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EZH2-IN-2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (2) Bcl-2 Family (1) Caspase (1) Histone Demethylase (1) Histone Methyltransferase (26) IAP (1) Ligands for Target Protein for PROTAC (2) PARP (2) PROTACs (12)
By Research Areas:	Cancer (25) Inflammation/Immunology (2) Neurological Disease (2)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-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-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-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-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-122640

NPD13668	Histone Methyltransferase	Cancer
NPD13668 is an *EZH2*-mediated gene silencing modulator. NPD13668 inhibits EZH2/PRC2 (polycomb repressive complex 2) activity. NPD13668 reactivates the expression of silenced H3K27me3 target genes together with depletion of the H3K27me3 modification. NPD13668 can be used for the study of prostate cancer and ovarian cancer .

HY-178694

DC-PRC2in-01	Histone Methyltransferase	Cancer
DC-PRC2in-01 is a potent EZH2-EED interaction inhibitor with an IC₅₀ of 4.21 μM and a K_d of 4.56 μM. DC-PRC2in-01 disrupts the EZH2-EED interaction, leading to degradation of PRC2 core proteins and decrease of H3K27me3 levels, inhibition of PRC2-driven lymphoma cell proliferation, and cell cycle arrest. DC-PRC2in-01 can be used for the research of PRC2-related cancers, such as Diffuse Large B-cell Lymphoma (DLBCL) and follicular lymphoma (FL) .

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-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-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. EZH2-IN-7 has the potential for the research of cancer diseases (extracted from patent WO2021129629A1, compound 259) .

HY-181325

*PROTAC EZH2* Degrader-24**	PROTACs Histone Methyltransferase	Cancer
PROTAC EZH2 Degrader-24 (compound 9) is an *EZH2*-targeting PROTAC with *EZH2* methyltransferase inhibitory activity .

HY-181309

*PROTAC EZH2* Degrader-15**	PROTACs Histone Methyltransferase	Cancer
PROTAC EZH2 Degrader-15 (compound 5) is an *EZH2*-targeting PROTAC. PROTAC EZH2 Degrader-15 functionally inhibits *EZH2* methyltransferase activity .

HY-185582

EZH2 ligand-4	Histone Methyltransferase Ligands for Target Protein for PROTAC	Cancer
EZH2 ligand-4 (Precursor 1) is a ligand for the target protein for PROTAC (EZH2). EZH2 ligand-4 can be used to synthesize MS8847 (HY-162250) .

HY-179500

EZH2 ligand-Linker Conjugate 1	Ligands for Target Protein for PROTAC Histone Methyltransferase	Cancer
EZH2 ligand-Linker Conjugate 1 is a target protein ligand-lnker conjugate that incorporates a target protein ligand for EZH2. EZH2 ligand-Linker Conjugate 1 can be used for the synthesis of PROTAC EZH2 Degrader-9 (HY-179499) .

HY-181318

*PROTAC EZH2* Degrader-20**	PROTACs Histone Methyltransferase	Cancer
PROTAC EZH2 Degrader-20 (compound 54) is an *EZH2*-target PROTAC degrader with antiproliferative activity and IC₅₀ values of about 10 μM against lymphoma cells. PROTAC EZH2 Degrader-20 can be used for the research of lymphoma .

HY-181308

*PROTAC EZH2* Degrader-13**	PROTACs Histone Methyltransferase	Cancer
PROTAC EZH2 Degrader-13 is an *EZH2*-targeting PROTAC with an IC₅₀ of 2.70 nM. PROTAC EZH2 Degrader-13 exerts antiproliferative effects in cancer cells. PROTAC EZH2 Degrader-13 can be used for the research of cancer .

HY-181391

*PROTAC EZH2* Degrader-34**	PROTACs Histone Methyltransferase	Cancer
PROTAC EZH2 Degrader-34 (compound E7 (13)) is an *EZH2*-target PROTAC degrader with a human *EZH2* IC₅₀ of 6.30 μM. PROTAC EZH2 Degrader-34 can be used for the research of pfeiffer cancer, prostate cancer .

HY-181326

*PROTAC EZH2* Degrader-25**	PROTACs Histone Methyltransferase	Cancer
PROTAC EZH2 Degrader-25 (compound 10) is an *EZH2*-targeting PROTAC degrader. PROTAC EZH2 Degrader-25 triggers ubiquitination and subsequent proteasomal degradation of *EZH2. PROTAC EZH2* Degrader-25 can be used for the research of lymphoma .

