Search Result

Results for "

EZH2 inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (16) Autophagy (3) BCL6 (1) CDK (1) Drug Metabolite (1) Epigenetic Reader Domain (1) HDAC (3) HIF/HIF Prolyl-Hydroxylase (2) Histamine Receptor (1) Histone Demethylase (1) Histone Methyltransferase (92) HSP (1) HyT (1) Keap1-Nrf2 (1) Necroptosis (1) Orthopoxvirus (4) PANoptosis (1) Parasite (1) PARP (3) Potassium Channel (1) PROTACs (10) Pyroptosis (1) Reactive Oxygen Species (ROS) (1) Reference Standards (4) S-adenosylhomocysteine hydrolase (SAHH) (3) Sirtuin (1) Wnt (1)
By Research Areas:	Cancer (93) Cardiovascular Disease (2) Infection (5) Inflammation/Immunology (8) Metabolic Disease (2) Neurological Disease (2)

By Targets:

Apoptosis (16)

Autophagy (3)

BCL6 (1)

CDK (1)

Drug Metabolite (1)

Epigenetic Reader Domain (1)

HDAC (3)

HIF/HIF Prolyl-Hydroxylase (2)

Histamine Receptor (1)

Histone Demethylase (1)

Histone Methyltransferase (92)

HSP (1)

HyT (1)

Keap1-Nrf2 (1)

Necroptosis (1)

Orthopoxvirus (4)

PANoptosis (1)

Parasite (1)

PARP (3)

Potassium Channel (1)

PROTACs (10)

Pyroptosis (1)

Reactive Oxygen Species (ROS) (1)

Reference Standards (4)

S-adenosylhomocysteine hydrolase (SAHH) (3)

Sirtuin (1)

Wnt (1)

By Research Areas:

Cancer (93)

Cardiovascular Disease (2)

Infection (5)

Inflammation/Immunology (8)

Metabolic Disease (2)

Neurological Disease (2)

Inhibitors & Agonists

Fluorescent Dyes

Biochemical Assay Reagents

Peptides

Natural
Products

GMP Molecules

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13803

Tazemetostat 85+ 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-13470

GSK126 Maximum Cited Publications 98 Publications Verification GSK2816126A	Histone Methyltransferase	Cancer
GSK126 (GSK2816126A) is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC₅₀ of 9.9 nM .

HY-10442

3-Deazaneplanocin A 30+ Cited Publications DZNep; 3-Deazaneplanocin	Histone Methyltransferase S-adenosylhomocysteine hydrolase (SAHH) Orthopoxvirus	Infection Metabolic Disease Inflammation/Immunology Cancer
3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor . 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity .

HY-13500

GSK343 30+ Cited Publications	Histone Methyltransferase Autophagy	Cancer
GSK343, a chemical probe, is a highly potent and selective *EZH2* inhibitor with an IC₅₀ of 4 nM.

HY-15646

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

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-12186

3-Deazaneplanocin A hydrochloride 30+ Cited Publications DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride	Histone Methyltransferase S-adenosylhomocysteine hydrolase (SAHH) Orthopoxvirus	Infection Inflammation/Immunology Cancer
3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor . 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor . 3-Deazaneplanocin A hydrochloride also has anti-orthopoxvirus and anti-variola activities .

HY-133129

MS1943 4 Publications Verification	HyT Histone Methyltransferase Apoptosis	Inflammation/Immunology Cancer
MS1943 is an orally active selective HyT degrader of *EZH2* that effectively reduces *EZH2* levels in cells. MS1943 has anticancer activity and exhibits cytotoxic effects in a variety of TNBC cells while sparing normal cells. In addition, MS1943 maintains high potency (IC₅₀=120 nM) in inhibiting EZH2 methyltransferase activity and is highly selective for *EZH2. (Structure Note: RED, EZH2* ligand (HY-148458); Blue, Hyt (HY-W001578)) .

HY-N5024

Gambogenic acid 2 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 EZH2 ubiquitination. Gambogenic acid can be used for the research of cancer .

HY-148333

MS177 3 Publications Verification	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-101512

A-395 4 Publications Verification	Histone Methyltransferase	Cancer
A-395, a chemical probe, 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-153191

EZH2-IN-15 1 Publications Verification	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-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-162250

MS8847	PROTACs Histone Methyltransferase	Cancer
MS8847 is a PROTAC degrader and antiproliferative agent targeting *EZH2* (DC₅₀=34.4 nM in EOL-1 MLL-rAML cells). MS8847 recruits the E3 ligase von Hippel-Lindau (VHL) to mediate the degradation of EZH2 via the ubiquitin-proteasome system. MS8847 induces antiproliferative effects in MLL-rearranged acute myeloid leukemia cells and inhibits the growth of triple-negative breast cancer cell lines or 3D triple-negative breast cancer models. MS8847 is applicable to research related to MLL-rearranged acute myeloid leukemia and triple-negative breast cancer .

