLL inhibitor with IC50 of 14.7 nM. It shows pronounced growth suppressive activity in a panel of human MLL leukemia cell lines(GI50 at 250 nM-570 nM range), but only a minimal effect in human leukemia cell lines without MLL translocations.
J Assoc Res Otolaryngol, 2021, 10.1007/s10162-021-00801-7
Johannes Gutenberg-Universität Mainz, 2021, 10.25358/openscience-5949
Cancers (Basel), 2020, 12(9)E2715
S7820New EPZ020411 2HCl EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.
Theranostics, 2020, 10(1):133-150
S7832 SGC707 SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively.
J Med Chem, 2020, 31
Transpl Int, 2020, 33(2):229-243
J Immunother Cancer, 2019, 7(1):277
S7868 S-Adenosyl-L-homocysteine (SAH) S-Adenosyl-L-homocysteine (SAH, S-Adenosylhomocysteine, AdoHcy, Formycinylhomocysteine) is an inhibitor for (Methyltransferase Like 3-14) METTL3-METTL14 heterodimer complex (METTL3-14) with IC50 of 0.9 μM.
S7884 AMI-1 AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.
Oncogene, 2021, 10.1038/s41388-020-01617-0
Oncogene, 2021, 40(7):1375-1389
Research Square, 2021, 10.21203/rs.3.rs-620216/v1
S7983 A-196 A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 0.025 and 0.144 μM, respectively; more than 100-fold selective over other histone methyltransferases and non-epigenetic targets.
PLoS One, 2021, 16(6):e0252504
J Immunother Cancer, 2019, 7(1):277
Nucleic Acids Res, 2019, 47(21):10977-10993
S8006 BIX 01294 BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3.
Adv Sci (Weinh), 2021, e2100779
Exp Mol Med, 2021, 10.1038/s12276-021-00715-7
Cancer Gene Ther, 2021, 10.1038/s41417-021-00335-3
S8068 Chaetocin Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively. Chaetocin is an anticancer agent and inhibitor of thioredoxin reductase (TrxR).
Free Radic Biol Med, 2021, 178:147-160
Cancer Discov, 2021, candisc.0872.2020
Stem Cells Int, 2021, 2021:8888416
S8071 UNC0638 UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP histone methyltransferase with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets. UNC0638 has anti-viral activities.
Adv Sci (Weinh), 2021, e2100779
Sci Adv, 2021, 7(3)eaba8053
Oxid Med Cell Longev, 2021, 2021:6650781
S8111 GSK591 GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM.
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
Cancer Sci, 2021, 10.1111/cas.14988
S8112 MS023 MS023 is a potent, selective, and cell-active Type I PRMT inhibitor with IC50 of 30 nM, 119 nM, 83 nM, 4 nM, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, respectively.
Oncogene, 2021, 10.1038/s41388-020-01617-0
Oncogene, 2021, 40(7):1375-1389
Proteome Sci, 2020, 19;18:6
S8147 MS049 MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.
Research Square, 2021, 10.21203/rs.3.rs-620216/v1
EMBO Rep, 2020, 21(2):e48597
S8209 HLCL-61 HCL HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.
Nat Commun, 2018, 9(1):1572
Cancer Res, 2018, 78(20):5731-5740
S8340 SGC2085 SGC2085 is a potent and selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) inhibitor with an IC50 value of 50 nM and >100-fold selective over other PRMTs.
S8353 Lirametostat (CPI-1205) Lirametostat (CPI-1205) is an orally available selective inhibitor of the histone lysine methyltransferase EZH2 with IC50 values of 2 nM and 52 nM for EZH2 and EZH1 respectively. It has potential antineoplastic activity.
Nat Commun, 2021, 12(1):6276
J Immunother Cancer, 2021, 9(5)e001335
Cancer Discov, 2021, candisc.0913.2020
S8494 PF-06726304 PF-06726304 is a selective EZH2 inhibitor with Ki values of 0.7 nM and 3 nM for WT EZH2 and Y641N respectively; also inhibits H3K27me3 with the IC50 value of 15 nM.
Elife, 2021, 10e65654
S8607 JQ-EZ-05 (JQEZ5) JQ-EZ-05 (JQEZ5) is a specific and reversible EZH1/2 inhibitor.
Nat Chem Biol, 2019, 15(4):391-400
S8624 Onametostat (JNJ-64619178) Onametostat (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.
Proc Natl Acad Sci U S A, 2021, 118(34)e2024055118
S8664 Pemrametostat (GSK3326595) Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models.
