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Results for "

EZH

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (10) Autophagy (2) E1/E2/E3 Enzyme (1) Epigenetic Reader Domain (2) Fluorescent Dye (1) HDAC (1) HIF/HIF Prolyl-Hydroxylase (1) Histone Methyltransferase (69) HSP (1) Keap1-Nrf2 (1) Ligands for Target Protein for PROTAC (1) Orthopoxvirus (3) PARP (2) PROTAC Linkers (1) PROTACs (7) Sirtuin (1) Small Interfering RNA (siRNA) (5) Wnt (1)
By Research Areas:	Cancer (75) Cardiovascular Disease (1) Infection (3) Inflammation/Immunology (2)

Inhibitors & Agonists

Fluorescent Dye

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Antibodies

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-148458

EZH2-IN-14	Histone Methyltransferase	Cancer
EZH2-IN-14 is a selective *EZH2* (Histone Methyltransferase) inhibitor with an IC₅₀ of 12 nM. EZH2-IN-14 inhibits the methyltransferase activity of EZH2/PRC2 (that is, reducing H3K27me3). EZH2-IN-14 shows >200-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 .

HY-147230

EZH2-IN-13	Histone Methyltransferase	Cancer
EZH2-IN-13 is a potent *EZH2* inhibitor, for details please refer to compound 73 in patent WO2017139404. EZH2-IN-13 can be used to study cancers or precancerous lesions associated with EZH2 activity .

HY-149463

EZH2-IN-16	Histone Methyltransferase	Cancer
EZH2-IN-16 (Compound 24) is an inhibitor for histone methyltransferase (EZH2). EZH2-IN-16 inhibits EZH2 and EZH2 Y641F, with IC₅₀ of 37.6 and 79.1 nM. EZH2-IN-16 inhibits proliferation of WSU-DLCL2, with GI₅₀ of 0.2 μM .

HY-122595

EZH2-IN-1	Histone Methyltransferase	Cancer
EZH2-IN-1 (compound 3) is a selective and SAM-competitive *EZH2* and *EZH1* inhibitor with an IC₅₀s of 32 nM, 197 nM and 213 nM for EZH2wt, EZH2 Y641N mutant and EZH1, respectively. EZH2-IN-1 reduces bulk H3K27me3 and H3K27me2 levels. EZH2-IN-1 has the potential for diffuse large B cell lymphoma research .

HY-144330

EZH2-IN-12	Histone Methyltransferase	Cancer
EZH2-IN-12 (Compound 5) is a potent inhibitor of *EZH2. EZH*2-IN-12 has the potential for the research of central nervous system malignancies .

HY-A0298

EZH2-IN-2	Histone Methyltransferase	Cancer
EZH2-IN-2 is a *EZH2* inhibitor extracted from patent WO2018133795A1, Compound Example 69, with an IC₅₀ of 64 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity .

HY-139150

EZH2-IN-4	Histone Methyltransferase	Cancer
EZH2-IN-4 is an orally active, potent *EZH2* inhibitor with IC₅₀s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity .

HY-161419

EZH2-IN-18	Histone Methyltransferase	Cancer
EZH2-IN-18 (compound 9e) is a potent inhibitor of enhancer of zeste homologue 2 (EZH2 ^WT) with the IC₅₀ of 1.01 nM. EZH2-IN-18 shows inhibition in proliferation and induction in apoptosis in tumor cells .

HY-141566

EZH2-IN-5

Histone Methyltransferase Cancer

EZH2-IN-5 is a potent EZH2 inhibitor with IC₅₀ values of 1.52 nM and 4.07 nM for wild-type and mutant Tyr641 EZH2, respectively .
HY-153191

EZH2-IN-15

Histone Methyltransferase Cancer

EZH2-IN-15 is a EZH2 inhibitor. EZH2-IN-15 has anti-tumor activity, and can be used for research of H3K27me3-dependent tumors .

EZH2-IN-5	Histone Methyltransferase	Cancer
EZH2-IN-5 is a potent *EZH2* inhibitor with IC₅₀ values of 1.52 nM and 4.07 nM for wild-type and mutant Tyr641 EZH2, respectively .

EZH2-IN-15	Histone Methyltransferase	Cancer
EZH2-IN-15 is a *EZH2* inhibitor. EZH2-IN-15 has anti-tumor activity, and can be used for research of H3K27me3-dependent tumors .

