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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
T21826 TC-E 5003 TC-E 5003 is a selective inhibitor of PRMT1 with IC50 of 1.5 μM.
T4166 UNC0642 UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM).
T6879 LLY507 LLY-507 is an effective, cell-active, and specific inhibitor of protein-lysine Methyltransferase SMYD2.
T6810 CPI360 CPI-360 is a potent, selective, and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.
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, r...
T1868 JIB04 JIB-04 is a pan-selective Jumonji histone demethylase inhibitor.
T2352 AMI1 AMI-1 is an effective and selective Histone Methyltransferase (HMT) inhibitor (IC50: 3.0/8.8 μM, for yeast Hmt1p, and human PRMT1).
T3458 EED226 EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.
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...
T0174 Cyproheptadine hydrochloride Cyproheptadine hydrochloride sesquihydrate, an antihistamine, is an antagonist of serotonin and histamine2.
T2167 Lutidinic acid 2, 4-Pyridinedicarboxylic acid is an in vitro and in cell inhibitor, as well as a known inhibitor of the histone lysine demethylases.
T2097 C7280948 C-7280948 is a PRMT1 inhibitor.
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.
T1987 PFI2 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...
T4314 EPZ020411 EPZ020411 is a specific and effective inhibitor of PRMT6 (IC50=10 nM).
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 selectivi...
T4021 UNC3866 UNC3866 is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen.
T4343 A196 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 oth...
T4334 EPZ020411 2HCl (1700663-41-7(free base)) EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).
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, >220...
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)-PF...
T7089 SGC2085 SGC2085 is an effective and selective coactivator-associated arginine methyltransferase 1 (CARM1) inhibitor (IC50: 50 nM).
T5322 BCI121 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).
T3084 SGC707 SGC707 is a potent, selective, and cell-active allosteric inhibitor of PRMT3.
T1841 UNC0379 UNC0379 is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8.
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 negati...
T3099 Pinometostat EPZ5676 has been used in trials studying the treatment of Leukemia, Acute Leukemias, Acute Myeloid Leukemia, Myelodysplastic Syndrome, and Acute Lymphocytic Leuk...
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 e...
T6790 BMS911543 BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2.
T2643 MI3 MI-3 (Menin-MLL Inhibitor) is an effective inhibitor of Menin-MLL interaction (IC50: 648 nM).
T2649 MI2 MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.
T2354 UNC0631 UNC0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).
T3081 EPZ004777 EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
T1775 GSK503 GSK-503, a potent EZH2 inhibitor, has potential antitumor activity.
T2079 GSK126 GSK126 is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 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 othe...
T1923 BRD4770 BRD4770 is a histone methyltransferase G9a inhibitor and induces cell senescence.
T3081L EPZ004777 HCl EPZ004777 hydrochloride is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
T6853 GSK591 GSK591, Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM).
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.
T1905 EPZ005687 EPZ005687 is a potent and selective inhibitor of EZH2.
T1788 EPZ6438 Tazemetostat is an orally available, small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone methyltransferase EZH2, with poten...
T6333 MM102 MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.
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.
T3057 UNC1999 UNC1999 is a orally bioavailable, effective and specific inhibitor of EZH2 (IC50=2 nM) and EZH1 (IC50=45).
T6809 CPI169 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.
T3624 A366 Potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC50 = 3.3 nM). Exhibits >1000-fold selectivity for G9a/GLP over 21 other methyltransfe...
T3082 SGC0946 SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.
T2435 EPZ011989 EPZ011989 is a effective, specific orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 Y646 and EZH2 wt; 15-fold selectivity over EZH1 and >3000-fold sele...
T6076 EPZ015666 EPZ015666 is an orally available inhibitor of PRMT5 enzymatic activity.
T5745 GSK3326595 GSK3326595 is an inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50:6.2 nM.).
T7305 JQEZ5 JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 nM).
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 prolifera...
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 spec...
T11486 GSK2807 Trifluoroacetate GSK2807 Trifluoroacetate is a selective and SAM-competitive inhibitor of SMYD3 (Ki: 14 nM; IC50: 130 nM).
T11500L GSK3368715 dihydrochloride GSK3368715 dihydrochloride is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) i...
T11500 GSK3368715 GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s:...
T13279 Valemetostat tosylate Valemetostat tosylate is a dual inhibitor of EZH1/2 and used in the research of relapsed/refractory peripheral T-cell lymphoma.
T15624 JNJ-64619178 JNJ-64619178 is a selective, orally active, and pseudo-irreversible inhibitor of protein arginine methyltransferase 5 (IC50: 0.14 nM). It has effective activity ...