HY-15573

EI1 2 Publications Verification 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-13803R

Tazemetostat (Standard) EPZ-6438 (Standard); E-7438 (Standard)	Reference Standards 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-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 .

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-A0298

EZH2-IN-2	Histone Methyltransferase	Cancer
EZH2-IN-2 (Example 69) is a *EZH2* inhibitor with an IC₅₀ and a TR-FRET IC₅₀ of 64 nM and 20 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity .

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-16986

EPZ011989 3 Publications Verification	Histone Methyltransferase	Cancer
EPZ011989 is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a K_i value of <3 nM. EPZ011989 shows robust methyl mark inhibition and anti-tumor activity. EPZ011989 can be used for the research of various cancers . EPZ011989 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-116804

ZLD1039	Histone Methyltransferase	Cancer
ZLD1039 is a potent, highly selective, and orally bioavailable *EZH2* inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC₅₀ values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis .

HY-157164

PROTAC EZH2 Degrader-2 1 Publications Verification	PROTACs Histone Methyltransferase Apoptosis	Cancer
PROTAC EZH2 Degrader-2 is a PROTAC *EZH2* inhibitor. PROTAC EZH2 Degrader-2 degrades *EZH2* in SU-DHL-6 cells in a dose-dependent manner. PROTAC EZH2 Degrader-2 induces apoptosis and reduces mitochondrial membrane potential in SU-DHL-6 cells. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity .

HY-111418

EBI-2511	Histone Methyltransferase	Cancer
EBI-2511 is a highly potent and orally active *EZH2* inhibitor, with an IC₅₀ of 6 nM in Pfeffiera cell lines, respectively.

HY-100846

JQEZ5 3 Publications Verification	Histone Methyltransferase	Cancer
JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitively inhibits polycomb repressive complex 2 (PRC2) with an IC₅₀ of 80 nM. JQEZ5 has anti-tumor effects .

HY-131246

DM-01	Histone Methyltransferase	Cancer
DM-01 is a powerful and selective *EZH2* inhibitor for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 genetically defined solid tumors .

HY-121093

DC-S239	Histone Methyltransferase	Cancer
DC-S239 is a selective histone methyltransferase SET7 inhibitor with an IC₅₀ value of 4.59 μM. DC-S239 also displays selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a. DC-S239 has anticancer activity .

HY-144330

TDI-6118	Histone Methyltransferase	Cancer
TDI-6118 (Compound 5) is a potent brain-penetrant inhibitor of *EZH2. EZH2-IN-12* has the potential for the research of central nervous system malignancies .

HY-12856

GSK503 5+ Cited Publications	Histone Methyltransferase	Cancer
GSK503 is a potent and specific inhibitor of *EZH2* methyltransferase with K_i ^app values of 3 to 27 nM.

HY-160765

WNTinib APS-8-100-2	Wnt Apoptosis	Cancer
WNTinib (APS-8-100-2) is a multi-kinase inhibitor that selectively antagonizes β-catenin (CTNNB1) mutated hepatocellular carcinoma (HCC). WNTinib downregulates oncogenicWntsignaling by inhibiting KIT/MAPK and downstream EZH2 activation .

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-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 .

HY-176165

CDK9/EZH2-IN-1	CDK Histone Methyltransferase	Cancer
CDK9/EZH2-IN-1 (Compound D16) is a *CDK9/EZH2* dual-target inhibitor (IC₅₀: 83.9/108.6 nM). CDK9/EZH2-IN-1 induces apoptosis and DNA double-strand breaks (DSBs). CDK9/EZH2-IN-1 inhibits the proliferation activity of MKN45, MDA-MB-453 and SW620 cancer cells (IC₅₀ values are 136.3, 171.3 and 315.7 nM, respectively) .

HY-162384

EPIC-0628	Histone Methyltransferase	Cancer
EPIC-0628 is an inhibitor of the *HOTAIR-EZH2* interaction and promotes ATF3 expression. The long noncoding RNA HOTAIR has been found to regulate glioblastoma (GBM) progression and mediate DNA damage repair (DDR) by interacting with the catalytic subunit EZH2 of PRC2. EPIC-0628 also inhibits the ATF3-p38-E2F1 DDR pathway to inhibit the HR pathway and upregulates CDKN1A (p21) expression, causing cell cycle arrest. EPIC-0628 also synergizes with Temozolomide (TMZ) (HY-17364) to enhance its in vivo potency .

HY-146999

YM458	Histone Methyltransferase Epigenetic Reader Domain Apoptosis	Cancer
YM458 is a potent *EZH2* and BRD4 dual inhibitor with IC₅₀s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer .

