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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.
カタログ番号 製品名
T12939 SMYD2-IN-1 SMYD2-IN-1 is an inhibitor of SMYD2 (IC50 of 4.45 nM).
T11436 GNA002 GNA002 is a highly potent, specific, and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor (IC50: 1.1 μM).
T22325 EPZ020411 hydrochloride EPZ020411 hydrochloride is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 10 nM.
T11084 Dot1L-IN-5 Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein ( DOT1L ) inhibitor with an IC 50 SPA DOT1L of 0.17 nM [1].
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 therap...
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...
T10427 AZ505 ditrifluoroacetate AZ505 ditrifluoroacetate is an effective and selective SMYD2 inhibitor (IC50: 0.12 μM).
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...
T11185 EML741 EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barri...
T11082 Dot1L-IN-2 Dot1l-in-2 is an effective, selective and oral bioutilization inhibitor of histone methyltransferase Dot1L, with IC50 and Ki of 0.4 nM and 0.08 nM, respectively....
T10882 CPUY074020 CPUY074020 is a potent and orally bioavailable inhibitor of histone methyltransferase G9a (IC50: 2.18 μM) with anti-proliferative activity.
T4334 EPZ020411 2HCl (1700663-41-7(free base)) EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).
T22342 GSK3368715 3HCl GSK3368715, a potent inhibitor of type I protein arginine methyltransferases (PRMT), could inhibit PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 ...
T13279 Valemetostat tosylate Valemetostat tosylate is a dual inhibitor of EZH1/2 and used in the research of relapsed/refractory peripheral T-cell lymphoma.
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.
T11500 GSK3368715 GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: ...
T2354 UNC 0631 UNC0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).
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 ...
T11500L GSK3368715 dihydrochloride GSK3368715 dihydrochloride is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) in...
T12541 PRMT5-IN-1 PRMT5-IN-1 is a covalent inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50 of 11 nM for PRMT5/MEP50).
T12428 PF-06726304 acetate PF-06726304 acetate is a selective inhibitor of EZH2, with robust antitumor growth activity.
T16577 PRMT5-IN-2 PRMT5-IN-2 is an inhibitor of protein arginine methyltransferase 5.
T15240 Tazemetostat trihydrochloride Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing ...
T9700 EZH2-IN-2 EZH2-IN-2 is a EZH2 inhibitor with an IC50 of 64 nM (Patent WO2018133795A1, Compound Example 69).
T3081L EPZ004777 hydrochloride EPZ004777 hydrochloride is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
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.
T11083 Dot1L-IN-4 Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.11 nM.
T12940 SMYD3-IN-1 SMYD3-IN-1 is an irreversible and selective SMYD3 (SET and MYND domain containing 3) inhibitor(IC50 of 11.7 nM).
T11081 Dot1L-IN-1 The Ki value of DOT1L-in-1 is 2pm.It is a highly effective, selective and novel Dot1L inhibitor.
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.
T13954 UNC6852 UNC6852 contains an EED ligand (IC50 = 247 nM) and a von Hippel-Lindau ligand and is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC.
T10840L CM-579 CM-579 is a dual inhibitor of G9a and DNMT( IC50:16 nM, 32 nM for G9a and DNMT). It has potent in vitro cellular activity in a wide range of cancer cells.
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...
T40254 MRTX-1719 MRTX-1719 is a potent, first-in-class, selective inhibitor of the PRMT5/MTA complex, with an IC50 of less than 10 nM in PRMT5/MTA MTAP DEL SDMA cells.
T9584 UNC6934 UNC6934 is a chemical probe targeting the N-terminal PWWP (PWWP1) domain of NSD2.
T28036 MI-2-2 MI-2-2 is an inhibitor of bivalent protein-protein interaction between menin and MLL with an IC50 of 46 nM. MI-2-2 binds to menin with Kd of 22 nM.
T2643 MI-3 MI-3 (Menin-MLL Inhibitor) is an effective inhibitor of Menin-MLL interaction (IC50: 648 nM).
T29231 ZLD1039 ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic acti...
T9742 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.
T9969 EZM0414 EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 ( IC 50 =18 nM in SETD2 biochemical assay; IC 50 =34 nM in cellular assay). EZM0414 can be...
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...
T60002 Ethyl 2-amino-4-methyl-5-[(3-nitrophenyl)carbamoyl]thiophene-3-carboxylate Ethyl 2-amino-4-methyl-5-[(3-nitrophenyl)carbamoyl]thiophene-3-carboxylate is a selective inhibitor of histone methyltransferase SETD7 (IC50 = 4.59 μM) with anti...
T10682L CARM1-IN-1 CARM1-IN-1 is a selective inhibitor of CARM1 with IC50 of 8.6 μM. CARM1-IN-1 shows weak activity against PRMT1 and SET7 with IC50 > 600 μM.
T7305 JQEZ5 JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 nM).
T9399 Menin-MLL inhibitor 20 Menin-MLL inhibitor 20 is an irreversible inhibitor of menin-MLL interaction with antitumor activities (WO2020142557A1, compound 6).
T5484 GSK467 GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM).
TQ0232 UNC0646 UNC 0646 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...
T0174 Cyproheptadine hydrochloride sesquihydrate Cyproheptadine hydrochloride sesquihydrate, an antihistamine, is an antagonist of serotonin and histamine2.
T21826 TC-E 5003 TC-E 5003 is a selective inhibitor of PRMT1 with IC50 of 1.5 μM.
T5745 GSK3326595 GSK3326595 is an inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50:6.2 nM.).
SMYD2-IN-1
T12939
SMYD2-IN-1 is an inhibitor of SMYD2 (IC50 of 4.45 nM).
