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Results for "

repressive

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (2) E1/E2/E3 Enzyme (5) E3 Ligase Ligand-Linker Conjugates (1) Endogenous Metabolite (1) Epigenetic Reader Domain (1) Glucocorticoid Receptor (2) Histone Demethylase (1) Histone Methyltransferase (14) HIV (1) MMP (2) Orphan Nuclear Receptor (1) PROTACs (6) Wnt (1)
By Research Areas:	Cancer (23) Infection (1) Inflammation/Immunology (3) Neurological Disease (1)

Inhibitors & Agonists

Peptides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-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-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-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-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-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-158102

ORIC-944	Histone Methyltransferase	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-101512

A-395 2 Publications Verification	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-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-126428

ZL0580	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-158102A

ORIC-944 TFA	Histone Methyltransferase	Cancer
ORIC-944 TFA is the TFA salt form of ORIC (HY-158102). ORIC-944 TFA is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). ORIC-944 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-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-160924

MS147	PROTACs E1/E2/E3 Enzyme	Cancer
MS147 is a VHL-based PROTAC degrader of PRC1 (Polycomb Repressive Complex 1). The dissociation constants (Kd) of MS147 for EED (Embryonic Ectoderm Development) and VHL (Von Hippel-Lindau) are 3.0 μM and 450 nM, respectively. MS147 specifically binds to the EED protein through its EED-binding moiety; EED is a core component of PRC2 (Polycomb Repressive Complex 2) and interacts with the core components of PRC1, BMI1 (B-lymphoma Mo-MLV insertion region 1 homolog) and RING1B (Ring Finger Protein 1B). By this binding, MS147 is able to recruit BMI1 and RING1B near to VHL. Through the degradation of BMI1 and RING1B, MS147 reduces the level of H2AK119ub (histone H2A lysine 119 ubiquitination), affecting the proliferation of cancer cells. (Blue: VHL ligand (HY-125845), Black: linker ; Pink: PRC1 ligand (HY-158771)) .

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-170823

PRC1-IN-1	E1/E2/E3 Enzyme	Others
PRC1-IN-1 (compound RB-4) is an inhibitor of the polycomb repressive complex PRC1 (IC₅₀=2.3 μM), targeting RING1B-BMI1, RING1A-BMI1, and RING1B-PCGF1 with IC₅₀s of 2.8, 2.6, and 1.8 μM, respectively .

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 . 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-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-13803

Tazemetostat Maximum Cited Publications 65 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-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-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 .

Cat. No.	Product Name	Target	Research Area

HY-P2254

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) .

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 .

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