T16072 MI-538 MI-538 is an interaction between menin and MLL fusion proteins inhibitor(IC50 of 21 nM).
T10882 CPUY074020 CPUY074020 is a potent and orally bioavailable inhibitor of histone methyltransferase G9a (IC50: 2.18 μM) with anti-proliferative activity.
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 spe...
T12428L PF-06726304 PF-06726304 shows robust antitumor growth activity. PF-06726304 is an effective and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH...
T16577 PRMT5-IN-2 PRMT5-IN-2 is an inhibitor of protein arginine methyltransferase 5.
T17002 Tazemetostat hydrobromide Tazemetostat hydrobromide is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)...
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 bar...
T17203 UNC0224 UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3, and JMJD2E. UNC0224 is a potent and selective histone methyltransferase G9a inhibitor (Ki: 2.6 nM, an IC...
T17204 UNC0321 UNC0321 is inactive against SET7/9, SET8/PreSET7, PRMT3, and JMJD2E. UNC0321 is an effective and selective histone methyltransferase G9a inhibitor (Ki: 63 pM) an...
T13279L Valemetostat Valemetostat is a first-in-class EZH1/2 dual inhibitor.
T22325 EPZ020411 2HCl EPZ020411 is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 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 ...
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 therap...
T8768 MM-102 TFA MM-102 TFA is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM. MM-102 compound prevents the interaction between mixed lineage leukemia 1 (MLL1) ...
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
T8881 Dot1L-IN-4 Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor.
T4021L UNC3866 TFA(1872382-47-2 free base) UNC3866 TFA is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen.
T11436 GNA002 GNA002 is a highly potent, specific, and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor (IC50: 1.1 μM).
T11131 DW14800 DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity.DW14800 is a protein arginine...
T7378 BRD9539 BRD9539 is an inhibitor of euchromatin histone methyltransferase 2 (EHMT2), also known as G9a, with an IC50 value of 6.3 µM
T12428 PF-06726304 acetate PF-06726304 acetate is a selective inhibitor of EZH2, with robust antitumor growth activity.
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).
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 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...
TQ0263 EPZ031686 EPZ031686 is a selective and orally available SMYD3 inhibitor (IC50: 3 nM).
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) .
T13780 MS1943 MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).
T12541 PRMT5-IN-1 PRMT5-IN-1 is a covalent inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50 of 11 nM for PRMT5/MEP50).
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...
T11081 Dot1L-IN-1 The Ki value of DOT1L-in-1 is 2pm.It is a highly effective, selective and novel Dot1L inhibitor.
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....
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.
T11084 Dot1L-IN-5 Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.17 nM.
T10427 AZ505 ditrifluoroacetate AZ505 ditrifluoroacetate is an effective and selective SMYD2 inhibitor (IC50: 0.12 μM).
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.
T15080 DC-05 DC-05 is an inhibitor of DNA methyltransferase 1 (DNMT1) (IC50 and a Kd: 10.3 μM and 1.09 μM, respectively).
T15194 EBI-2511 EBI-2511 is a highly potent and orally active inhibitor of EZH2 (IC50: 6 nM in Pfeffiera cell lines).
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 ...
T12939 SMYD2-IN-1 SMYD2-IN-1 is an inhibitor of SMYD2 (IC50 of 4.45 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).
T6857 HLCL-61 hydrochloride HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.
TC-E 5003
T21826CAS 17328-16-4
TC-E 5003 is a selective inhibitor of PRMT1 with IC50 of 1.5 μM.
UNC0642
T4166CAS 1481677-78-4
UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM).
LLY507
T6879CAS 1793053-37-8
LLY-507 is an effective, cell-active, and specific inhibitor of protein-lysine Methyltransferase SMYD2.
CPI360
T6810CAS 1802175-06-9
CPI-360 is a potent, selective, and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.
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, r...
JIB04
T1868CAS 199596-05-9
JIB-04 is a pan-selective Jumonji histone demethylase inhibitor.
AMI1
T2352CAS 20324-87-2
AMI-1 is an effective and selective Histone Methyltransferase (HMT) inhibitor (IC50: 3.0/8.8 μM, for yeast Hmt1p, and human PRMT1).
EED226
T3458CAS 2083627-02-3
EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.
Chaetocin
T6803CAS 28097-03-2
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...
Cyproheptadine hydrochloride
T0174CAS 41354-29-4
Cyproheptadine hydrochloride sesquihydrate, an antihistamine, is an antagonist of serotonin and histamine2.
lutidinic acid
T2167CAS 499-80-9
2, 4-Pyridinedicarboxylic acid is an in vitro and in cell inhibitor, as well as a known inhibitor of the histone lysine demethylases.