Sci Adv, 2021, 7(13)eabc1834
Proc Natl Acad Sci U S A, 2021, 118(34)e2024055118
Cell Chem Biol, 2021, S2451-9456(21)00400-1
S8702 EBI-2511 EBI-2511 is a highly potent and orally active EZH2 inhibitor with an IC50 of 4 nM for EZH2(A667G).
S8918 MS1943 MS1943 is an orally bioavailable EZH2 selective degrader that effectively reduces EZH2 levels in cells with IC50 of 120 nM for inhibiting EZH2 methyltransferase activity.
S8934 VTP50469 VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL interaction with Ki of 104 pM. VTP50469 exhibits anti-leukemia activity.
S8983 MAK683 MAK683 (EED inhibitor-1, example 2) is an inhibitor of embryonic ectoderm development (EED). MAK683 exhibits IC50 of 59 nM, 89 nM and 26 nM in EED Alphascreen binding, LC-MS and ELISA assay, respectively.
S9659 UNC6852 UNC6852 is a selective degrader that targets polycomb repressive complex 2 (PRC2) with IC50 of 247 nM for EED. UNC6852 is based on PROTAC and contains an EED226-derived ligand and a ligand for VHL.
A5058 Brd4 Rabbit Recombinant mAb Brd4 Rabbit Recombinant mAb detects endogenous levels of total Brd4.
A5240 ASH2L Rabbit Recombinant mAb ASH2L Rabbit Recombinant mAb detects endogenous level of total ASH2L.
A5247 PRMT5 Rabbit Recombinant mAb PRMT5 Rabbit Recombinant mAb detects endogenous level of total PRMT5.
S2184 WDR5-0103 WDR5-0103 (WD-Repeat Protein 5-0103) is a small-molecule antagonist of WDR5 (WD40 repeat protein 5) with Kd of 450 nM.
S7833 OICR-9429 OICR-9429 is a potent antagonist of the interaction of WDR5 with peptide regions of MLL and Histone 3 and reduces viability of acute myeloid leukemia cells in vitro. It binds to WDR5 with high affinity (KD = 93 ± 28 nM.
iScience, 2022, 25(1):103679
Nature, 2021, 10.1038/s41586-021-04116-8
J Exp Clin Cancer Res, 2021, 40(1):203
S8359 UNC3866 UNC3866 is a potent antagonist of the methyllysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. UNC3866 binds the chromodomains of CBX4 and CBX7 most potently, with a K(d) of ∼100 nM for each, and is 6- to 18-fold selective as compared to seven other CBX and CDY chromodomains.
Leukemia, 2021, 10.1038/s41375-021-01121-8
Int J Mol Sci, 2021, 22(2)E619
Leukemia, 2021, 10.1038/s41375-021-01121-8
S8496 EED226 EED226 is a potent, selective, and orally bioavailable a novel allosteric Polycomb repressive complex 2 (PRC2) inhibitor with an IC50 of 23.4 nM when the H3K27me0 peptide was used as substrate and an IC50 of 53.5 nM when the mononucleosome was used as the substrate. It directly binds to the H3K27me3 binding pocket of EED.
Mol Cell, 2021, 81(10):2183-2200.e13
Nat Commun, 2021, 12(1):6985
Proc Natl Acad Sci U S A, 2021, 118(30)e2102718118
S3147 Entacapone Entacapone (OR-611) inhibits catechol-O-methyltransferase(COMT) with IC50 of 151 nM. Entacapone can be used for the research of Parkinson's disease. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.
bioRxiv, 2021, 10.1101/2021.03.22.436393
S4021 Tolcapone Tolcapone (Ro 40-7592) is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM.
Viruses, 2021, 13(8)1533
S4589 Amodiaquine dihydrochloride dihydrate Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase with estimated Ki of 18.6 nM. It is also used as an antimalarial and anti-inflammatory agent.
Nat Biomed Eng, 2021, 10.1038/s41551-021-00718-9
J Med Chem, 2020, 31
bioRxiv, 2020, 10.1101/2020.04.13.039917
S5445 AMI-1 (free acid) AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.
S7004 EPZ005687 EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM in a cell-free assay, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
Cancer Cell, 2021, 39(3):407-422.e13
Cancer Biol Ther, 2021, 22(4):333-344
Nat Commun, 2020, 11(1):604
S7020 UNC0646 UNC0646 is a selective histone lysine methyltransferase (HMTase) inhibitor for G9a and GLP with IC50 of 6 nM and 15 nM , respectively, with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity.
S7061 GSK126 GSK126 (GSK2816126A, GSK2816126) is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases.