HY-144096

EZH2-IN-11	Histone Methyltransferase	Cancer
EZH2-IN-11 is a potent inhibitor of E2HZ. The oncogenic activities of EZH2 have been shown by a number of studies in various different cancer types. EZH2-IN-11 has the potential for the research of cancer diseases (extracted from patent WO2019204490A1, compound 17) .

HY-149726

EZH2-IN-17	Histone Methyltransferase	Cancer
EZH2-IN-17 (compound 28) is a potent and orally active *EZH2* inhibitor with an IC₅₀ value of 0.95 nM. EZH2-IN-17 exhibits high anti-proliferation activity against different lymphoma cell lines including WSU-DLCL2, Pfeiffer and Karpas-422 (IC50 values of 2.36 nM, 1.73 nM, and 1.82 nM, respectively) .

HY-144094

EZH2-IN-9	Histone Methyltransferase	Cancer
EZH2-IN-9 is a potent inhibitor of *EZH2. EZH2 overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) all lead to abnormal elevation of H3K27me3 and promote the growth and development of many types of tumors, such as breast cancer, prostate cancer, leukemia, etc. EZH*2-IN-9 has the potential for the research of cancer diseases (extracted from patent WO2021180235A1, compound 17) .

HY-143616

EZH2-IN-7	Histone Methyltransferase	Cancer
EZH2-IN-7 is a potent inhibitor of *EZH2. EZH2 overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) all lead to abnormal elevation of H3K27me3 and promote the growth and development of many types of tumors, such as breast cancer, prostate cancer, leukemia, etc. EZH*2-IN-7 has the potential for the research of cancer diseases (extracted from patent WO2021129629A1, compound 259) .

HY-163288

EZH2/HSP90-IN-29	Histone Methyltransferase HSP Apoptosis	Cancer
EZH2/HSP90-IN-29 is a dual inhibitor for *EZH2* and HSP90, with IC₅₀s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively. EZH2/HSP90-IN-29 increases apoptosis/necrosis-related gene expression, induces cell cycle arrest at M phase and inhibits reactive oxygen species (ROS) catabolism pathway. EZH2/HSP90-IN-29 is able to cross the blood-brain-barrier (BBB) .

HY-D2274

EZH2-AF647

Fluorescent Dye Others

EZH2-AF647 is a fluorescent probe derived from UNC2239 that improves receptor TR-FRET properties by using Alexa 647 dye .

EZH2-AF647	Fluorescent Dye	Others
EZH2-AF647 is a fluorescent probe derived from UNC2239 that improves receptor TR-FRET properties by using Alexa 647 dye .

HY-RS04616

EZH1 Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
EZH1 Human Pre-designed siRNA Set A contains three designed siRNAs for EZH1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

EZH1 Human Pre-designed siRNA Set A EZH1 Human Pre-designed siRNA Set A

HY-RS04618

Ezh1 Rat Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Ezh1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Ezh1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Ezh1 Rat Pre-designed siRNA Set A Ezh1 Rat Pre-designed siRNA Set A

HY-RS04619

EZH2 Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
EZH2 Human Pre-designed siRNA Set A contains three designed siRNAs for EZH2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

EZH2 Human Pre-designed siRNA Set A EZH2 Human Pre-designed siRNA Set A

HY-RS04620

Ezh2 Mouse Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Ezh2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Ezh2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Ezh2 Mouse Pre-designed siRNA Set A Ezh2 Mouse Pre-designed siRNA Set A

HY-RS04621

Ezh2 Rat Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Ezh2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Ezh2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Ezh2 Rat Pre-designed siRNA Set A Ezh2 Rat Pre-designed siRNA Set A

HY-P2266

*SAH-EZH2*	Histone Methyltransferase	Cancer
SAH-EZH2, a stable EZH2 α-helical peptide, is an EZH2/EED interaction inhibitor. SAH-EZH2 targets native embryonic ectoderm development (EED), disturbs its interactions with EZH1 and EZH2, and selectively decreases trimethylation of H3K27 .

