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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.
Cat No. product name
TQ0058 MI-463 MI-463 is a potent and orally bioavailable inhibitor of the menin-mLL interaction (IC50: 15.3 nM).
T8879 MR837 ZINC30303842 is a NSD2-PWWP1 antagonist.
T9575 MRTX9768 MRTX-9768 is a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors.
T1959 BIX-01294 trihydrochloride BIX01294 is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.
T3201 WDR5-0103 WDR5-0103 is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
T16886 Sinefungin Sinefungin is an effective inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication. Sinefungin i...
T15201 MAK683 MAK683 is an inhibitor of embryonic ectoderm development (EED) (IC50s: 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay).
T16072 MI-538 MI-538 is an interaction between menin and MLL fusion proteins inhibitor(IC50 of 21 nM).
T14841 BVT948 BVT948 is a protein tyrosine phosphatase (PTP) inhibitor. It can also inhibit several CYP450 isoforms and lysine methyltransferase SETD8 (KMT5A).
T8381 Amodiaquine Amodiaquine is a synthetic aminoquinoline, used to treat malaria.
T13780 MS1943 MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).
T1868 JIB-04 JIB-04 is a pan-selective Jumonji histone demethylase inhibitor.
T9102 WM-3835 WM-3835 is a novel and high-specific small molecule inhibitor of Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) , able to potently suppressed OS cell proliferati...
T10205 A-395 A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12, IC5...
T2379 UNC1215 UNC1215, an effective and specific MBT (malignant brain tumor) antagonist, binds L3MBTL3 (IC50/Kd: 40/120 nM). The selectivity of UNC1215 for L3MBTL3 is 50-fold ...
T8548 Metoprine Metoprine is a potent inhibitor of histamine N-methyltransferase (HMT), with potential antineoplastic activity.
T13336 VTP50469 VTP50469 is a highly selective and orally active inhibitor of Menin-MLL interaction( Ki: 104 pM) and has potently anti-leukemia activity.
T3257 UNC0638 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 ep...
T6916 OICR-9429 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 leukemi...
T2649 Menin-MLL inhibitor MI-2 MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.
T3081L EPZ004777 hydrochloride EPZ004777 hydrochloride is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
T0174 Cyproheptadine hydrochloride sesquihydrate Cyproheptadine hydrochloride sesquihydrate, an antihistamine, is an antagonist of serotonin and histamine2.
T27133 DCLX069 DCLX069 is a potent and selective PRMT1 inhibitor. DCLX069 occupies the SAM binding pocket to exert the inhibitory effect. DCLX069 effectively blocks cell prolif...
T6857 HLCL-61 hydrochloride HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.
T16435 PBIT PBIT inhibits JARID1B histone demethylase (IC50 of about 3 μM). PBIT also inhibits JARID1A and JARID1C (IC50s of 6 μM and 4.9 μM, respectively). PBIT is a specif...
T6809 CPI-169 racemate 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.
T6484 EI1 EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
T6810 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.
T3624 A-366 Potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC50 = 3.3 nM). Exhibits >1000-fold selectivity for G9a/GLP over 21 other methyltransfer...
T6803 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 an...
T12943 SNDX-5613 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-rearra...
T3081 EPZ004777 EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
T0381 Amodiaquine dihydrochloride dihydrate Amodiaquine Hydrochloride is the hydrochloride salt of amodiaquine, an orally active 4-aminoquinoline derivative with antimalarial and anti-inflammatory properti...
T8838 CCI-007 CCI 007 is a selective inhibitor of MLL-r, CALM-AF10 and SET-NUP214 leukemia with IC50 of 3.5 uM against MLL-r leukemia cell line PER-485
T2643 MI-3 MI-3 (Menin-MLL Inhibitor) is an effective inhibitor of Menin-MLL interaction (IC50: 648 nM).
T11925 M‑89 M-89 inhibits the menin-mixed lineage leukemia (Menin-MLL) protein-protein interaction and has potential to treat MLL leukemia. M-89 is a highly potent and speci...
T12886 SGC-iMLLT SGC-iMLLT is a potent and selective MLLT1/3-histone interactions inhibitor(IC50 of 0.26 μM),and is a first-in-class chemical probe.
