Search Result

Search Result

Results for "

repressive

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) E1/E2/E3 Enzyme (1) E3 Ligase Ligand-Linker Conjugates (1) Epigenetic Reader Domain (1) Glucocorticoid Receptor (2) Histone Methyltransferase (10) HIV (1) MMP (2) PROTACs (4)
By Research Areas:	Cancer (17) Infection (1) Inflammation/Immunology (3) Neurological Disease (1)

17

Inhibitors & Agonists

3

Peptides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

TLX agonist 1	Others	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 .

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 .

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 .

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 .

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.

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 .

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 .

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.

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 .

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 .

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 .

MS37452	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 .

(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 .

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 .

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-139514

RB-3

E1/E2/E3 Enzyme Cancer

RB-3, a PRC1 inhibitor, binds to RING1B-BMI1f, with a K_d of 2.8 μM .

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 .

Cat. No.	Product Name	Target	Research Area

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) .

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) .

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) .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

MedChemExpress Magic Cece

MedChemExpress: Contact Us; About Us; Headquarters; Distributors; Statement on False Report; Careers

Customer Support: Technical Support; Service; Ordering Information; Easy Return; Shipping Rates & Policies; Intellectual Property Promise

Resources: Free Sample; Resources; Molarity Calculator; Dilution Calculator; Terms & Conditions; Reconstitution Calculator; Specific Activity Calculator

Subscribe to our E-newsletter

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.

Copyright © 2013-2024 MedChemExpress. All Rights Reserved.: Site Map Privacy Policy

Join with us