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$0.00 Histone Methyltransferase
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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 -
CPI-360
Catalog No. A15908 EZH1 inhibitorCPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases. 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 -
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 -
GSK503
Catalog No. A15549 EZH2 InhibitorGSK-503 is a potent EZH2 inhibitor with potential anticancer activity. 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 -
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 -
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 -
WDR5-0103
Catalog No. A15928 WDR5 antagonistWDR5-0103 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). 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 -
MI-2 (Menin-MLL inhibitor 2)
Catalog No. A12929 Menin-MLL interaction inhibitorMI-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. Learn More -
LLY-507
Catalog No. A15813 SMYD2 inhibitorLLY-507 is a cell-active, small molecule inhibitor of SMYD2 with IC50 of= 15 nM. Learn More -
UNC0638
Catalog No. A12947 G9a/GLP HMTase inhibitorUNC0638 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. 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 -
UNC3866
Catalog No. A11599 CBX4 /CBX7 chromodomains antagonistUNC3866 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. Learn More -
UNC 2400
Catalog No. A13282 EZH1/EZH2 inhibitorUNC 2400, a close analogue of UNC1999, is a negative control of UNC1999 that inhibits EZH2 and EZH1. 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 -
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 -
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 -
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 -
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 -
UNC0642
Catalog No. A15487 G9a/GLP inhibitorUNC0642 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. 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 -
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 -
EPZ-6438 (Tazemetostat)
Catalog No. A12712 EZH2 inhibitorEPZ-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. 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 0224
Catalog No. A15388 G9a inhibitorUNC0224 is a potent and selective G9a inhibitor with IC50 of 15 nM in in the G9a Thioglo assay. Learn More -
BRD4770
Catalog No. A14401 -
3-deazaneplanocin A HCl (DZNep HCl)
Catalog No. A13947 EZH2 inhibitor3-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. 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 -
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 -
MI-3
Catalog No. A14218 menin-MLL interaction inhibitorMI-3 is a potent menin-MLL interaction inhibitor with IC50 of 648 nM. Learn More -
UNC 0638
Catalog No. A13690 G9a/GLP inhibitorUNC 0638 is a selective inhibitor of G9a and GLP histone lysine methyltransferases. 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 -
EPZ005687
Catalog No. A12439 -
Amodiaquine dihydrochloride dihydrate
Catalog No. A16405 Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase in human erythrocytes, also used as an antimalarial and anti-inflammatory agent. Learn More
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- Inhibitor (41)
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- COMT (1)
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- EZH2 (13)
- G9a (EHMT2) (10)
- GLP (EHMT1) (5)
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