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Chromatin/Epigenetic Histone Methyltransferase

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
T3081 EPZ004777 EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
T3082 SGC0946 SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.
T3084 SGC707 SGC707 is a potent, selective, and cell-active allosteric inhibitor of PRMT3.
T3099 Pinometostat EPZ5676 has been used in trials studying the treatment of Leukemia, Acute Leukemias, Acute Myeloid Leukemia, Myelodysplastic Syndrome, and Acute Lymphocytic Leu...
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 ...
T3458 EED226 EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.
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 methyltransf...
T3896 Shanzhiside methyl ester Shanzhiside methylester reduces neuropathic pain by activating spinal GLP-1 receptors and subsequently stimulating microglial β-endorphin expression via the p3...
T3984 GLP-1(7-36) GLP-1 (7-36) amide is a peptide hormone released from intestinal L-cells upon nutrient consumption. It binds the GLP-1 receptor in the pancreas and displays var...
T4013 SGC2085 HCl SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) Inhibitor with an IC50 of 50 nM and more than undred-fold selectiv...
T4021 UNC3866 UNC3866 is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen.
T4166 UNC-0642 UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM).
T4314 EPZ020411 EPZ020411 is a specific and effective inhibitor of PRMT6 (IC50=10 nM).
T4334 EPZ020411 2HCl (1700663-41-7(free base)) EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).
T4343 A-196 A-196 is a potent and selective inhibitor of SUV420 h1 and SUV420 h2 with IC50 values of 0.025 and 0.144 μM, respectively; more than 100-fold selective over ot...
T4378 MS049 MS 049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC 50 of 34 nM and 43 nM, respectively.
T4393 MS049 2HCl (1502816-23-0(free base)) MS049 is a potent and selective inhibitor of PRMT4 (IC50 = 34 nM) and PRMT6 (IC50 = 43 nM). It is less active against additional type I PRMTs (IC50s = >130, >22...
T4583 (R)-PFI-2 hydrochloride PFI-2 hydrochloride is a potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 (IC50: 2 nM), 500 fold active than (S)-P...
T5322 BCI-121 BCI-121 is a substrate-competitive SMYD3 inhibitor that inhibits the proliferation of the cancer cell.
T5605 EZM 2302 EZM2302 is a selective, and orally available arginine methyltransferase CARM1 inhibitor (IC50: 6 nM).
T5745 GSK3326595 GSK3326595 is an inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50:6.2 nM.).
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 ot...
T6076 EPZ015666 EPZ015666 is an orally available inhibitor of PRMT5 enzymatic activity.
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.
T6790 BMS-911543 BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2.
T6809 CPI-169 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.
T6853 GSK591 GSK591,Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM).
T6857 HLCL-61 hydrochloride HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.
T6876 Liraglutide Liraglutide is a long-acting GLP-1 receptor agonist.
T6879 LLY-507 LLY-507 is an effective, cell-active, and specific inhibitor of protein-lysine Methyltransferase SMYD2.
T6900 MS023 MS023 is a potent, selective, and cell-active Type I PRMT inhibitor with IC50 of 30 nM, 119 nM, 83 nM, 4 nM, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, ...
T7089 SGC2085 SGC2085 is an effective and selective coactivator-associated arginine methyltransferase 1 (CARM1) inhibitor (IC50: 50 nM).
T7157 XY1 XY1 is a very close analogue of SGC707 (a potent, selective, and non-competitive inhibitor of PRMT3 with IC50 of 31 nM), It is intended to be used as a negative...
T7305 JQEZ5 JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 nM).
T7378 BRD9539 BRD9539 is an inhibitor of euchromatin histone methyltransferase 2 (EHMT2), also known as G9a, with an IC50 value of 6.3 μM
T7403 BAY-598 BAY-598 is a selective inhibitor of SMYD2 with IC50 values of 27 nM.
T7697 BIX-01294 BIX-01294 is an G9a Histone Methyltransferase inhibitor(IC50 : 1.9 μM).
T8201 Gambogenic acid Gambogenic acid is a natural product,is an effective inhibitor of EZH2,with anticancer activity. 