Nat Commun, 2022, 13(1):12
Cell, 2021, 184(25):6119-6137.e26
Sci Adv, 2021, 7(15)eabe2261
S7062 Pinometostat (EPZ5676) Pinometostat (EPZ5676) is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM in a cell-free assay, demonstrating >37,000-fold selectivity against all other PMTs tested, inhibits H3K79 methylation in tumor. Phase 1.
Nat Biotechnol, 2021, 10.1038/s41587-021-00837-3
Proc Natl Acad Sci U S A, 2021, 118(29)e2104013118
EMBO Rep, 2021, 22(2):e51184
S7079 SGC 0946 SGC 0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM in a cell-free assay, is inactive against a panel of 12 PMTs and DNMT1.
Transpl Int, 2020, 33(2):229-243
Cancer Cell, 2019, 36(2):179-193
Cell, 2019, 36(2):179-193
S7120 3-deazaneplanocin A (DZNeP) HCl 3-deazaneplanocin A HCl (DZNeP, NSC 617989), an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM in a cell-free assay.
Nat Cell Biol, 2021, 23(4):341-354
Theranostics, 2021, 11(1):361-378
J Pathol, 2021, 10.1002/path.5657
S7128 Tazemetostat (EPZ-6438) Tazemetostat (EPZ-6438, E7438) is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.
Nat Commun, 2022, 13(1):12
Cell, 2021, 184(25):6119-6137.e26
Nat Cell Biol, 2021, 23(4):341-354
S7164 GSK343 GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases. GSK343 induces autophagy.
J Immunol, 2022, 208(2):347-357
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
S7165 UNC1999 UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets. UNC1999 is a potent autophagy inducer. UNC1999 specifically suppresses H3K27me3/2 and induces a range of anti-leukemia effects including anti-proliferation, differentiation, and apoptosis.
J Immunol, 2022, 208(2):347-357
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
S7230 UNC0642 UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels.
Blood, 2021, blood.2020009195
Blood, 2021, 138(9):790-805
Cell Death Dis, 2021, 12(6):570
S7265 MM-102 MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM in a cell-free assay.
J Cell Mol Med, 2020, 10.1111/jcmm.16030
Mol Carcinog, 2020, 10.1002/mc.23147
Front Genet, 2020, 11:80
S7294 PFI-2 HCl 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.
Brain Behav Immun, 2019, 82:382-395
Cancer Res, 2018, 78(20):5731-5740
Cell Death Dis, 2018,
S7353 EPZ004777 EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM in a cell-free assay and demonstrates >1,200-fold selectivity for DOT1L over all other tested PMTs. EPZ004777 induces apoptosis.
Proc Natl Acad Sci U S A, 2021, 118(29)e2104013118
Nat Chem Biol, 2020, 10.1038/s41589-020-0618-6
Cancer Cell, 2019, 35(5):752-766
S7570 UNC0379 UNC0379 is a selective, substrate competitive inhibitor of N-lysine methyltransferase SETD8 with IC50 of 7.9 μM, high selectivity over 15 other methyltransferases.
Acta Biochim Biophys Sin (Shanghai), 2021, gmab140
J Biol Chem, 2020, 10.1074/jbc.RA119.010951
Biochim Biophys Acta Gene Regul Mech, 2019, 1862(2):173-183
S7572 A-366 A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 of 3.3nM, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases.
Nat Med, 2019, 25(7):1073-1081
Genome Res, 2019, 29(10):1659-1672
Cancer Res, 2018, 78(20):5731-5740
S7575 LLY-507 LLY-507 is a cell-active, potent, and selective inhibitor of protein-lysine Methyltransferase SMYD2.
Oncol Lett, 2020, 20(5):153
J Immunother Cancer, 2019, 7(1):277
Biochem Biophys Res Commun, 2019, 513(2):340-346
S7591 BRD4770 BRD4770 is a histone methyltransferase G9a inhibitor with IC50 of 6.3 μM, and induces cell senescence.
Cancer Res, 2018, 78(20):5731-5740
Hum Pathol, 2018, 72:117-126
S7611 EI1 EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
Cancer Res, 2018, 78(20):5731-5740
Mol Cancer, 2017, 10.1186/s12943-016-0575-6
Virology, 2017, 506:34-44
S7616 CPI-169 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.
Cell Chem Biol, 2021, S2451-9456(21)00213-0
Cancer Sci, 2020, 112(1):133-143
J Clin Invest, 2020, 134217
S7618 MI-2 (Menin-MLL Inhibitor) MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.