HY-156292

*IHMT-EZH2-426*	Histone Methyltransferase	Cancer
IHMT-EZH2-426 (compound 38) is a potent and covalent *EZH2* degrader with IC₅₀s of 1.3 nM, 1.2 nM, and 1.7-3.5 nM against EZH2 wild-type, EZH2-A687V, and EZH2-Y641F/Y641N/Y641S, respectively. IHMT-EZH2-426 exhibits potent antiproliferation effects against both B-cell lymphoma and triple negative breast cancer (TNBC) cell lines by reducing the levels of H3K27me3 and EZH2 .

HY-147525

*PROTAC EZH2 Degrader-1* 1 Publications Verification	PROTACs Histone Methyltransferase	Cancer
PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC₅₀ of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes .

HY-161083

*PARP/EZH2-IN-2*	PARP Histone Methyltransferase	Cancer
PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and *EZH2* inhibitor, with IC₅₀ values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy .

HY-157164

*PROTAC EZH2 Degrader-2*	PROTACs Histone Methyltransferase	Cancer
PROTAC EZH2 Degrader-2 (compound E-3P-MDM2), an EZH2 inhibitor, is a PROTAC composed of Tazemetostat (EPZ6438) and an E3 ligase system ligand. PROTAC EZH2 Degrader-2 degrades EZH2 in SU-DHL-6 cells in a dose-dependent manner, inhibits the expression of H3K27me3, and simultaneously degrades EED and SUZ12 proteins without affecting their mRNA levels. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity .

HY-132885

*PARP/EZH2-IN-1*	PARP Histone Methyltransferase	Cancer
PARP/EZH2-IN-1 is a first-in-class dual PARP (IC₅₀ 6.87 nM) and *EZH2* (IC₅₀ 36.51 nM) inhibitor for triple-negative breast cancer with wild-type BRCA.

HY-145602

Tulmimetostat CPI-0209	Histone Methyltransferase	Cancer
Tulmimetostat (CPI-0209) is an orally active *EZH1/EZH2* inhibitor that targets and inhibits the *EZH2* enzyme.Tulmimetostat has antitumor activity and is used in a variety of solid tumor studies .

HY-148333

MS177	PROTACs Histone Methyltransferase Apoptosis	Cancer
MS177 is an effective and fast-acting *EZH2* degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC₅₀): 12 nM). MS177 effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest .

HY-N5024

Gambogenic acid 1 Publications Verification	Histone Methyltransferase	Cancer
Gambogenic acid is an active ingredient that can be isolated from gamboge. Gambogenic acid acts as an effective inhibitor of *EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH*2 ubiquitination. Gambogenic acid can be used for the research of cancer .

HY-15573

EI1 KB-145943	Histone Methyltransferase Apoptosis	Cancer
EI1 (KB-145943) is a potent and selective EZH2* inhibitor* with IC₅₀ of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.

HY-144881

(S)-HH2853	Histone Methyltransferase	Inflammation/Immunology Cancer
(S)-HH2853 (compound 200), a PYRIDINO five membered aromatic ring compound, is a potent *EZH1/2* dual inhibitor with an IC₅₀ of <100 nM for EZH2_Y641F. (S)-HH2853 has the potential to be used in the research of anti-tumor or autoimmune diseases .

HY-101508

GNA002	Histone Methyltransferase	Cancer
GNA002 is a highly potent, specific and covalent *EZH2* (Enhancer of zeste homolog 2) inhibitor with an IC₅₀ of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes .

HY-15646

UNC1999 5+ Cited Publications	Histone Methyltransferase Autophagy	Cancer
UNC1999 is a SAM-competitive, potent and selective inhibitor of *EZH2/1* with IC₅₀s of <10 nM and 45 nM, repectively.

HY-144882

(R)-HH2853	Histone Methyltransferase	Inflammation/Immunology Cancer
(R)-HH2853 is a mutant EZH2 inhibitor with an IC₅₀ of <100 nM for *EZH2-Y641F*. (R)-HH2853 can be used for cancer and autoimmune diseases (WO2018045971A1; compound 201) .

HY-154854

BBDDL2059	Histone Methyltransferase	Cancer
BBDDL2059 is a selective covalent inhibitor of histone methyltransferase EZH2 with an IC₅₀ of 1.5 nM for EZH2-Y641F. BBDDL2059 inhibits lymphoma cell growth at nanomolar concentrations and can be used for anticancer research .