T3057 UNC1999 UNC1999 is a orally bioavailable, effective and specific inhibitor of EZH2 (IC50=2 nM) and EZH1 (IC50=45).
T6360 3-deazaneplanocin A HCl 3-deazaneplanocin A (DZNeP)HCl, an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM.
T7697 BIX-01294 BIX-01294 is an G9a Histone Methyltransferase inhibitor(IC50 : 1.9 μM).
T28996 TP-064 TP-064 is a potent and selective PRMT4 inhibitor. TP-064 includes inhibition of PRMT4 with IC50 < 10nM for methylation of H3 (1-25) and greater than 100-fold sel...
T6059 GSK343 GSK343, a specific and effective EZH2 inhibitor (IC50=4 nM), exhibits 60 fold specificity activity against EZH1, and >1000 fold specificity activity against othe...
TQ0069 MI-503 MI-503 is a highly effective and orally bioavailable inhibitor of the menin-mLL interaction.
T7194 CM-272 CM-272 is a dual G9a/DNA methyltransferases (DNMTs) inhibitor.
T5484 GSK467 GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM).
T6292 3-Deazaneplanocin A 3-Deazaneplanocin A (DZNep) is an attractive epigenetic anticancer agent through the inhibition of the cellular enhancer of zeste homolog 2 (EZH2) protein.
T9399 Menin-MLL inhibitor 20 Menin-MLL inhibitor 20 is an irreversible menin-MLL interaction inhibitor with antitumor activities (WO2020142557A1, compound 6)[1].
T1905 EPZ005687 EPZ005687 is a potent and selective inhibitor of EZH2.
T1923 BRD4770 BRD4770 is a histone methyltransferase G9a inhibitor and induces cell senescence.
T1987 PFI-2 PFI-2 is an effective, specific and cell-active lysine methyltransferase SETD7 inhibitor (Ki/IC50: 0.33/2 nM), 1000-fold selectivity over other methyltransferase...
MI-463
TQ0058
MI-463 is a potent and orally bioavailable inhibitor of the menin-mLL interaction (IC50: 15.3 nM).
MR837
T8879
ZINC30303842 is a NSD2-PWWP1 antagonist.
MRTX9768
T9575
MRTX-9768 is a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors.
BIX-01294 trihydrochloride
T1959
BIX01294 is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.
WDR5-0103
T3201
WDR5-0103 is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).
Sinefungin
T16886
Sinefungin is an effective inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication. Sinefungin i...
MAK683
T15201
MAK683 is an inhibitor of embryonic ectoderm development (EED) (IC50s: 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay).
MI-538
T16072
MI-538 is an interaction between menin and MLL fusion proteins inhibitor(IC50 of 21 nM).
BVT948
T14841
BVT948 is a protein tyrosine phosphatase (PTP) inhibitor. It can also inhibit several CYP450 isoforms and lysine methyltransferase SETD8 (KMT5A).
Amodiaquine
T8381
Amodiaquine is a synthetic aminoquinoline, used to treat malaria.
MS1943
T13780
MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).
JIB-04
T1868
JIB-04 is a pan-selective Jumonji histone demethylase inhibitor.
WM-3835
T9102
WM-3835 is a novel and high-specific small molecule inhibitor of Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) , able to potently suppressed OS cell proliferati...
A-395
T10205
A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12, IC5...
UNC1215
T2379
UNC1215, an effective and specific MBT (malignant brain tumor) antagonist, binds L3MBTL3 (IC50/Kd: 40/120 nM). The selectivity of UNC1215 for L3MBTL3 is 50-fold ...
Metoprine
T8548
Metoprine is a potent inhibitor of histamine N-methyltransferase (HMT), with potential antineoplastic activity.
VTP50469
T13336
VTP50469 is a highly selective and orally active inhibitor of Menin-MLL interaction( Ki: 104 pM) and has potently anti-leukemia activity.
UNC0638
T3257
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 e...
OICR-9429
T6916
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 leukemi...
Menin-MLL inhibitor MI-2
T2649
MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.
