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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
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.
T28996 TP-064 2080306-20-1 99.07%
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...
T9742 SETDB1-TTD-IN-1 2755823-12-0 99.05%
SETDB1-TTD-IN-1
SETDB1-TTD-IN-1 is a potent, selective and endogenous binder competitive inhibitor of SETDB1-TTD with a Kd of 88 nM.
T17002 Tazemetostat hydrobromide 1467052-75-0 99.03%
Tazemetostat hydrobromide
Tazemetostat hydrobromide (E-7438 hydrobromide) is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repre...
T15194 EBI-2511 2098546-05-3 99.01%
EBI-2511
EBI-2511 is a highly potent and orally active inhibitor of EZH2 (IC50: 6 nM in Pfeffiera cell lines).
T3081 EPZ004777 1338466-77-5 98.99%
EPZ004777
EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
T1959 BIX-01294 trihydrochloride 1392399-03-9 98.98%
BIX-01294 trihydrochloride
BIX-01294 trihydrochloride is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.
T63351L MS8511 HCl 98.90%
MS8511 HCl
MS8511 HCl is a selective and potent covalent inhibitor of G9a/GLP that acts by targeting cysteine residues in the substrate binding site. MS8511 has anticancer ...
T9969 EZM0414 2411748-50-8 98.9%
EZM0414
EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 with IC50 of 18 nM in SETD2 biochemical assay and IC50 of 34 nM in a cellular assay. EZM04...
T9399 Menin-MLL inhibitor 20 2448173-47-3 98.89%
Menin-MLL inhibitor 20
Menin-MLL inhibitor 20 is an irreversible inhibitor of menin-MLL interaction with antitumor activities (WO2020142557A1, compound 6).
T2379 UNC1215 1415800-43-9 98.87%
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 ...
T9681 MAK-683 hydrochloride 2170606-94-5 98.87%
MAK-683 hydrochloride
MAK683 hydrochloride is an inhibitor of embryonic ectoderm development (EED) (patent US20160176882 A1, compound example 2). MAK683 exhibits IC50s of 59, 26, 89 n...
T67883 EZH2-IN-15 2098545-98-1 98.85%
EZH2-IN-15
EZH2-IN-15 is a specific inhibitor of histone modifier enhancer of zeste 2 (EZH2). EZH2 is aberrantly overexpressed in a number of human cancers that controls th...
T8381 Amodiaquine 86-42-0 98.84%
Amodiaquine
Amodiaquine is a synthetic aminoquinoline, used to treat malaria.
T15767 LLY-283 2040291-27-6 98.79%
LLY-283
LLY-283 is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM and a Kd of 6 nM for PRMT5:MEP50 complex, a...
T13279L Valemetostat 1809336-39-7 98.77%
Valemetostat
Valemetostat (DS-3201) is a first-in-class EZH1/2 dual inhibitor.
T6333 MM-102 1417329-24-8 98.77%
MM-102
MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.
T2354 UNC 0631 1320288-19-4 98.76%
UNC 0631
UNC 0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).
T4166 UNC0642 1481677-78-4 98.75%
UNC0642
UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM).
T14841 BVT948 39674-97-0 98.70%
BVT948
BVT948 is a protein tyrosine phosphatase (PTP) inhibitor. It can also inhibit several CYP450 isoforms and lysine methyltransferase SETD8 (KMT5A).
CPUY074020
T10882
CPUY074020 is a potent and orally bioavailable inhibitor of histone methyltransferase G9a (IC50: 2.18 μM) with anti-proliferative activity.
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...
SETDB1-TTD-IN-1
T9742
SETDB1-TTD-IN-1 is a potent, selective and endogenous binder competitive inhibitor of SETDB1-TTD with a Kd of 88 nM.
Tazemetostat hydrobromide
T17002
Tazemetostat hydrobromide (E-7438 hydrobromide) is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repre...
EBI-2511
T15194
EBI-2511 is a highly potent and orally active inhibitor of EZH2 (IC50: 6 nM in Pfeffiera cell lines).
EPZ004777
T3081
EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
BIX-01294 trihydrochloride
T1959
BIX-01294 trihydrochloride is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.
MS8511 HCl
T63351L
MS8511 HCl is a selective and potent covalent inhibitor of G9a/GLP that acts by targeting cysteine residues in the substrate binding site. MS8511 has anticancer ...
EZM0414
T9969
EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 with IC50 of 18 nM in SETD2 biochemical assay and IC50 of 34 nM in a cellular assay. EZM04...
Menin-MLL inhibitor 20
T9399
Menin-MLL inhibitor 20 is an irreversible inhibitor of menin-MLL interaction with antitumor activities (WO2020142557A1, compound 6).
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 ...
MAK-683 hydrochloride
T9681
MAK683 hydrochloride is an inhibitor of embryonic ectoderm development (EED) (patent US20160176882 A1, compound example 2). MAK683 exhibits IC50s of 59, 26, 89 n...
EZH2-IN-15
T67883
EZH2-IN-15 is a specific inhibitor of histone modifier enhancer of zeste 2 (EZH2). EZH2 is aberrantly overexpressed in a number of human cancers that controls th...
Amodiaquine
T8381
Amodiaquine is a synthetic aminoquinoline, used to treat malaria.
LLY-283
T15767
LLY-283 is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM and a Kd of 6 nM for PRMT5:MEP50 complex, a...
Valemetostat
T13279L
Valemetostat (DS-3201) is a first-in-class EZH1/2 dual inhibitor.
MM-102
T6333
MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.
UNC 0631
T2354
UNC 0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).
UNC0642
T4166
UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM).
BVT948
T14841
BVT948 is a protein tyrosine phosphatase (PTP) inhibitor. It can also inhibit several CYP450 isoforms and lysine methyltransferase SETD8 (KMT5A).
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TargetMol