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Results for "

repressive

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Apoptosis (2) BMI1 (1) E1/E2/E3 Enzyme (4) E3 Ligase Ligand-Linker Conjugates (1) Endogenous Metabolite (1) Epigenetic Reader Domain (1) Glucocorticoid Receptor (2) Histone Demethylase (3) Histone Methyltransferase (23) HIV (1) MMP (2) mTOR (1) NF-κB (1) Notch (2) Orphan Nuclear Receptor (1) p38 MAPK (1) PI3K (1) PROTACs (6) Reference Standards (4) REV-ERB (1) TGF-beta/Smad (2) Wnt (1)
By Research Areas:	Cancer (33) Infection (1) Inflammation/Immunology (5) Metabolic Disease (1) Neurological Disease (2)

Inhibitors & Agonists

Peptides

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13803

Tazemetostat Maximum Cited Publications 89 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-19817

PRT4165 5+ Cited Publications NSC600157	E1/E2/E3 Enzyme	Cancer
PRT4165 is a potent inhibitor of polycomb-repressive complex 1 (PRC1)-mediated H2A ubiquitylation.

HY-139514

RB-3	E1/E2/E3 Enzyme	Cancer
RB-3, a polycomb repressive complex 1 (PRC1) inhibitor, binds to RING1B-BMI1f, with a K_d of 2.8 μM .

HY-158102

Rinzimetostat 1 Publications Verification ORIC-944	Histone Methyltransferase	Cancer
Rinzimetostat (ORIC-944) is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). Rinzimetostat is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer.

HY-101117

EED226 10+ 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 . 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 4 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 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-176851

GSK1362	REV-ERB	Inflammation/Immunology
GSK1362 is a selective inverse agonist of REV-ERB. GSK1362disrupts the interaction of REV-ERBα with repressive co-modulators (NCoR1, SMRT2, RIP140). GSK1362 exerts an inverse agonist effect by increasing the transcription of BMAL1 to relieve BMAL1 repression by endogenous REV-ERB ligands. GSK1362 suppresses LPS (HY-D1056)-induced inflammatory cytokine expression, inhibits IL-1β-induced Cxcl5 transcription in cells. GSK1362 can be used for the study of inflammatory diseases .

HY-132922

EEDi-5273 APG-5918	Histone Methyltransferase	Cancer
EEDi-5273 (APG-5918) is a potent and orally active embryonic ectoderm development (EED) inhibitor with an IC₅₀ of 0.2 nM. EEDi-5273 can inhibit the polycomb repressive complex 2 (PRC2) activity and block trimethylation of histone H3 lysine 27. EEDi-5273 can be used for the research of cancer, such as ovarian cancer .

HY-119344

MS37452 1 Publications Verification	Histone Methyltransferase	Cancer
MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3, with a K_d of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells .

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-130615

PROTAC EED degrader-2 1 Publications Verification	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-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-160924

MS147	PROTACs BMI1 E1/E2/E3 Enzyme Histone Methyltransferase	Cancer
MS147 is a VHL-based PROTAC degrader of BMI1 and RING1B (polycomb repressive complex 1 core components). MS147 directly binds EED and VHL E3 ligase, recruiting the ligase to the EED-BMI1/RING1B complex to induce time-dependent, ubiquitination-mediated degradation of BMI1 and RING1B. MS147 reduces histone H₂A Lys119 mono-ubiquitination without altering histone H₃ Lys27 tri-methylation and inhibits cancer cells proliferation. MS147 can be used for the research of cancer, such as chronic myelogenous leukemia and b-cell lymphoma . (Pink: BMI1/RING1B ligand (HY-183634); Blue: VHL ligand (HY-125845); Black: linker)

HY-135572

TLX agonist 1	Orphan Nuclear Receptor	Neurological Disease Cancer
TLX agonist 1 (ccrp2) is an orphan nuclear receptor tailless (TLX, NR2E1) modulator (EC₅₀=1μM; K_d= 650 nM). TLX agonist 1 potentiates TLX transcriptional repressive activity .