EPZ004777 hydrochloride
T3081L
EPZ004777 hydrochloride is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
Cyproheptadine hydrochloride sesquihydrate
T0174
Cyproheptadine hydrochloride sesquihydrate, an antihistamine, is an antagonist of serotonin and histamine2.
DCLX069
T27133
DCLX069 is a potent and selective PRMT1 inhibitor. DCLX069 occupies the SAM binding pocket to exert the inhibitory effect. DCLX069 effectively blocks cell prolif...
HLCL-61 hydrochloride
T6857
HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.
PBIT
T16435
PBIT inhibits JARID1B histone demethylase (IC50 of about 3 μM). PBIT also inhibits JARID1A and JARID1C (IC50s of 6 μM and 4.9 μM, respectively). PBIT is a spe...
CPI-169 racemate
T6809
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.
EI1
T6484
EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
CPI-360
T6810
CPI-360 is a potent, selective, and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.
A-366
T3624
Potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC50 = 3.3 nM). Exhibits >1000-fold selectivity for G9a/GLP over 21 other methyltransfer...
Chaetocin
T6803
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...
SNDX-5613
T12943
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-rearra...
EPZ004777
T3081
EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
Amodiaquine dihydrochloride dihydrate
T0381
Amodiaquine Hydrochloride is the hydrochloride salt of amodiaquine, an orally active 4-aminoquinoline derivative with antimalarial and anti-inflammatory properti...
CCI-007
T8838
CCI 007 is a selective inhibitor of MLL-r, CALM-AF10 and SET-NUP214 leukemia with IC50 of 3.5 uM against MLL-r leukemia cell line PER-485
MI-3
T2643
MI-3 (Menin-MLL Inhibitor) is an effective inhibitor of Menin-MLL interaction (IC50: 648 nM).
M‑89
T11925
M-89 inhibits the menin-mixed lineage leukemia (Menin-MLL) protein-protein interaction and has potential to treat MLL leukemia. M-89 is a highly potent and speci...
SGC-iMLLT
T12886
SGC-iMLLT is a potent and selective MLLT1/3-histone interactions inhibitor(IC50 of 0.26 μM),and is a first-in-class chemical probe.
UNC1999
T3057
UNC1999 is a orally bioavailable, effective and specific inhibitor of EZH2 (IC50=2 nM) and EZH1 (IC50=45).
3-deazaneplanocin A HCl
T6360
3-deazaneplanocin A (DZNeP)HCl, an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM.
BIX-01294
T7697
BIX-01294 is an G9a Histone Methyltransferase inhibitor(IC50 : 1.9 μM).
TP-064
T28996
TP-064 is a potent and selective PRMT4 inhibitor. TP-064 includes inhibition of PRMT4 with IC50 < 10nM for methylation of H3 (1-25) and greater than 100-fold sel...
GSK343
T6059
GSK343, a specific and effective EZH2 inhibitor (IC50=4 nM), exhibits 60 fold specificity activity against EZH1, and >1000 fold specificity activity against othe...
MI-503
TQ0069
MI-503 is a highly effective and orally bioavailable inhibitor of the menin-mLL interaction.
CM-272
T7194
CM-272 is a dual G9a/DNA methyltransferases (DNMTs) inhibitor.
GSK467
T5484
GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM).
3-Deazaneplanocin A
T6292
3-Deazaneplanocin A (DZNep) is an attractive epigenetic anticancer agent through the inhibition of the cellular enhancer of zeste homolog 2 (EZH2) protein.
Menin-MLL inhibitor 20
T9399
Menin-MLL inhibitor 20 is an irreversible menin-MLL interaction inhibitor with antitumor activities (WO2020142557A1, compound 6)[1].
EPZ005687
T1905
EPZ005687 is a potent and selective inhibitor of EZH2.
BRD4770
T1923
BRD4770 is a histone methyltransferase G9a inhibitor and induces cell senescence.
PFI-2
T1987
PFI-2 is an effective, specific and cell-active lysine methyltransferase SETD7 inhibitor (Ki/IC50: 0.33/2 nM), 1000-fold selectivity over other methyltransferase...
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