GNA002
T11436
GNA002 is a highly potent, specific, and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor (IC50: 1.1 μM).
EPZ020411 hydrochloride
T22325
EPZ020411 hydrochloride is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 10 nM.
Dot1L-IN-5
T11084
Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein ( DOT1L ) inhibitor with an IC 50 SPA DOT1L of 0.17 nM [1].
Tanshindiol C
TN5097
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 therap...
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...
AZ505 ditrifluoroacetate
T10427
AZ505 ditrifluoroacetate is an effective and selective SMYD2 inhibitor (IC50: 0.12 μM).
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...
EML741
T11185
EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barr...
Dot1L-IN-2
T11082
Dot1l-in-2 is an effective, selective and oral bioutilization inhibitor of histone methyltransferase Dot1L, with IC50 and Ki of 0.4 nM and 0.08 nM, respectively....
CPUY074020
T10882
CPUY074020 is a potent and orally bioavailable inhibitor of histone methyltransferase G9a (IC50: 2.18 μM) with anti-proliferative activity.
EPZ020411 2HCl (1700663-41-7(free base))
T4334
EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).
GSK3368715 3HCl
T22342
GSK3368715, a potent inhibitor of type I protein arginine methyltransferases (PRMT), could inhibit PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 ...
Valemetostat tosylate
T13279
Valemetostat tosylate is a dual inhibitor of EZH1/2 and used in the research of relapsed/refractory peripheral T-cell lymphoma.
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.
GSK3368715
T11500
GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: ...
UNC 0631
T2354
UNC0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).
Tanshindiol B
TN5096
Tanshindiol B possesses a unique anti-cancer activity whose mechanism involves the inhibition of EZH2 activity and would provide chemically valuable information ...
GSK3368715 dihydrochloride
T11500L
GSK3368715 dihydrochloride is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) in...
PRMT5-IN-1
T12541
PRMT5-IN-1 is a covalent inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50 of 11 nM for PRMT5/MEP50).
PF-06726304 acetate
T12428
PF-06726304 acetate is a selective inhibitor of EZH2, with robust antitumor growth activity.
PRMT5-IN-2
T16577
PRMT5-IN-2 is an inhibitor of protein arginine methyltransferase 5.
Tazemetostat trihydrochloride
T15240
Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing ...
EZH2-IN-2
T9700
EZH2-IN-2 is a EZH2 inhibitor with an IC50 of 64 nM (Patent WO2018133795A1, Compound Example 69).
EPZ004777 hydrochloride
T3081L
EPZ004777 hydrochloride is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
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.
Dot1L-IN-4
T11083
Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.11 nM.
SMYD3-IN-1
T12940
SMYD3-IN-1 is an irreversible and selective SMYD3 (SET and MYND domain containing 3) inhibitor(IC50 of 11.7 nM).
Dot1L-IN-1
T11081
The Ki value of DOT1L-in-1 is 2pm.It is a highly effective, selective and novel Dot1L inhibitor.
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.
UNC6852
T13954
UNC6852 contains an EED ligand (IC50 = 247 nM) and a von Hippel-Lindau ligand and is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC.
CM-579
T10840L
CM-579 is a dual inhibitor of G9a and DNMT( IC50:16 nM, 32 nM for G9a and DNMT). It has potent in vitro cellular activity in a wide range of cancer cells.
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...
MRTX-1719
T40254
MRTX-1719 is a potent, first-in-class, selective inhibitor of the PRMT5/MTA complex, with an IC50 of less than 10 nM in PRMT5/MTA MTAP DEL SDMA cells.
UNC6934
T9584
UNC6934 is a chemical probe targeting the N-terminal PWWP (PWWP1) domain of NSD2.
MI-2-2
T28036
MI-2-2 is an inhibitor of bivalent protein-protein interaction between menin and MLL with an IC50 of 46 nM. MI-2-2 binds to menin with Kd of 22 nM.
MI-3
T2643
MI-3 (Menin-MLL Inhibitor) is an effective inhibitor of Menin-MLL interaction (IC50: 648 nM).
ZLD1039
T29231
ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic acti...
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.
EZM0414
T9969
EZM0414 is a potent, selective, orally bioavailable inhibitor of SETD2 ( IC 50 =18 nM in SETD2 biochemical assay; IC 50 =34 nM in cellular assay). EZM0414 can be...
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...
Ethyl 2-amino-4-methyl-5-[(3-nitrophenyl)carbamoyl]thiophene-3-carboxylate
T60002
Ethyl 2-amino-4-methyl-5-[(3-nitrophenyl)carbamoyl]thiophene-3-carboxylate is a selective inhibitor of histone methyltransferase SETD7 (IC50 = 4.59 μM) with ant...
CARM1-IN-1
T10682L
CARM1-IN-1 is a selective inhibitor of CARM1 with IC50 of 8.6 μM. CARM1-IN-1 shows weak activity against PRMT1 and SET7 with IC50 > 600 μM.
JQEZ5
T7305
JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 nM).
Menin-MLL inhibitor 20
T9399
Menin-MLL inhibitor 20 is an irreversible inhibitor of menin-MLL interaction with antitumor activities (WO2020142557A1, compound 6).
GSK467
T5484
GSK467 is a potent and selective inhibitor of KDM5 (JARID1)(Ki : 10 nM).
UNC0646
TQ0232
UNC 0646 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...
Cyproheptadine hydrochloride sesquihydrate
T0174
Cyproheptadine hydrochloride sesquihydrate, an antihistamine, is an antagonist of serotonin and histamine2.
TC-E 5003
T21826
TC-E 5003 is a selective inhibitor of PRMT1 with IC50 of 1.5 μM.
GSK3326595
T5745
GSK3326595 is an inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50:6.2 nM.).
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