C7280948
T2097CAS 587850-67-7
C-7280948 is a PRMT1 inhibitor.
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.
PFI2
T1987CAS 1627676-59-8
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...
EPZ020411
T4314CAS 1700663-41-7
EPZ020411 is a specific and effective inhibitor of PRMT6 (IC50=10 nM).
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 selectivi...
UNC3866
T4021CAS 1872382-47-2
UNC3866 is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen.
A196
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 oth...
EPZ020411 2HCl (1700663-41-7(free base))
T4334CAS T4334
EPZ020411 is an effective and specific small molecule PRMT6 inhibitor (IC50=10 nM).
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, >220...
(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)-PF...
SGC2085
T7089CAS 1821908-48-8
SGC2085 is an effective and selective coactivator-associated arginine methyltransferase 1 (CARM1) inhibitor (IC50: 50 nM).
BCI121
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).
SGC707
T3084CAS 1687736-54-4
SGC707 is a potent, selective, and cell-active allosteric inhibitor of PRMT3.
UNC0379
T1841CAS 1620401-82-2
UNC0379 is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8.
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 negati...
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 Leuk...
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 e...
BMS911543
T6790CAS 1271022-90-2
BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2.
MI3
T2643CAS 1271738-59-0
MI-3 (Menin-MLL Inhibitor) is an effective inhibitor of Menin-MLL interaction (IC50: 648 nM).
MI2
T2649CAS 1271738-62-5
MI-2 (Menin-MLL Inhibitor) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.
UNC0631
T2354CAS 1320288-19-4
UNC0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).
EPZ004777
T3081CAS 1338466-77-5
EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
GSK503
T1775CAS 1346572-63-1
GSK-503, a potent EZH2 inhibitor, has potential antitumor activity.
GSK126
T2079CAS 1346574-57-9
GSK126 is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 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 othe...
BRD4770
T1923CAS 1374601-40-7
BRD4770 is a histone methyltransferase G9a inhibitor and induces cell senescence.
EPZ004777 HCl
T3081LCAS 1380316-03-9
EPZ004777 hydrochloride is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.
GSK591
T6853CAS 1616391-87-7
GSK591, Alternative Names are EPZ015866, GSK3203591, is a potent selective inhibitor of the arginine methyltransferase PRMT5 (IC50=11 nM).
BIX 01294 Trihydrochloride
T1959CAS 1392399-03-9
BIX01294 is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.
EPZ005687
T1905CAS 1396772-26-1
EPZ005687 is a potent and selective inhibitor of EZH2.
EPZ6438
T1788CAS 1403254-99-8
Tazemetostat is an orally available, small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone methyltransferase EZH2, with poten...
MM102
T6333CAS 1417329-24-8
MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.
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.
UNC1999
T3057CAS 1431612-23-5
UNC1999 is a orally bioavailable, effective and specific inhibitor of EZH2 (IC50=2 nM) and EZH1 (IC50=45).
CPI169
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.
A366
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 methyltransfe...
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.
EPZ011989
T2435CAS 1598383-40-4
EPZ011989 is a effective, specific orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 Y646 and EZH2 wt; 15-fold selectivity over EZH1 and >3000-fold sele...
EPZ015666
T6076CAS 1616391-65-1
EPZ015666 is an orally available inhibitor of PRMT5 enzymatic activity.
GSK3326595
T5745CAS 1616392-22-3
GSK3326595 is an inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50:6.2 nM.).
JQEZ5
T7305CAS 1913252-04-6
JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 nM).
WM-3835
T9102CAS 2229025-70-9
WM-3835 is a novel and high-specific small molecule inhibitor of Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) , able to potently suppressed OS cell prolifera...
M‑89
T11925CAS 2363165-42-6
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 spec...
GSK2807 Trifluoroacetate
T11486CAS 2245255-66-5
GSK2807 Trifluoroacetate is a selective and SAM-competitive inhibitor of SMYD3 (Ki: 14 nM; IC50: 130 nM).
GSK3368715 dihydrochloride
T11500LCAS 1628925-77-8
GSK3368715 dihydrochloride is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) i...
GSK3368715
T11500CAS 1629013-22-4
GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s:...
Valemetostat tosylate
T13279CAS 1809336-93-3
Valemetostat tosylate is a dual inhibitor of EZH1/2 and used in the research of relapsed/refractory peripheral T-cell lymphoma.
JNJ-64619178
T15624CAS 2086772-26-9
JNJ-64619178 is a selective, orally active, and pseudo-irreversible inhibitor of protein arginine methyltransferase 5 (IC50: 0.14 nM). It has effective activity ...