T8510 CPI-1205 CPI-1205 is a highly potent and selective inhibitor of EZH2(IC50 : 0.002 μM, EC50 : 0.032 μM) .
TN5096 Tanshindiol B Tanshindiol B possesses a unique anti-cancer activity whose mechanism involves the inhibition of EZH2 activity and would provide chemically valuable information...
TN5097 Tanshindiol C Tanshindiol C protects macrophages from oxLDL induced foam cell formation via activation of Prdx1/ABCA1 signaling and that Prdx1 may be a novel target for thera...
TQ0058 MI-463 MI-463 is a potent and orally bioavailable inhibitor of the menin-mLL interaction (IC50: 15.3 nM).
TQ0069 MI-503 MI-503 is a highly effective and orally bioavailable inhibitor of the menin-mLL interaction.
TQ0100 AZ505 AZ505 is an effective and specific SMYD2 inhibitor (IC50: 0.12 μM).
TQ0232 UNC 0646 UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases, G9a and GLP (IC50s: 6 nM/15 nM for G9a/GLP). UNC0646 potently b...
TQ0263 EPZ031686 EPZ031686 is a selective and orally available SMYD3 inhibitor (IC50: 3 nM).
EPZ004777
T3081CAS 1338466-77-5
EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
SGC0946
T3082CAS 1561178-17-3
SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.
SGC707
T3084CAS 1687736-54-4
SGC707 is a potent, selective, and cell-active allosteric inhibitor of PRMT3.
Pinometostat
T3099CAS 1380288-87-8
EPZ5676 has been used in trials studying the treatment of Leukemia, Acute Leukemias, Acute Myeloid Leukemia, Myelodysplastic Syndrome, and Acute Lymphocytic Leu...
UNC0638
T3257CAS 1255580-76-7
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 ...
EED226
T3458CAS 2083627-02-3
EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.
A-366
T3624CAS 1527503-11-2
Potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC50 = 3.3 nM). Exhibits >1000-fold selectivity for G9a/GLP over 21 other methyltransf...
Shanzhiside methyl ester
T3896CAS 64421-28-9
Shanzhiside methylester reduces neuropathic pain by activating spinal GLP-1 receptors and subsequently stimulating microglial β-endorphin expression via the p3...
GLP-1(7-36)
T3984CAS 107444-51-9
GLP-1 (7-36) amide is a peptide hormone released from intestinal L-cells upon nutrient consumption. It binds the GLP-1 receptor in the pancreas and displays var...
SGC2085 HCl
T4013CAS 1821908-49-9
SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) Inhibitor with an IC50 of 50 nM and more than undred-fold selectiv...
UNC3866
T4021CAS 1872382-47-2
UNC3866 is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen.
UNC-0642
T4166CAS 1481677-78-4
UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM).
EPZ020411
T4314CAS 1700663-41-7
EPZ020411 is a specific and effective inhibitor of PRMT6 (IC50=10 nM).
EPZ020411 2HCl (1700663-41-7(free base))
T4334CAS T4334
EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).
A-196
T4343CAS 1982372-88-2
A-196 is a potent and selective inhibitor of SUV420 h1 and SUV420 h2 with IC50 values of 0.025 and 0.144 μM, respectively; more than 100-fold selective over ot...
MS049
T4378CAS 1502816-23-0
MS 049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC 50 of 34 nM and 43 nM, respectively.
MS049 2HCl (1502816-23-0(free base))
T4393CAS T4393
MS049 is a potent and selective inhibitor of PRMT4 (IC50 = 34 nM) and PRMT6 (IC50 = 43 nM). It is less active against additional type I PRMTs (IC50s = >130, >22...
(R)-PFI-2 hydrochloride
T4583CAS 1627607-87-7
PFI-2 hydrochloride is a potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 (IC50: 2 nM), 500 fold active than (S)-P...
BCI-121
T5322CAS 432529-82-3
BCI-121 is a substrate-competitive SMYD3 inhibitor that inhibits the proliferation of the cancer cell.