J Immunol, 2021, ji1901348
Cell Rep, 2019, 26(2):415-428
Endocrinology, 2019, 10.1210/en.2019-00274
S7619 MI-3 (Menin-MLL Inhibitor) MI-3 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 648 nM.
Nature, 2021, 10.1038/s41586-021-04116-8
Clin Epigenetics, 2019, 11(1):137
Cancer Res, 2018, 78(20):5731-5740
S7656 CPI-360 CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.
Cancer Res, 2018, 78(20):5731-5740
S7748 EPZ015666 (GSK3235025) EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.
Sci Adv, 2021, 7(13)eabc1834
Front Immunol, 2021, 12:695947
Ann Transl Med, 2021, 9(9):755
S7804 GSK503 GSK503 is a potent and specific EZH2 methyltransferase inhibitor.
Cancer Cell, 2019, 36(4):385-401
Cancer Res, 2018, 78(20):5731-5740
J Pathol, 2018, 245(4):433-444
S7805 EPZ011989 EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM.
Mol Cancer Ther, 2021, 20(3):541-552
Cancer Lett, 2020, S0304-3835(20)30632-7
Cancer Cell, 2019, 36(4):385-401
S7815 MI-136 MI-136 can specifically inhibit the menin-MLL interaction. It inhibits DHT-induced expression of androgen receptor (AR) target genes.
J Med Chem, 2020, 31
S7816 MI-463 MI-463 is a potent inhibitor of Menin-MLL interaction with an IC50 value of 15.3 nM.
Front Oncol, 2020, 10:524922
S7817 MI-503 MI-503 is a potent and selective Menin-MLL inhibitor with IC50 of 14.7 nM. It shows pronounced growth suppressive activity in a panel of human MLL leukemia cell lines(GI50 at 250 nM-570 nM range), but only a minimal effect in human leukemia cell lines without MLL translocations.
J Assoc Res Otolaryngol, 2021, 10.1007/s10162-021-00801-7
Johannes Gutenberg-Universität Mainz, 2021, 10.25358/openscience-5949
Cancers (Basel), 2020, 12(9)E2715
S7820New EPZ020411 2HCl EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.
Theranostics, 2020, 10(1):133-150
S7832 SGC707 SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively.
J Med Chem, 2020, 31
Transpl Int, 2020, 33(2):229-243
J Immunother Cancer, 2019, 7(1):277
S7868 S-Adenosyl-L-homocysteine (SAH) S-Adenosyl-L-homocysteine (SAH, S-Adenosylhomocysteine, AdoHcy, Formycinylhomocysteine) is an inhibitor for (Methyltransferase Like 3-14) METTL3-METTL14 heterodimer complex (METTL3-14) with IC50 of 0.9 μM.
S7884 AMI-1 AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.
Oncogene, 2021, 10.1038/s41388-020-01617-0
Oncogene, 2021, 40(7):1375-1389
Research Square, 2021, 10.21203/rs.3.rs-620216/v1
S7983 A-196 A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 0.025 and 0.144 μM, respectively; more than 100-fold selective over other histone methyltransferases and non-epigenetic targets.
PLoS One, 2021, 16(6):e0252504
J Immunother Cancer, 2019, 7(1):277
Nucleic Acids Res, 2019, 47(21):10977-10993
S8006 BIX 01294 BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases. BIX01294 induces autophagy. BIX01294 also inhibits H3K36 methylation by oncoproteins NSD1, NSD2 and NSD3.
Adv Sci (Weinh), 2021, e2100779
Exp Mol Med, 2021, 10.1038/s12276-021-00715-7
Cancer Gene Ther, 2021, 10.1038/s41417-021-00335-3
S8068 Chaetocin Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively. Chaetocin is an anticancer agent and inhibitor of thioredoxin reductase (TrxR).
Free Radic Biol Med, 2021, 178:147-160
Cancer Discov, 2021, candisc.0872.2020
Stem Cells Int, 2021, 2021:8888416
S8071 UNC0638 UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP histone methyltransferase with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets. UNC0638 has anti-viral activities.
Adv Sci (Weinh), 2021, e2100779
Sci Adv, 2021, 7(3)eaba8053
Oxid Med Cell Longev, 2021, 2021:6650781
S8111 GSK591 GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM.
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
Cancer Sci, 2021, 10.1111/cas.14988
S8112 MS023 MS023 is a potent, selective, and cell-active Type I PRMT inhibitor with IC50 of 30 nM, 119 nM, 83 nM, 4 nM, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, respectively.