HY-126428

ZL0580 1 Publications Verification	HIV Epigenetic Reader Domain	Infection Inflammation/Immunology
ZL0580, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of BRD4. ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter .

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-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-158239

MS181	PROTACs E1/E2/E3 Enzyme	Cancer
MS181 (compound 1) is a potent cereblon (CRBN)-recruiting and EED-binding *polycomb repressive* complex 1 (PRC1)** PROTAC degrader. MS181 decreases the expression of EED, EZH2, SUZ12, BMI1 and RING1B. MS181 shows antiproliferative activity (Strtucture Note: Red, EED binder (HY-158771); Blue, CRBN ligand (HY-41547); Black, Linker HY-131717) .

HY-P2254

H3K27(Me3) (15-34)	Histone Methyltransferase	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) .

HY-158102A

Rinzimetostat TFA 1 Publications Verification ORIC-944 TFA	Histone Methyltransferase	Cancer
Rinzimetostat (ORIC-944) TFA is the TFA salt form of ORIC (HY-158102). Rinzimetostat TFA is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). Rinzimetostat TFA is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer .

HY-130816

(S,R,S)-AHPC-O-Ph-PEG1-NH2 VH032-O-Ph-PEG1-NH2	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-O-Ph-PEG1-NH2 (VH032-O-Ph-PEG1-NH2) is E3 ligase ligand-linker conjugate and incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-O-Ph-PEG1-NH2 is used in PROTAC EED degrader-1 (HY-130614). PROTAC EED degrader-1 is a PROTAC targeting EED with a pK_D of 9.02 .

HY-142941

Glucocorticoid receptor-IN-1	Glucocorticoid Receptor MMP	Inflammation/Immunology
Glucocorticoid receptor-IN-1 (Compound WX002) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-1 exhibits very good transcriptional repressive activity with an IC₅₀ of 2.11 nM against hMMP1, and transcriptional activation activity with an EC₅₀ of 5.59 nM against MMTV .

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-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-P2252

H3K27(Me) (15-34)	Histone Methyltransferase	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) .

HY-P2253

H3K27(Me2) (15-34)	Histone Demethylase	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) .

HY-142942

Glucocorticoid receptor-IN-2	Glucocorticoid Receptor MMP	Inflammation/Immunology
Glucocorticoid receptor-IN-2 (Compound WX019) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-2 exhibits very good transcriptional repressive activity with an IC₅₀ of 0.171 nM against hMMP1, and comparable transcriptional activation activity with an EC₅₀ of 0.94 nM against MMTV .

HY-P10488

cycFWRPW	Wnt Others	Cancer
cycFWRPW is a peptide inhibitor of TLE1. TLE1 is an oncogenic transcriptional co‐repressor that exerts its repressive effects through binding of transcription factors, and inhibits Wnt signaling .

HY-101512D

rel-A-395 hydrochloride	Histone Methyltransferase	Cancer
rel-A-395 hydrochloride is the relative configuration of A-395 (HY-101512) hydrochloride. 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-100846R

JQEZ5 (Standard)	Histone Methyltransferase Reference Standards	Cancer
JQEZ5 (Standard) is the analytical standard of JQEZ5 (HY-100846). This product is intended for research and analytical applications. 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-101512R

A-395 (Standard)	Reference Standards Histone Methyltransferase	Cancer
A-395 (Standard) is the analytical standard of A-395 (HY-101512). This product is intended for research and analytical applications. 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-W783478

Calebin A	PI3K Akt mTOR p38 MAPK NF-κB	Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Calebin A is a PI3K/Akt/mTOR, MAPK, and NF-κB inhibitor with oral effectiveness. Calebin A can block the autophagy-repressive, inhibiting apoptosis. Calebin A has anti-tumor activity by epigenetic regulation. Calebin A suppresses adipogenesis, modulates thermogenesis, and enriches gut probiotics. Calebin A can be used in research on osteoarthritis, Alzheimer's disease, type 2 diabetes, malignant peripheral nerve sheath tumors, and colorectal cancer .

