|
T2079 |
GSK126
|
GSK2816126A,EZH2 inhibitor |
Histone Methyltransferase
|
|
GSK126 (GSK2816126A) is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 nM). |
|
T6484 |
EI1
|
KB-145943,Ezh2 inhibitor |
Apoptosis
,
Histone Methyltransferase
|
|
EI1 (Ezh2 inhibitor) is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively. |
|
T7305 |
JQEZ5
|
|
Histone Methyltransferase
|
|
JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 nM). |
|
T25400 |
EZH2-IN-3
|
EZH2 inhibitor 3,EZH2-inhibitor-3 |
|
|
EZH2-IN-3 is an inhibitor of EZH2 and EZH1 with selective impact on diffuse large B cell lymphoma cell growth. |
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T12428L |
PF-06726304
|
|
Histone Methyltransferase
|
|
PF-06726304 shows robust antitumor growth activity. PF-06726304 is an effective and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 (Kis: 0.7 and 3.0 nM, respectively). |
|
T1788 |
Tazemetostat
|
E-7438,EPZ6438 |
Histone Methyltransferase
|
|
Tazemetostat (EPZ6438) is a histone methyltransferase EZH2 inhibitor (IC50=11 nM) that is orally active, selective, and SAM-competitive. Tazemetostat exhibits antitumor activity and may be used for the treatment of epith... |
|
T17002 |
Tazemetostat hydrobromide
|
E-7438 hydrobromide,EPZ-6438 hydrobromide |
Histone Methyltransferase
|
|
Tazemetostat hydrobromide (E-7438 hydrobromide) is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 (Ki: 2.5 n... |
|
T9700 |
EZH2-IN-2
|
|
Histone Methyltransferase
|
|
EZH2-IN-2 is a EZH2 inhibitor with an IC50 of 64 nM. |
|
T64043 |
EZH2-IN-13
|
|
Histone Methyltransferase
|
|
EZH2-IN-13 is a potent EZH2 inhibitor with potential anticancer activity.EZH2-IN-13 may be used to study diseases associated with EZH2 activity. |
|
T2435 |
EPZ011989
|
|
Histone Methyltransferase
|
|
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 selectivity over other HMTase. |
|
T6809 |
CPI-169 racemate
|
CPI 169,CPI-169,CPI169 |
Epigenetic Reader Domain
,
Histone Methyltransferase
|
|
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. |
|
T1775 |
GSK503
|
|
Histone Methyltransferase
|
|
GSK-503, a potent EZH2 inhibitor, has potential antitumor activity. |
|
T12430 |
PF-06821497
|
|
Histone Methyltransferase
|
|
|
|
T1905 |
EPZ005687
|
|
Histone Methyltransferase
|
|
EPZ005687 is a potent and selective inhibitor of EZH2. |
|
T67883 |
EZH2-IN-15
|
SHR2554 |
Histone Methyltransferase
|
|
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 the adaptive response via regulation of Treg activity. Intrat... |
|
T73116 |
(R)-HH2853
|
|
|
|
(R)-HH2853, an EZH2 inhibitor variant, demonstrates potent inhibitory action with an IC50 of less than 100 nM specifically targeting the EZH2-Y641F mutation. This compound holds potential therapeutic applications in trea... |
|
T3057 |
UNC1999
|
|
Histone Methyltransferase
,
Autophagy
|
|
UNC1999 is a orally bioavailable, effective and specific inhibitor of EZH2 (IC50=2 nM) and EZH1 (IC50=45). |
|
T6810 |
CPI-360
|
Synonym 2,CPI 360,CPI360 |
Apoptosis
,
Histone Methyltransferase
|
|
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. |
|
T15194 |
EBI-2511
|
|
Histone Methyltransferase
|
|
EBI-2511 is a highly potent and orally active inhibitor of EZH2 (IC50: 6 nM in Pfeffiera cell lines). |
|
T6059 |
GSK343
|
|
Histone Methyltransferase
,
Autophagy
|
|
GSK343, a specific and effective EZH2 inhibitor (IC50=4 nM), exhibits 60 fold specificity activity against EZH1, and >1000 fold specificity activity against other histone methyltransferases. |
|
T60194 |
N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-4′-morpholino-[1,1′-biphenyl]-3-carboxamide
|
|
Histone Methyltransferase
|
|
N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(N-ethylcyclopropanecarboxamido)-4-methyl-4′-morpholino-[1,1′-biphenyl]-3-carboxamide is a potent and selective Enhancer of Zeste Homolog 2 (EZH2) inhibitor with I... |
|
T8510 |
CPI-1205
|
Lirametostat |
Histone Methyltransferase
|
|
CPI-1205 is a highly potent and selective inhibitor of EZH2(IC50 : 0.002 μM, EC50 : 0.032 μM) . |
|
T6360 |
3-deazaneplanocin A HCl
|
|
Others
,
Histone Methyltransferase
|
|
3-deazaneplanocin A (DZNeP)HCl, an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM. |
|
T29231 |
ZLD1039
|
ZLD-1039,ZLD 1039 |
Histone Methyltransferase
|
|
ZLD1039 is a potent, orally bioavailable EZH2 (Enhancer of Zeste Homolog 2) inhibitor with high selectivity. It demonstrates strong, concentration-dependent inhibition of both wild-type and mutant (Y641F and A677G) PRC2 ... |
|
T25471 |
GSK-A
|
GSK A |
|
|
GSK-A is a Histone Lysine Methyltransferase EZH2 inhibitor. |
|
T69771 |
