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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.
Signaling Pathways | Target | TargetMol
Cat. No. Product name CAS No. Purity Chemical Structure
T3257 UNC0638 1255580-76-7 99.53%
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...
T6810 CPI-360 1802175-06-9 99.52%
CPI-360
CPI-360 is a small molecule EZH2 inhibitor (IC50: 0.002 μM, EC50: 0.080 μM) that shows antitumor activity in an EZH200-dependent tumor xenograft model.
T3057 UNC1999 1431612-23-5 99.49%
UNC1999
UNC1999 is a orally bioavailable, effective and specific inhibitor of EZH2 (IC50=2 nM) and EZH1 (IC50=45).
T9329 BRD0639 2760881-74-9 99.46%
BRD0639
BRD0639 is a pioneering inhibitor targeting the interaction between PRMT5 and its substrate adaptor. As a competitive inhibitor of the PRMT5 binding motif (PBM),...
T2079 GSK126 1346574-57-9 99.43%
GSK126
GSK126 (GSK2816126A) is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 nM).
T21767 MS37452 423748-02-1 99.39%
MS37452
MS37452 is a competitive inhibitor of CBX7 chromodomain binding to H3K27me3 (Ki = 43 µM).
T36631 BAY-6035 2247890-13-5 99.39%
BAY-6035
BAY-6035 is an inhibitor of SET and MYND domain-containing protein 3 (SMYD3). BAY-6035 has more than 100-fold selectivity over other histone methyltransferases.
T60002 DC-S239 303141-21-1 99.36%
DC-S239
DC-S239 (DC-S239) is a selective inhibitor of histone methyltransferase SETD7 (IC50 = 4.59 μM) with anticancer activity.
T6853 GSK591 1616391-87-7 99.35%
GSK591
GSK591 (GSK3203591), Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM).
T4583 PFI-2 hydrochloride 1627607-87-7 99.31%
PFI-2 hydrochloride
PFI-2 hydrochloride ((R)-PFI-2 hydrochloride) is a potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 (IC50: 2 nM), 5...
T8768 MM-102 TFA 1883545-52-5 99.3%
MM-102 TFA
MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM. MM-102 compound prevents the interaction between mixed l...
T6076 EPZ015666 1616391-65-1 99.29%
EPZ015666
EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 enzymatic activity.
TQ0058 MI-463 1628317-18-9 99.28%
MI-463
MI-463 is a potent and orally bioavailable inhibitor of the menin-mLL interaction (IC50: 15.3 nM).
T17204 UNC0321 1238673-32-9 99.25%
UNC0321
UNC0321 is an effective inhibitor of histone methyltransferase G9a with a Ki of 63 pM and with IC50s 9 nM and 6 nM in ECSD and CLOT assays. UNC0321 inhibits GLP ...
T3099 Pinometostat 1380288-87-8 99.19%
Pinometostat
Pinometostat (EPZ-5676) has been used in trials studying the treatment of Leukemia, Acute Leukemias, Acute Myeloid Leukemia, Myelodysplastic Syndrome, and Acute ...
T7403 BAY-598 1906919-67-2 99.18%
BAY-598
BAY-598 is a selective inhibitor of SMYD2 with IC50 values of 27 nM.
T6809 CPI-169 racemate 1450655-76-1 99.14%
CPI-169 racemate
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.
T11131 DW14800 2243709-60-4 99.12%
DW14800
DW14800 is an inhibitor of PRMT5 (IC50 = 17 nM), enhances the transcription of HNF4α, and reduces the level of H4R3me2s.
T8548 Metoprine 7761-45-7 99.09%
Metoprine
Metoprine is a potent inhibitor of histamine N-methyltransferase (HMT), with potential antineoplastic activity.
T10882 CPUY074020 902279-44-1 99.07%
CPUY074020
CPUY074020 is a potent and orally bioavailable inhibitor of histone methyltransferase G9a (IC50: 2.18 μM) with anti-proliferative 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 ep...
CPI-360
T6810
CPI-360 is a small molecule EZH2 inhibitor (IC50: 0.002 μM, EC50: 0.080 μM) that shows antitumor activity in an EZH200-dependent tumor xenograft model.
UNC1999
T3057
UNC1999 is a orally bioavailable, effective and specific inhibitor of EZH2 (IC50=2 nM) and EZH1 (IC50=45).
BRD0639
T9329
BRD0639 is a pioneering inhibitor targeting the interaction between PRMT5 and its substrate adaptor. As a competitive inhibitor of the PRMT5 binding motif (PBM),...
GSK126
T2079
GSK126 (GSK2816126A) is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 nM).
MS37452
T21767
MS37452 is a competitive inhibitor of CBX7 chromodomain binding to H3K27me3 (Ki = 43 µM).
BAY-6035
T36631
BAY-6035 is an inhibitor of SET and MYND domain-containing protein 3 (SMYD3). BAY-6035 has more than 100-fold selectivity over other histone methyltransferases.
DC-S239
T60002
DC-S239 (DC-S239) is a selective inhibitor of histone methyltransferase SETD7 (IC50 = 4.59 μM) with anticancer activity.
GSK591
T6853
GSK591 (GSK3203591), Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM).
PFI-2 hydrochloride
T4583
PFI-2 hydrochloride ((R)-PFI-2 hydrochloride) is a potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 (IC50: 2 nM), 5...
MM-102 TFA
T8768
MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM. MM-102 compound prevents the interaction between mixed l...
EPZ015666
T6076
EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 enzymatic activity.
MI-463
TQ0058
MI-463 is a potent and orally bioavailable inhibitor of the menin-mLL interaction (IC50: 15.3 nM).
UNC0321
T17204
UNC0321 is an effective inhibitor of histone methyltransferase G9a with a Ki of 63 pM and with IC50s 9 nM and 6 nM in ECSD and CLOT assays. UNC0321 inhibits GLP ...
Pinometostat
T3099
Pinometostat (EPZ-5676) has been used in trials studying the treatment of Leukemia, Acute Leukemias, Acute Myeloid Leukemia, Myelodysplastic Syndrome, and Acute ...
BAY-598
T7403
BAY-598 is a selective inhibitor of SMYD2 with IC50 values of 27 nM.
CPI-169 racemate
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.
DW14800
T11131
DW14800 is an inhibitor of PRMT5 (IC50 = 17 nM), enhances the transcription of HNF4α, and reduces the level of H4R3me2s.
Metoprine
T8548
Metoprine is a potent inhibitor of histamine N-methyltransferase (HMT), with potential antineoplastic activity.
CPUY074020
T10882
CPUY074020 is a potent and orally bioavailable inhibitor of histone methyltransferase G9a (IC50: 2.18 μM) with anti-proliferative activity.
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