MI-538
T16072CAS 1857417-10-7
MI-538 is an interaction between menin and MLL fusion proteins inhibitor(IC50 of 21 nM).
CPUY074020
T10882CAS 902279-44-1
CPUY074020 is a potent and orally bioavailable inhibitor of histone methyltransferase G9a (IC50: 2.18 μM) with anti-proliferative activity.
PBIT
T16435CAS 2514-30-9
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...
PF-06726304
T12428LCAS 1616287-82-1
PF-06726304 shows robust antitumor growth activity. PF-06726304 is an effective and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH...
PRMT5-IN-2
T16577CAS 1989620-04-3
PRMT5-IN-2 is an inhibitor of protein arginine methyltransferase 5.
Tazemetostat hydrobromide
T17002CAS 1467052-75-0
Tazemetostat hydrobromide is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)...
EML741
T11185CAS 2328074-38-8
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 bar...
UNC0224
T17203CAS 1197196-48-7
UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3, and JMJD2E. UNC0224 is a potent and selective histone methyltransferase G9a inhibitor (Ki: 2.6 nM, an IC...
UNC0321
T17204CAS 1238673-32-9
UNC0321 is inactive against SET7/9, SET8/PreSET7, PRMT3, and JMJD2E. UNC0321 is an effective and selective histone methyltransferase G9a inhibitor (Ki: 63 pM) an...
Valemetostat
T13279LCAS 1809336-39-7
Valemetostat is a first-in-class EZH1/2 dual inhibitor.
EPZ020411 2HCl
T22325CAS 2070015-25-5
EPZ020411 is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 10 nM.
GSK3368715 3HCl
T22342CAS 2227587-26-8
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 ...
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 therap...
MM-102 TFA
T8768CAS 1883545-52-5
MM-102 TFA is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM. MM-102 compound prevents the interaction between mixed lineage leukemia 1 (MLL1) ...
CCI 007
T8838CAS 939228-52-1
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
Dot1L-IN-4
T8881CAS 2565705-02-2
Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor.
UNC3866 TFA(1872382-47-2 free base)
T4021LCAS 1872382-48-3
UNC3866 TFA is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen.
GNA002
T11436CAS 1385035-79-9
GNA002 is a highly potent, specific, and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor (IC50: 1.1 μM).
DW14800
T11131CAS 2243709-60-4
DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity.DW14800 is a protein arginine...
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
PF-06726304 acetate
T12428CAS 2080306-28-9
PF-06726304 acetate is a selective inhibitor of EZH2, with robust antitumor growth activity.
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).
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
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...
EPZ031686
TQ0263CAS 1808011-22-4
EPZ031686 is a selective and orally available SMYD3 inhibitor (IC50: 3 nM).
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) .
MS1943
T13780CAS 2225938-17-8
MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).
PRMT5-IN-1
T12541CAS 2366149-83-7
PRMT5-IN-1 is a covalent inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50 of 11 nM for PRMT5/MEP50).
SNDX-5613
T12943CAS 2169919-21-3
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...
Dot1L-IN-1
T11081CAS 2088518-50-5
The Ki value of DOT1L-in-1 is 2pm.It is a highly effective, selective and novel Dot1L inhibitor.
Dot1L-IN-2
T11082CAS 1940206-71-2
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....
Dot1L-IN-4
T11083CAS 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.
Dot1L-IN-5
T11084CAS T11084
Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.17 nM.
AZ505 ditrifluoroacetate
T10427CAS 1035227-44-1
AZ505 ditrifluoroacetate is an effective and selective SMYD2 inhibitor (IC50: 0.12 μM).
CM-579
T10840LCAS 1846570-40-8
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.
DC-05
T15080CAS 890643-16-0
DC-05 is an inhibitor of DNA methyltransferase 1 (DNMT1) (IC50 and a Kd: 10.3 μM and 1.09 μM, respectively).
EBI-2511
T15194CAS 2098546-05-3
EBI-2511 is a highly potent and orally active inhibitor of EZH2 (IC50: 6 nM in Pfeffiera cell lines).
Tazemetostat trihydrochloride
T15240CAS 1403255-00-4
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 ...
SMYD2-IN-1
T12939CAS 2023788-96-5
SMYD2-IN-1 is an inhibitor of SMYD2 (IC50 of 4.45 nM).
SMYD3-IN-1
T12940CAS 2095160-79-3
SMYD3-IN-1 is an irreversible and selective SMYD3 (SET and MYND domain containing 3) inhibitor(IC50 of 11.7 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.