MS-177
|
|
PROTACs
|
|
MS177, a potent and rapid EZH2 degrader, functions as a PROTAC comprised of a CRBN ligand, linker, and a powerful enzymatic EZH2 inhibitor C24 (C24 IC50: 12 nM). It successfully targets and depletes both canonical EZH2–P... |
|
T12428 |
PF-06726304 acetate
|
|
Histone Methyltransferase
|
|
PF-06726304 acetate is a selective inhibitor of EZH2, with robust antitumor growth activity. |
|
T62896 |
EZH2-IN-12
|
|
|
|
EZH2-IN-12 (Compound 5) is a potent inhibitor of EZH2, which has potential for studies of CNS malignancies. |
|
T74602 |
PROTAC EZH2 Degrader-1
|
|
PROTACs
|
|
PROTAC EZH2 Degrader-1 (Compound 150d), a potent inhibitor, effectively suppresses EZH2 methyltransferase activity, demonstrating an IC50 of 2.7 nM. EZH2 is crucial in various tumorigenesis and development processes [1]. |
|
T40323 |
EZH2-IN-6
|
EZH2-IN-6 |
|
|
EZH2-IN-6 is an EZH2 inhibitor with enhanced antitumor activity. |
|
T15240 |
Tazemetostat trihydrochloride
|
EPZ-6438 trihydrochloride,E-7438 trihydrochloride |
Histone Methyltransferase
|
|
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 wild-type EZH2 (Ki: 2.5 nM). It inhibits EZH2 (IC50s: 11 an... |
|
T2435L |
EPZ011989 HCl(1598383-40-4 Free base)
|
EPZ-011989 TFA,EPZ011989 TFA salt,EPZ 011989 TFA,EPZ011989 TFA |
|
|
EPZ011989 is a highly potent and selective oral EZH2 inhibitor with Ki value <3 nM. |
|
T27129 |
DCE_254
|
DCE 254,DCE-254,DCE254 |
|
|
DCE_254 is a novel EZH2 inhibitor, it also displays significant anti-proliferation activity against lymphoma cell lines. |
|
T39971 |
CPI-1328
|
|
|
|
CPI-1328 is an EZH2 inhibitor with a K i value of 63 fM. |
|
T73134 |
EZH2-IN-14
|
|
|
|
EZH2-IN-14 is a selective inhibitor of EZH2 (Histone Methyltransferase), demonstrating potent inhibition with an IC50 value of 12 nM. It specifically targets the methyltransferase activity of EZH2/PRC2, effectively reduc... |
|
T25470 |
GSK926
|
GSK 926,GSK-926 |
|
|
GSK926 is a selective, SAM-competitive, and cell-active EZH2 inhibitor. |
|
T27069 |
CPI-169
|
CPI 169 (R),CPI-169 (R) |
|
|
CPI-169 (R) is a novel and potent inhibitor of EZH2. |
|
T40310 |
PARP/EZH2-IN-1
|
PARP/EZH2-IN-1 |
|
|
PARP/EZH2-IN-1 is a novel compound that functions as a dual inhibitor for both PARP (IC50 6.87 nM) and EZH2 (IC50 36.51 nM), showing promising potential for the treatment of triple-negative breast cancer with wild-type B... |
|
T38827 |
EZH2-IN-5
|
EZH2-IN-5 |
|
|
EZH2-IN-5 is a highly effective inhibitor of EZH2, displaying remarkable potency against both wild-type and mutant Tyr641 EZH2, with IC50 values of 1.52 nM and 4.07 nM, respectively. |
|
T29232 |
ZLD10A
|
ZLD 10 A,ZLD-10-A |
|
|
ZLD10A is a highly potent and selective small molecule inhibitor of EZH2. |
|
T39497 |
EZH2-IN-4
|
EZH2-IN-4 |
|
|
EZH2-IN-4 is a highly potent EZH2 inhibitor that can be taken orally. It exhibits inhibitory effects against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, with IC 50 values of 0.923 nM and 2.65 nM, respec... |
|
T27074 |
CPI-905
|
CPI 905 |
|
|
CPI-905 is a potent and selective EZH2 inhibitor with IC50 value of 39.5 nM. |
|
T27130 |
DCE_42
|
DCE 42,DCE42,DCE-42 |
|
|
DCE_42 is a novel EZH2 inhibitor, it also displays significant anti-proliferation activity against lymphoma cell lines. |
|
T11436 |
GNA002
|
|
Histone Methyltransferase
|
|
GNA002 is a highly potent, specific, and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor (IC50: 1.1 μM). |
|
T69264 |
Aristeromycin diphosphate
|
|
|
|
Aristeromycin diphosphate is an inhibitor of S-adenosylhomocysteine hydrolase (AHCY), inducing miR-26a and regulating oncogenic EZH2 expression, showing high inhibitory activity against AHCY, and causing growth inhibitio... |
|
T73246 |
EZH2-IN-7
|
|
|
|
EZH2-IN-7, a potent inhibitor of EZH2, addresses overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) that cause an abnormal increase in H3K27me3, contributing to the proliferation o... |
|
T64307 |
EZH2-IN-8
|
|
|
|
EZH2-IN-8 is a potent inhibitor of EZH2. EZH2-IN-8 has the potential to be used in the study of cancer diseases. |
|
T70588 |
Tazemetostat HCl
|
|
|
|
Tazemetostat HCl is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. EPZ-6438 induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells. Treatment of... |
|
T63747 |
MC4355
|
|
|
|
MC4355 is a dual inhibitor of EZH2 and histone deacetylase (HDAC). |
|
T63970 |
EZH2-IN-11
|
|
|
|
EZH2-IN-11 is a potent inhibitor of E2HZ. The oncogenic activity of EZH2 has been demonstrated in numerous studies in a variety of different cancer types and EZH2-IN-11 has shown research potential for cancer diseases. |