HY-124660A

A-395N	Endogenous Metabolite	Others
A-395N serves as a control probe for A-395, a highly potent and selective chemical probe targeting the polycomb protein EED, a key player in Polycomb repressive complex 2 (PRC2) responsible for transcriptional repression via histone H3K27 methylation. While A-395N bears structural similarities to A-395, it demonstrates no pharmacological activity in biochemical or cellular assays, making it an ideal control compound.

HY-183067

TAS1440	Histone Demethylase TGF-beta/Smad Notch	Cancer
TAS1440 is an orally active LSD1/KDM1A inhibitor with a human IC₅₀ of 4.8 nM. TAS1440 non-covalently binds to the histone H₃-binding pocket of LSD1, inhibiting demethylase activity and disrupting repressive complexes with INSM1 and SMAD2. TAS1440 activates tumor-suppressive TGF-β and NOTCH signaling pathways via transcriptional reprogramming. TAS1440 can be used for the research of small cell lung cancer, specifically the SCLC-A subtype .

HY-183067A

TAS1440 benzoate	Histone Demethylase TGF-beta/Smad Notch	Cancer
TAS1440 benzoate is an orally active LSD1/KDM1A inhibitor with a human IC₅₀ of 4.8 nM. TAS1440 benzoate non-covalently binds to the histone H3-binding pocket of LSD1, inhibiting demethylase activity and disrupting repressive complexes with INSM1 and SMAD2. TAS1440 benzoate activates tumor-suppressive TGF-β and NOTCH signaling pathways via transcriptional reprogramming. TAS1440 benzoate can be used for the research of small cell lung cancer, specifically the SCLC-A subtype .

HY-101117R

EED226 (Standard)	Histone Methyltransferase Reference Standards	Cancer
EED226 (Standard) is the analytical standard of EED226 (HY-101117). This product is intended for research and analytical applications. 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 . 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-183058

EZM8266	Histone Methyltransferase	Cancer
EZM8266 is an orally active and selective G9a (EHMT2) histone methyltransferase inhibitor with a human EHMT2 IC₅₀ of 1 pM. EZM8266 reduces repressive H3K9me2 marks at immune-stimulatory gene and endogenous retroviral element promoters. EZM8266 reduces colony formation, migration, and invasion of cancer cells. EZM8266 enhances IFN-γ response, increases MHC class I expression, and enhances CXCL10-mediated T cell recruitment in cancer cells. EZM8266 can be used for the research of hepatocellular carcinoma .

Cat. No.	Product Name	Target	Research Area

HY-P2254

H3K27(Me3) (15-34)	Histone Methyltransferase	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) .

HY-P2252

H3K27(Me) (15-34)	Histone Methyltransferase	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) .

HY-P2253

H3K27(Me2) (15-34)	Histone Demethylase	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) .

HY-P10488

cycFWRPW	Wnt Peptides	Cancer
cycFWRPW is a peptide inhibitor of TLE1. TLE1 is an oncogenic transcriptional co‐repressor that exerts its repressive effects through binding of transcription factors, and inhibits Wnt signaling .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-W783478

Calebin A	Structural Classification Phenols Polyphenols Plants Curcuma longa Source Classification Zingiberaceae	PI3K Akt mTOR p38 MAPK NF-κB
Calebin A is a PI3K/Akt/mTOR, MAPK, and NF-κB inhibitor with oral effectiveness. Calebin A can block the autophagy-repressive, inhibiting apoptosis. Calebin A has anti-tumor activity by epigenetic regulation. Calebin A suppresses adipogenesis, modulates thermogenesis, and enriches gut probiotics. Calebin A can be used in research on osteoarthritis, Alzheimer's disease, type 2 diabetes, malignant peripheral nerve sheath tumors, and colorectal cancer .

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repressive

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