Oncogene, 2021, 10.1038/s41388-020-01617-0
Oncogene, 2021, 40(7):1375-1389
Proteome Sci, 2020, 19;18:6
S8147 MS049 MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.
Research Square, 2021, 10.21203/rs.3.rs-620216/v1
EMBO Rep, 2020, 21(2):e48597
S8209 HLCL-61 HCL HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.
Nat Commun, 2018, 9(1):1572
Cancer Res, 2018, 78(20):5731-5740
S8340 SGC2085 SGC2085 is a potent and selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) inhibitor with an IC50 value of 50 nM and >100-fold selective over other PRMTs.
S8353 Lirametostat (CPI-1205) Lirametostat (CPI-1205) is an orally available selective inhibitor of the histone lysine methyltransferase EZH2 with IC50 values of 2 nM and 52 nM for EZH2 and EZH1 respectively. It has potential antineoplastic activity.
Nat Commun, 2021, 12(1):6276
J Immunother Cancer, 2021, 9(5)e001335
Cancer Discov, 2021, candisc.0913.2020
S8494 PF-06726304 PF-06726304 is a selective EZH2 inhibitor with Ki values of 0.7 nM and 3 nM for WT EZH2 and Y641N respectively; also inhibits H3K27me3 with the IC50 value of 15 nM.
Elife, 2021, 10e65654
S8607 JQ-EZ-05 (JQEZ5) JQ-EZ-05 (JQEZ5) is a specific and reversible EZH1/2 inhibitor.
Nat Chem Biol, 2019, 15(4):391-400
S8624 Onametostat (JNJ-64619178) Onametostat (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.
Proc Natl Acad Sci U S A, 2021, 118(34)e2024055118
S8664 Pemrametostat (GSK3326595) Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models.
Sci Adv, 2021, 7(13)eabc1834
Proc Natl Acad Sci U S A, 2021, 118(34)e2024055118
Cell Chem Biol, 2021, S2451-9456(21)00400-1
S8702 EBI-2511 EBI-2511 is a highly potent and orally active EZH2 inhibitor with an IC50 of 4 nM for EZH2(A667G).
S8918 MS1943 MS1943 is an orally bioavailable EZH2 selective degrader that effectively reduces EZH2 levels in cells with IC50 of 120 nM for inhibiting EZH2 methyltransferase activity.
S8934 VTP50469 VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL interaction with Ki of 104 pM. VTP50469 exhibits anti-leukemia activity.
S8983 MAK683 MAK683 (EED inhibitor-1, example 2) is an inhibitor of embryonic ectoderm development (EED). MAK683 exhibits IC50 of 59 nM, 89 nM and 26 nM in EED Alphascreen binding, LC-MS and ELISA assay, respectively.
S9659 UNC6852 UNC6852 is a selective degrader that targets polycomb repressive complex 2 (PRC2) with IC50 of 247 nM for EED. UNC6852 is based on PROTAC and contains an EED226-derived ligand and a ligand for VHL.
A5058 Brd4 Rabbit Recombinant mAb Brd4 Rabbit Recombinant mAb detects endogenous levels of total Brd4.
A5240 ASH2L Rabbit Recombinant mAb ASH2L Rabbit Recombinant mAb detects endogenous level of total ASH2L.
A5247 PRMT5 Rabbit Recombinant mAb PRMT5 Rabbit Recombinant mAb detects endogenous level of total PRMT5.
S2184 WDR5-0103 WDR5-0103 (WD-Repeat Protein 5-0103) is a small-molecule antagonist of WDR5 (WD40 repeat protein 5) with Kd of 450 nM.
S7833 OICR-9429 OICR-9429 is a potent antagonist of the interaction of WDR5 with peptide regions of MLL and Histone 3 and reduces viability of acute myeloid leukemia cells in vitro. It binds to WDR5 with high affinity (KD = 93 ± 28 nM.
iScience, 2022, 25(1):103679
Nature, 2021, 10.1038/s41586-021-04116-8
J Exp Clin Cancer Res, 2021, 40(1):203
S8359 UNC3866 UNC3866 is a potent antagonist of the methyllysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. UNC3866 binds the chromodomains of CBX4 and CBX7 most potently, with a K(d) of ∼100 nM for each, and is 6- to 18-fold selective as compared to seven other CBX and CDY chromodomains.
Leukemia, 2021, 10.1038/s41375-021-01121-8
Int J Mol Sci, 2021, 22(2)E619
Leukemia, 2021, 10.1038/s41375-021-01121-8
S7820New EPZ020411 2HCl EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.
Theranostics, 2020, 10(1):133-150