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-161313

DYB-03	Histone Methyltransferase HIF/HIF Prolyl-Hydroxylase	Cancer
DYB-03 is an oral active *HIF-1α/EZH2* inhibitor. DYB-03 inhibits migration, invasion, and angiogenesis of lung cancer cells and HUVECs in vitro and in vivo. DYB-03 induces apoptosis in 2-ME2 ^- and GSK126 ^-resistant of A549 and H460 cells .

HY-150109A

Purinostat	HDAC	Cancer
Purinostat is a selective inhibitor of HDAC I/IIb with anti-leukemic activity. Purinostat mesylate (HY-150109), the mesylate salt of Purinostat, inhibits the survival of Ph+ leukemic cells and CD34+ leukemic cells derived from CML patients. Purinostat mesylate targets HDAC I/IIb to inhibit several important factors for leukemic stem cell (LSC) survival, including c-Myc, β-Catenin, E2f, Ezh2, Alox5, and mTOR. Purinostat mesylate increases glutamate metabolism in LSC by increasing GLS1 .

HY-W516880

Desmethylastemizole O-Demethylastemizole	Drug Metabolite Parasite Histamine Receptor Potassium Channel	Infection Cardiovascular Disease
Desmethylastemizole (O-Demethylastemizole) , a metabolite of Astemizole (HY-12532), is a β-hematin (βH) inhibitor. Desmethylastemizole has an antiplasmodium activity against P. falciparum with IC₅₀ of 0.12, 0.11 and 0.06  μM for Pf3D7, PfDd2, and PfItG strains, respectively. Desmethylastemizole is also a Histamine H1 receptor antagonist. Desmethylastemizole significantly blocks hERG K ⁺ channels and also inhibits histone-lysine N-methyltransferase EZH2 activity. Desmethylastemizole can be used for long QT syndrome and malaria research .

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-174372

EZH2-IN-23	Histone Methyltransferase	Cancer
EZH2-IN-23 (Compound 25) is an *EZH2* inhibitor that exhibits potent enzymatic inhibition of the PRC2 complex (EZH2, EED, SUZ12, AEBP2, RbAp48) with a biochemical IC₅₀ of 0.8 nM. EZH2-IN-23 inhibits H3K27 trimethylation in cellular assays, showing an IC₅₀ of 40 nM. EZH2-IN-23 displays good rat PKproperties with 100 % oral bioavailability.

HY-168131

PROTAC EZH2 Degrader-3	PROTACs Histone Methyltransferase Apoptosis	Cancer
PROTAC EZH2 Degrader-3 (compound ZJ-20) is a *EZH2* PROTAC degrader. PROTAC EZH2 Degrader-3 (5 μM, 24 h) not only potently inhibits the expression of EZH2 protein, but also had a strong inhibits effect on the expression levels of other subunits of PRC2 as well as H3k27me3 protein. PROTAC EZH2 Degrader-3 shows anti-proliferative activity and blocks the cell cycle in the G0-G1 phase and induces cell apoptosis((Blue: cereblon ligand Pomalidomide (HY-10984), Black: linker HY-W361751；Pink: EZH2 inhibitor Tazemetostat (HY-13803)) .

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-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-122936

Tanshindiol C	Histone Methyltransferase Keap1-Nrf2 Sirtuin	Cardiovascular Disease Cancer
Tanshindiol C is a S-adenosylmethionine-competitive *EZH2* (Histone Methyltransferase) inhibitor with an IC₅₀ of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research .

HY-16986B

EPZ011989 hydrochloride 3 Publications Verification	Histone Methyltransferase	Cancer
EPZ011989 hydrochloride is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor, with a K_i value of <3 nM. EPZ011989 shows anti-tumor activity. EPZ011989 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups .

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-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-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-179386

PARP1/EZH2-IN-1	PARP Histone Methyltransferase Apoptosis Pyroptosis Necroptosis Reactive Oxygen Species (ROS) PANoptosis	Cancer
PARP1/EZH2-IN-1 is a selective PARP1 and *EZH2* dual inhibitor. PARP1/EZH2-IN-1 has IC₅₀s of 28 nM, 414 nM and 74 nM for PARP1, PARP2 and *EZH2, respectively. PARP1/EZH2-IN-1* inhibits the proliferation and migration of TNBC cells (triple-negative breast Cancer cells). PARP1/EZH2-IN-1 induces PANoptosis (Apoptosis, Pyroptosis and Necroptosis), increases the level of reactive oxygen species (ROS), and activates related inflammatory pathways. PARP1/EZH2-IN-1 can be used in triple-negative breast cancer research .

Cat. No.	Product Name	Target	Research Area