Histone Methyltransferase
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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 .
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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.
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EZH2 Inhibitor
GSK-503 is a potent EZH2 inhibitor with potential anticancer activity.
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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.
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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.
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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.
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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)
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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.
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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.
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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.
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- Lucy E. Dawson, .et al. Induction of Myogenic Differentiation Improves Chemosensitivity of Chemoresistant Cells in Soft-Tissue Sarcoma Cell Lines, Sarcoma, 2020, 2020: 8647981 PMID: 32300280
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Dupret B, .et al. The histone lysine methyltransferase Ezh2 is required for maintenance of the intestine integrity and for caudal fin regeneration in zebrafish, Biochim Biophys Acta Gene Regul Mech, 2017, Oct;1860(10):1079-1093 PMID: 28887218
- Theresa Baker, .et al. Acquisition of a single EZH2 D1 domain mutation confers acquired resistance to EZH2-targeted inhibitors, Oncotarget, 2015, Oct 20; 6(32): 32646-32655 PMID: 26360609
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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.
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G9a inhibitor
CPUY074020 is a potent G9a inhibitor with an IC50 of 2.18 μM, and possesses anti-proliferative activity .
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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.
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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.
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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.
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- Guang Bai, .et al. Chapter 1 - Epigenetic Tools in Chronic Pain Studies, Epigenetics of Chronic Pain, 2019, Pages 1-48
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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.
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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.
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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.
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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.
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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.
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COMT inhibitor
Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor.
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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).
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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).
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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.
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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.
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G9a/GLP inhibitor
A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 value of 3.3 nM.
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EZH2 inhibitor
JQEZ5 is a potent and selective SAM-competitive EZH2 lysine methyltransferase inhibitor with IC50 value of 11 nM.
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EZH2 inhibitor
PF-06726304 is a potent and SAM-competitive EZH2 (Enhancer of Zeste Homolog 2) lysine methyltransferase inhibitor.
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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.
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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)
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SMYD3 inhibitor
BCI-121 is an SMYD3 inhibitor. It acts by impairing cancer cell growth.
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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.
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histone lysine methyltransferase inhibitor
BIX-01338 hydrate is a histone lysine methyltransferase inhibitor.
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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.
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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.
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G9a/GLP HMT inhibitor
BIX 01294 is a G9a-like protein and G9a histone lysine methyltransferase inhibitor.
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DOT1L Inhibitor
EPZ-5676 is a small molecule inhibitor of histone methyltransferase with potential antineoplastic activity.
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- Yoo H, .et al. Epigenetic priming by Dot1l in lymphatic endothelial progenitors ensures normal lymphatic development and function, Cell Death Dis, 2020, Jan; 11(1): 14 PMID: 31908356
- Guang Bai, .et al. Chapter 1 - Epigenetic Tools in Chronic Pain Studies, Epigenetics of Chronic Pain, 2019, Pages 1-48
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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.
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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).
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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.
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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).
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- Nie L, .et al. CDK2-mediated site-specific phosphorylation of EZH2 drives and maintains triple-negative breast cancer, Nat Commun, 2019, Nov 8;10(1):5114 PMID: 31704972
- Yang PM, .et al. p38α/S1P/SREBP2 activation by the SAM-competitive EZH2 inhibitor GSK343 limits its anticancer activity but creates a druggable vulnerability in hepatocellular carcinoma, Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
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COMT inhibitor
opicapone is a novel catechol-O-methyltransferase inhibitor
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G9a HMTase inhibitor
UNC0321 is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date
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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.
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DOT1L inhibitor
SGC 0946 is a potent DOT1L methyltransferase inhibitor that blocks H3K79 methylation in A431 cells and MCF10A cells.
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G9a/GLP inhibitor
UNC 0638 is a selective inhibitor of G9a and GLP histone lysine methyltransferases.
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menin-MLL interaction inhibitor
MI-3 is a potent menin-MLL interaction inhibitor with IC50 of 648 nM.
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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.
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MLL1 inhibitor
MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 uM.
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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.
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