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$0.00 Histone Methyltransferase
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OICR-9429
Catalog No. A16641 Wdr5-MLL interaction antagonistOICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction with IC50 of 5 uM. inhibit proliferation and induce differentiation . Learn More -
Flopropione
Catalog No. A16550 5-HT1A receptor antagonist/COMT inhibitorFlopropione is a 5-HT1A receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor. Learn More -
GSK503
Catalog No. A15549 EZH2 InhibitorGSK-503 is a potent EZH2 inhibitor with potential anticancer activity. Learn More -
EPZ011989
Catalog No. A15544 EZH2 InhibitorEPZ011989 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 -
CPI-360
Catalog No. A15908 EZH2 inhibitorCPI-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. Learn More -
CPI-169
Catalog No. A15920 EZH2 inhibitorCPI-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 -
CM-272
Catalog No. A17173 G9a/DNMT inhibitorCM-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) Learn More -
CM-579
Catalog No. A18692 G9a/DNMT inhibitorCM-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. Learn More -
SMYD3-IN-1
Catalog No. A18572 SMYD3 inhibitorSMYD3-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. Learn More -
GSK126
Catalog No. A11757 EZH2 inhibitorGSK126 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 -
Entacapone
Catalog No. A10355 COMT inhibitorEntacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment. Learn More -
CPUY074020
Catalog No. A12190 G9a inhibitorCPUY074020 is a potent G9a inhibitor with an IC50 of 2.18 μM, and possesses anti-proliferative activity . Learn More -
OICR-0547
Catalog No. A20877 Wdr5-MLL interaction antagonistOICR-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. Learn More -
PF-06821497
Catalog No. A21388 EZH2 inhibitorPF-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. Learn More -
UNC-1999
Catalog No. A13166 EZH2/EZH1 InhibitorUNC1999 is the first orally bioavailable inhibitor that has high in vitro potency for wildtype and mutant EZH2 as well as EZH1. Learn More -
GSK2807 Trifluoroacetate
Catalog No. A21731 SMYD3 inhibitorGSK2807 Trifluoroacetate is a potent, selective and SAM-competitive inhibitor of SMYD3, with a Ki of 14 nM and an IC50 of 130 nM. Learn More -
Entacapone sodium salt
Catalog No. A21888 COMT inhibitorEntacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment. Learn More -
DZNep
Catalog No. A11377 EZH2 Inhibitor3 Deazaneplanocin A (DZNep) is a cyclopentenyl analog of 3-deazaadenosine, originally synthesized as an inhibitor of S-adenosyl-L-homocysteine hydrolase. Learn More -
MM-589 TFA
Catalog No. A21892 WDR5 and MLL protein-protein interaction inhibitorMM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. Learn More -
MM-102 TFA
Catalog No. A21941 WDR5/MLL interaction inhibitorMM-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. Learn More -
Tolcapone
Catalog No. A20966 COMT inhibitorTolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor. Learn More -
AZ505
Catalog No. A13061 SMYD2 inhibitorAZ505 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 -
AZ505 ditrifluoroacetate
Catalog No. A13169 SMYD2 inhibitorAZ505 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 -
CPI-1205
Catalog No. A16357 EZH2 inhibitorCPI-1205 is a highly potent (biochemical IC50 = 0.002 μM, cellular EC50 = 0.032 μM) and selective inhibitor of EZH2. Learn More -
EPZ031686
Catalog No. A16375 SMYD3/ MEKK2 inhibitorEPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ki=1.2 and 1.1 nM respectively. Learn More -
A-366
Catalog No. A15969 G9a/GLP inhibitorA-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 value of 3.3 nM. Learn More -
JQEZ5
Catalog No. A16961 EZH2 inhibitorJQEZ5 is a potent and selective SAM-competitive EZH2 lysine methyltransferase inhibitor with IC50 value of 11 nM. Learn More -
PF-06726304
Catalog No. A16937 EZH2 inhibitorPF-06726304 is a potent and SAM-competitive EZH2 (Enhancer of Zeste Homolog 2) lysine methyltransferase inhibitor. Learn More -
JNJ-64619178
Catalog No. A16861 Histone Methyltransferase inhibitorJNJ-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 -
BAY-598
Catalog No. A17012 SMYD2 inhibitorBAY-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 -
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BCI-121
Catalog No. A17065 SMYD3 inhibitorBCI-121 is an SMYD3 inhibitor. It acts by impairing cancer cell growth. Learn More -
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GNA002
Catalog No. A13266 covalent EZH2 inhibitorGNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. Learn More -
BIX-01338 hydrate
Catalog No. A21812 histone lysine methyltransferase inhibitorBIX-01338 hydrate is a histone lysine methyltransferase inhibitor. Learn More -
MI-503
Catalog No. A20975 menin-mLL interaction inhibitorMI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction. Learn More -
PFI-2
Catalog No. A14216 SETD7 inhibitorPFI-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 -
BIX 01294
Catalog No. A11763 G9a/GLP HMT inhibitorBIX 01294 is a G9a-like protein and G9a histone lysine methyltransferase inhibitor. Learn More -
EPZ-5676 (Pinometostat)
Catalog No. A12735 DOT1L InhibitorEPZ-5676 is a small molecule inhibitor of histone methyltransferase with potential antineoplastic activity. Learn More -
Chaetocin
Catalog No. A12812 SUV39H HMT InhibitorChaetocin 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 -
UNC0646
Catalog No. A13194 G9a/GLP HMTase inhibitorUNC0646 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 -
UNC0631
Catalog No. A13195 G9a inhibitorUNC-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 -
GSK343
Catalog No. A13114 EZH2 inhibitorGSK343 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 -
Opicapone (BIA 9-1067)
Catalog No. A13110 -
UNC0321
Catalog No. A13200 G9a HMTase inhibitorUNC0321 is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date Learn More -
EPZ004777
Catalog No. A12983 DOT1L inhibitorEPZ004777 is a potent, selective inhibitor of DOT1L. EPZ004777 selectively inhibits cellular H3K79 methylation and inhibits expression of key MLL fusion target genes. Learn More -
SGC 0946
Catalog No. A12941 DOT1L inhibitorSGC 0946 is a potent DOT1L methyltransferase inhibitor that blocks H3K79 methylation in A431 cells and MCF10A cells. Learn More -
UNC 0638
Catalog No. A13690 G9a/GLP inhibitorUNC 0638 is a selective inhibitor of G9a and GLP histone lysine methyltransferases. Learn More -
MI-3
Catalog No. A14218 menin-MLL interaction inhibitorMI-3 is a potent menin-MLL interaction inhibitor with IC50 of 648 nM. Learn More -
EI1
Catalog No. A12711 EZH2 inhibitorEI1 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 -
MM-102
Catalog No. A14315 MLL1 inhibitorMM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 uM. Learn More -
UNC0379
Catalog No. A14320 SETD8 HMTase inhibitorUNC0379 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
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- Inhibitor (57)
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- COMT (1)
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- EZH1 (1)
- EZH2 (13)
- G9a (EHMT2) (10)
- GLP (EHMT1) (5)
- Menin-MLL interaction (2)
- MLL1 (1)
- SETD7 (1)
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- SMYD2 (2)
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- SUV39H (1)
- WDR5 (1)
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