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Results for "

PRC2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (2) E3 Ligase Ligand-Linker Conjugates (1) Histone Methyltransferase (15) Ligands for Target Protein for PROTAC (1) PROTAC Linkers (2) PROTACs (5)
By Research Areas:	Cancer (23)

Inhibitors & Agonists

Peptides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-101117

EED226 5+ Cited Publications	Histone Methyltransferase	Cancer
EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model . EED226 is a potent, selective, and orally bioavailable EED inhibitor ^[2]. EED226 inhibits *PRC2* with an IC₅₀ of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays .

HY-130708

UNC6852 2 Publications Verification	Histone Methyltransferase PROTACs	Cancer
UNC6852 is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC and contains an EED (embryonic ectoderm development) ligand and a von Hippel-Lindau ligand, with an IC₅₀ of 247 nM for EED .

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-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-15647

BRD9539 1 Publications Verification	Histone Methyltransferase	Cancer
BRD9539 is a histone methyltransferase G9a inhibitor with an IC₅₀ of 6.3 μM. BRD9539 also inhibits *PRC2* activity and is inactive against SUV39H1, NSD2 and DNMT1 .

HY-132970

EED ligand 1	Histone Methyltransferase	Cancer
EED ligand 1 is a diverse, potent, and efficacious inhibitor that target the EED subunit of the polycomb repressive complex 2 (PRC2) methyltransferase.

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-13803

Tazemetostat Maximum Cited Publications 51 Publications Verification 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-158102

ORIC-944	Others	Cancer
ORIC-944 is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). ORIC-944 is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer.

HY-130979

EED226-COOH	Ligands for Target Protein for PROTAC	Cancer
EED226-COOH is an EED226-derived ligand for target protein EED ligand for PROTAC, binds to a ligand for VHL via linker to form UNC6852 (HY-130708) to degrade PRC2 .

HY-W014099

Boc-NH-C4-acid	PROTAC Linkers	Cancer
Boc-NH-C4-acid is a PROTAC linker, which belongs to a Alkyl/ether linker. Boc-NH-C4-acid can be used in the synthesis of the compound PROTAC1, and specifically degrades EED, EZH2, and SUZ12 in the PRC2 Complex.

HY-130614

PROTAC EED degrader-1	PROTACs Histone Methyltransferase	Cancer
PROTAC EED degrader-1 is a von Hippel-Lindau-based PROTAC targeting EED with a pK_D of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC₅₀=8.17) targeting the EED subunit .

HY-130615

PROTAC EED degrader-2	PROTACs Histone Methyltransferase	Cancer
PROTAC EED degrader-2 is a von Hippel-Lindau-based PROTAC targeting EED with a pK_D of 9.27. PROTAC EED degrader-2 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC₅₀=8.11) targeting the EED subunit .

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-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-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-130638

(S,R,S)-AHPC-O-Ph-PEG1-NH-Boc VH032-O-Ph-PEG1-NH-Boc	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-O-Ph-PEG1-NH-Boc (VH032-O-Ph-PEG1-NH-Boc) is a synthesized E3 ligase ligand-linker conjugate which is used for the EED-targeted PROTAC .

HY-130637

Boc-NH-PEG1-Ph-O-CH2COOH

PROTAC Linkers Cancer

Boc-NH-PEG1-Ph-O-CH2COOH is a PROTAC Linker which is used for the EED-targeted PROTAC .

Boc-NH-PEG1-Ph-O-CH2COOH	PROTAC Linkers	Cancer
Boc-NH-PEG1-Ph-O-CH2COOH is a PROTAC Linker which is used for the EED-targeted PROTAC .

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-152038

SPEN-IN-1	Others	Others
SPEN-IN-1 (compound X1) is an inhibitor of SPEN which is a protein factor with a K_d value of 47 nM. SPEN-IN-1 has high selectivity for RepA, a 431-nucleotide domain in Xist (a non-coding RNA prototype) that comprises 8.5 units of a GC-rich motif responsible for gene silencing .

HY-147525

PROTAC EZH2 Degrader-1	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 .

H3K27(Me3) (15-34)	Peptides	Cancer
H3K27(Me3) (15-34), a histone peptide, is a repressive chromatin mark derived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) ^[2].

H3K27(Me) (15-34)	Peptides	Cancer
H3K27(Me) (15-34), a histone peptide, is a repressive chromatin markderived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) ^[2].

H3K27(Me2) (15-34)	Peptides	Cancer
H3K27(Me2) (15-34), a histone peptide, is a repressive chromatin mark derived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) ^[2].

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 .

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