HY-136188

UNC2399

Histone Methyltransferase Cancer

UNC2399, a biotinylated UNC1999, is a selective EZH2 inhibitor, maintaining high in vitro potency for EZH2, with an IC₅₀ of 17 nM .

UNC2399	Histone Methyltransferase	Cancer
UNC2399, a biotinylated UNC1999, is a selective *EZH2* inhibitor, maintaining high in vitro potency for EZH2, with an IC₅₀ of 17 nM .

HY-13803

Tazemetostat 50+ Cited Publications EPZ-6438; E-7438	Histone Methyltransferase Apoptosis	Cancer
Tazemetostat (EPZ-6438) is a potent, selective and orally available *EZH2* inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a K_i value of 2.5 nM. Tazemetostat inhibits EZH2 with IC₅₀s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC₅₀ of 4 nM. Tazemetostat also inhibits EZH1 with an IC₅₀ of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells .

HY-147091

Tazemetostat de(methyl morpholine)-COOH	Ligands for Target Protein for PROTAC	Cancer
Tazemetostat de(methyl morpholine)-COOH (compound 7) is a ligand for the PROTAC target protein *EZH2, which can be used to synthesis of EZH2* degraders (PROTACs). *EZH2* degraders have potent cell viability inhibition in diffuse large B-cell lymphoma (DLBCL) and other subtypes of lymphoma .

HY-13803R

Tazemetostat (Standard)	Histone Methyltransferase Apoptosis	Cancer
Tazemetostat (Standard) is the analytical standard of Tazemetostat. This product is intended for research and analytical applications. Tazemetostat (EPZ-6438) is a potent, selective and orally available *EZH2* inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a K_i value of 2.5 nM. Tazemetostat inhibits EZH2 with IC₅₀s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC₅₀ of 4 nM. Tazemetostat also inhibits EZH1 with an IC₅₀ of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells .

HY-15555

EPZ005687 5 Publications Verification	Histone Methyltransferase	Cancer
EPZ005687 is a potent and selective inhibitor of *EZH2* with K_i of 24 nM, and has 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.

HY-109108

Valemetostat 1 Publications Verification DS-3201	Histone Methyltransferase	Cancer
Valemetostat (DS-3201), a first-in-class *EZH1/2* dual inhibitor with IC₅₀ values ＜10 nM. Valemetostat can be used for the research of relapsed/refractory peripheral T-cell lymphoma .

HY-109108A

Valemetostat tosylate 1 Publications Verification DS-3201 tosylate	Histone Methyltransferase	Cancer
Valemetostat (DS-3201) tosylate, a first-in-class *EZH1/2* dual inhibitor with IC₅₀ values ＜10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma .

HY-101512

A-395	Histone Methyltransferase	Cancer
A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC₅₀ of 18 nM .

HY-134899

CPI-1328

Histone Methyltransferase Cancer

CPI-1328 is an EZH2 inhibitor with a K_i value of 63 fM.

CPI-1328	Histone Methyltransferase	Cancer
CPI-1328 is an *EZH2* inhibitor with a K_i value of 63 fM.

HY-101571A

PF-06821497	Epigenetic Reader Domain Histone Methyltransferase	Cancer
PF-06821497 (compound 23a) is a potent, selective and orally active Enhancer of Zeste Homolog 2 (EZH2) inhibitor, with a K_i value <0.1 nM against mutant Y641N EZH2. Exhibits robust tumor growth inhibition .

HY-148334

MS8815	PROTACs Histone Methyltransferase	Cancer
MS8815 is a selective enhancer of zeste homolog 2 (EZH2) PROTAC degrader. MS8815 has inhibition activity for EZH2 with an IC₅₀ value of 8.6 nM. MS8815 can be used for the research of triple-negative breast cancer (TNBC) .

HY-13500

GSK343

20+ Cited Publications

Histone Methyltransferase Autophagy Cancer

GSK343 is a highly potent and selective EZH2 inhibitor with an IC₅₀ of 4 nM.
HY-156615

Igermetostat

Histone Methyltransferase Cancer

Igermetostat is EZH2 inhibitor, used in cancer research in vivo and in vitro .

HY-103682

PF-06726304 1 Publications Verification	Histone Methyltransferase	Cancer
PF-06726304 is a potent and selective *EZH2* inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 with K_is of 0.7 and 3.0 nM, respectively. PF-06726304 displays robust antitumor growth activity .

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