|
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. |
|
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... |
|
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. |
|
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. |
|
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... |
|
T40323 |
EZH2-IN-6
|
EZH2-IN-6 |
|
|
EZH2-IN-6 is an EZH2 inhibitor with enhanced antitumor activity. |
|
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. |
|
TP2115 |
SAH-EZH2
|
|
|
|
EZH2/EPP interaction inhibitor (Kd = 320 nM). Suppresses EZH2 expression and H3K27 trimethylation by PCR2 complex. Arrests proliferation and induces monocyte to macrophage differentiation of MLL-AF9 leukemia cell line. |
|
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... |
|
T62896 |
EZH2-IN-12
|
|
|
|
EZH2-IN-12 (Compound 5) is a potent inhibitor of EZH2, which has potential for studies of CNS malignancies. |
|
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... |
|
T79780 |
IHMT-EZH2-426
|
|
Histone Methyltransferase
|
|
IHMT-EZH2-426 (compound 38) is a potent, covalent degrader of EZH2, demonstrating IC50 values of 1.3 nM for EZH2 wild-type, 1.2 nM for EZH2-A687V, and 1.7-3.5 nM for EZH2-Y641F/Y641N/Y641S mutants. The compound effective... |
|
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. |
|
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. |
|
T64208 |
EZH2-IN-9
|
|
|
|
EZH2-IN-9 is a potent inhibitor of EZH2, whose overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) cause abnormal elevations in H3K27me3 and contribute to the growth and development... |
|
T74602 |
PROTAC EZH2 Degrader-1
|
|
|
|
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]. |
|
T7305 |
JQEZ5
|
|
Histone Methyltransferase
|
|
JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 nM). |
|
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... |
|
T1775 |
GSK503
|
|
Histone Methyltransferase
|
|
GSK-503, a potent EZH2 inhibitor, has potential antitumor activity. |
|
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. |
|
T1905 |
EPZ005687
|
|
Histone Methyltransferase
|
|
EPZ005687 is a potent and selective inhibitor of EZH2. |
|
T12430 |
PF-06821497
|
|
Histone Methyltransferase
|
|
|
|
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. |
|
T3057 |
UNC1999
|
|
Histone Methyltransferase
,
Autophagy
|
|
UNC1999 is a orally bioavailable, effective and specific inhibitor of EZH2 (IC50=2 nM) and EZH1 (IC50=45). |
|
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. |
|
T15194 |
EBI-2511
|
|
Histone Methyltransferase
|
|
EBI-2511 is a highly potent and orally active inhibitor of EZH2 (IC50: 6 nM in Pfeffiera cell lines). |
|
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) . |
|
T13780 |
MS1943
|
|
Apoptosis
,
Histone Methyltransferase
|
|
MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM). |
|
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. |
|
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... |
|
T40199 |
Tulmimetostat
|
CPI-0209 |
Histone Methyltransferase
|
|
Tulmimetostat (CPI-0209) is an orally active EZH1/EZH2 inhibitor.Tulmimetostat has antitumor activity and is used in the study of ovarian cancer and advanced solid tumors. |
|
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. |
|
T10205 |
A-395
|
|
Histone Methyltransferase
|
|
A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12, IC50: 18 nM). |
|
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 ... |
|
T40038 |
UNC2399
|
UNC2399 |
|
|
UNC2399, a biotinylated version of UNC1999, functions as a selective degrader of EZH2 and exhibits strong in vitro efficacy against EZH2, demonstrated by its IC 50 value of 17 nM. |
|
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... |
|
T12428 |
PF-06726304 acetate
|
|
Histone Methyltransferase
|
|
PF-06726304 acetate is a selective inhibitor of EZH2, with robust antitumor growth activity. |
|
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. |
|
T11436 |
GNA002
|
|
Histone Methyltransferase
|
|
GNA002 is a highly potent, specific, and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor (IC50: 1.1 μM). |
|
T27069 |
CPI-169
|
CPI 169 (R),CPI-169 (R) |
|
|
CPI-169 (R) is a novel and potent inhibitor of EZH2. |
|
T79200 |
BBDDL2059
|
|
Histone Methyltransferase
|
|
BBDDL2059 is a selective covalent inhibitor targeting EZH2, exhibiting an IC50 of 1.5 nM against the EZH2-Y641F mutant. It demonstrates potency in inhibiting lymphoma cell proliferation at nanomolar concentrations, provi... |
|
T69771 |
MS-177
|
|
|
|
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... |
|
T25471 |
GSK-A
|
GSK A |
|
|
GSK-A is a Histone Lysine Methyltransferase EZH2 inhibitor. |
|
T74542 |
YM458
|
|
Histone Methyltransferase
|
|
YM458, a potent dual inhibitor of EZH2 and BRD4, exhibits IC50 values of 490 nM and 34 nM, respectively. This compound effectively hinders cell proliferation and colony formation, while also inducing cell cycle arrest an... |
|
T77940 |
Tazemetostat de(methyl morpholine)-COOH
|
|
Ligands for Target Protein for PROTAC
|
|
Tazemetostat de(methyl morpholine)-COOH (compound 7), a PROTAC ligand for EZH2, facilitates the synthesis of PROTACs that target this enzyme. These EZH2 degraders exhibit potent inhibition of cell viability in diffuse la... |