EZM 2302
T5605CAS 1628830-21-6
EZM2302 is a selective, and orally available arginine methyltransferase CARM1 inhibitor (IC50: 6 nM).
GSK3326595
T5745CAS 1616392-22-3
GSK3326595 is an inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50:6.2 nM.).
GSK343
T6059CAS 1346704-33-3
GSK343,a specific and effective EZH2 inhibitor (IC50=4 nM), exhibits 60 fold specificity activity against EZH1, and >1000 fold specificity activity against ot...
EPZ015666
T6076CAS 1616391-65-1
EPZ015666 is an orally available inhibitor of PRMT5 enzymatic activity.
EI1
T6484CAS 1418308-27-6
EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
BMS-911543
T6790CAS 1271022-90-2
BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2.
CPI-169
T6809CAS 1450655-76-1
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.
GSK591
T6853CAS 1616391-87-7
GSK591,Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM).
HLCL-61 hydrochloride
T6857CAS 1158279-20-9
HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.
Liraglutide
T6876CAS 204656-20-2
Liraglutide is a long-acting GLP-1 receptor agonist.
LLY-507
T6879CAS 1793053-37-8
LLY-507 is an effective, cell-active, and specific inhibitor of protein-lysine Methyltransferase SMYD2.
MS023
T6900CAS 1831110-54-3
MS023 is a potent, selective, and cell-active Type I PRMT inhibitor with IC50 of 30 nM, 119 nM, 83 nM, 4 nM, and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6 and PRMT8, ...
SGC2085
T7089CAS 1821908-48-8
SGC2085 is an effective and selective coactivator-associated arginine methyltransferase 1 (CARM1) inhibitor (IC50: 50 nM).
XY1
T7157CAS 1624117-53-8
XY1 is a very close analogue of SGC707 (a potent, selective, and non-competitive inhibitor of PRMT3 with IC50 of 31 nM), It is intended to be used as a negative...
JQEZ5
T7305CAS 1913252-04-6
JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 nM).
BRD9539
T7378CAS 1374601-41-8
BRD9539 is an inhibitor of euchromatin histone methyltransferase 2 (EHMT2), also known as G9a, with an IC50 value of 6.3 μM
BAY-598
T7403CAS 1906919-67-2
BAY-598 is a selective inhibitor of SMYD2 with IC50 values of 27 nM.
BIX-01294
T7697CAS 935693-62-2
BIX-01294 is an G9a Histone Methyltransferase inhibitor(IC50 : 1.9 μM).
Gambogenic acid
T8201CAS 173932-75-7
Gambogenic acid is a natural product,is an effective inhibitor of EZH2,with anticancer activity. 
CPI-1205
T8510CAS 1621862-70-1
CPI-1205 is a highly potent and selective inhibitor of EZH2(IC50 : 0.002 μM, EC50 : 0.032 μM) .
Tanshindiol B
TN5096CAS 97465-70-8
Tanshindiol B possesses a unique anti-cancer activity whose mechanism involves the inhibition of EZH2 activity and would provide chemically valuable information...
Tanshindiol C
TN5097CAS 97465-71-9
Tanshindiol C protects macrophages from oxLDL induced foam cell formation via activation of Prdx1/ABCA1 signaling and that Prdx1 may be a novel target for thera...
MI-463
TQ0058CAS 1628317-18-9
MI-463 is a potent and orally bioavailable inhibitor of the menin-mLL interaction (IC50: 15.3 nM).
MI-503
TQ0069CAS 1857417-13-0
MI-503 is a highly effective and orally bioavailable inhibitor of the menin-mLL interaction.
AZ505
TQ0100CAS 1035227-43-0
AZ505 is an effective and specific SMYD2 inhibitor (IC50: 0.12 μM).
UNC 0646
TQ0232CAS 1320288-17-2
UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases, G9a and GLP (IC50s: 6 nM/15 nM for G9a/GLP). UNC0646 potently b...
EPZ031686
TQ0263CAS 1808011-22-4
EPZ031686 is a selective and orally available SMYD3 inhibitor (IC50: 3 nM).