HY-181306

*PROTAC EZH2* Degrader-11**	PROTACs Histone Methyltransferase	Cancer
PROTAC EZH2 Degrader-11 (compound 2) is a *EZH2*-targeting PROTAC protein degrader. PROTAC EZH2 Degrader-11 reduces tumor size and viability in 3D spheroid models. PROTAC EZH2 Degrader-11 can be used for the research of cancer .

HY-181411

*PROTAC EZH2* Degrader-42**	PROTACs Histone Methyltransferase	Cancer
PROTAC EZH2 Degrader-42 (compound 57) is an *EZH2*-targeting PROTAC degrader and antiproliferative agent. PROTAC EZH2 Degrader-42 induces cIAP-mediated ubiquitination and subsequent proteasomal degradation of *EZH2. PROTAC EZH2* Degrader-42 can be used for the research of lymphoma .

HY-181410

*PROTAC EZH2* Degrader-41**	PROTACs Histone Methyltransferase IAP	Cancer
PROTAC EZH2 Degrader-41 is an *EZH2*-targeting PROTAC and cIAP E3 ubiquitin ligase recruiter. PROTAC EZH2 Degrader-41 induces *EZH2* degradation via ubiquitination and proteasomal breakdown. PROTAC EZH2 Degrader-41 exerts antiproliferative effects in lymphoma cells. PROTAC EZH2 Degrader-41 can be used for the research of lymphoma .

HY-181413

*PROTAC EZH2* Degrader-44**	PROTACs Histone Methyltransferase Bcl-2 Family Caspase PARP	Cancer
PROTAC EZH2 Degrader-44 (compound 60) is a highly efficient PROTAC degrader targeting the *EZH2-*PRC2 complex. By recruiting the CRBN E3 ligase and relying on the proteasome system, PROTAC EZH2 Degrader-44 simultaneously induces the degradation of core components EZH2, SUZ12 and EED, thereby significantly reducing the levels of H3K27me3 and CARM1. PROTAC EZH2 Degrader-44 exerts antiproliferative effects through a dual mechanism: on the one hand, it triggers mitochondrial dysfunction leading to decreased membrane potential; on the other hand, it strongly promotes apoptosis by regulating Bcl-2 family proteins (upregulating Bax, Caspase-3 and PARP, and downregulating Bcl-2). PROTAC EZH2 Degrader-44 exhibits only extremely low cytotoxicity in human normal mammary epithelial, liver and kidney cells, showing a favorable safety window. PROTAC EZH2 Degrader-44 is an ideal tool molecule for exploring the mechanisms of targeted therapy for triple-negative breast cancer .

HY-182365

EED-IN-4	Histone Demethylase	Neurological Disease Inflammation/Immunology
EED-IN-4 is an orally active, *EZH2*-selective immunomodulator and EED-H3K27me3 inhibitor (EED, IC₅₀=28.21 nM) with anti-inflammatory activity. In mouse models, EED-IN-4 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-4 reduces the infiltration of immune cells into the central nervous system and effectively alleviates spinal cord inflammation. EED-IN-4 shows weak inhibitory activity against hERG channels and is non-mutagenic, with no obvious toxicity observed upon long-term oral administration. EED-IN-4 can be used for the research of multiple sclerosis .

HY-182366

EED-IN-5	Histone Methyltransferase	Neurological Disease Inflammation/Immunology
EED-IN-5 is an orally active, *EZH2*-selective trisubstituted pyridine-based EED-H3K27me3 inhibitor and immunomodulator with anti-inflammatory activity. The IC₅₀ value of EED-IN-5 against EED is 28.21 nM. In mouse models, EED-IN-5 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-5 decreases the infiltration of specific dendritic cells, macrophages and T cells into the spinal cord and brain. EED-IN-5 exhibits hERG inhibitory activity, shows negative results in the Mini-Ames test, and causes no obvious toxicity upon long-term high-dose administration. EED-IN-5 can be used for the research of multiple sclerosis .

Cat. No.	Product Name	Target	Research Area

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 .

Gambogenic acid 2 Publications Verification	Classification of Application Fields Ketones, Aldehydes, Acids Guttiferae Phenols Polyphenols Plants Garcinia hanburyi Hook. f. Disease Research Fields Cancer Source Classification	Histone Methyltransferase
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 .

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EZH2-IN-2

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