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Repression

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Apoptosis (3) Bacterial (1) BCL6 (2) c-Myc (1) Calcium Channel (1) Cryptochrome (1) Deubiquitinase (2) Drug Derivative (3) E1/E2/E3 Enzyme (1) Endogenous Metabolite (2) Epigenetic Reader Domain (1) Fungal (1) G-quadruplex (1) HDAC (1) Histone Demethylase (1) HIV (1) IFNAR (1) Influenza Virus (1) LXR (1) MDM-2/p53 (1) PARP (1) PPAR (2) REV-ERB (4) SARS-CoV (1) STAT (1) STING (1)
By Research Areas:	Cancer (12) Cardiovascular Disease (1) Infection (2) Inflammation/Immunology (3) Metabolic Disease (5) Neurological Disease (3)

Inhibitors & Agonists

Peptides

Natural
Products

Recombinant Proteins

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-14415

SR8278 Maximum Cited Publications 15 Publications Verification	REV-ERB	Neurological Disease Metabolic Disease
SR8278 is a REV-ERBα antagonist and inhibits the REV-ERBα transcriptional repression activity with an EC₅₀ of 0.47 μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm. SR8278 also can be used for the research of Duchenne muscular dystrophy and Alzheimer's disease .

HY-114268

BRD-K98645985 3 Publications Verification	HIV	Infection
BRD-K98645985 is a BAF (mammalian SWI/SNF) transcriptional repression inhibitor with an EC₅₀ of ~2.37 μM. BRD-K98645985 binds ARID1A-specific BAF complexes, prevents nucleosomal positioning, and potently reverses HIV-1 latency, without T cell activation or toxicity .

HY-P1939

Cyclo(L-Leu-L-Pro) Cyclo(L-prolyl-L-leucyl)	Fungal Bacterial Influenza Virus	Infection
Cyclo(L-Leu-L-Pro) is a cyclic dipeptide with broad-spectrum antibacterial, antiviral and antifungal activities. Its biological activity is highly dependent on the stereoconfiguration and is widely present in microbial metabolites. Cyclo(L-Leu-L-Pro) efficiently and specifically inhibits the production of aflatoxin by Aspergillus flavus. The cis configuration of Cyclo(L-Leu-L-Pro) (cis-cyclo(L-Leu-L-Pro)) has broad-spectrum antibacterial activity against multi-drug resistant bacteria and significantly inhibits the influenza A virus H3N2 .

HY-138794

XL177A 5 Publications Verification	Deubiquitinase Histone Demethylase SARS-CoV	Cancer
XL177A is a covalent USP7 inhibitor that blocks the deubiquitinase activity of USP7. XL177A destabilizes non-canonical PRC1 complexes or KDM6A and reduces chromatin deposition of H2AK119Ub, thereby relieving the repression of neuronal differentiation programs. Meanwhile, XL177A also regulates the ELOF1-UVSSA-USP7-nuclear β-catenin axis, decreasing the transcription levels of related proteins and the accumulation of nuclear β-catenin. XL177A exerts antiviral effects by reducing the expression levels of coronavirus receptors, and exhibits inhibitory activity against APC-mutated colorectal cancer cells, neuroblastoma, and coronaviruses including SARS-CoV-2 variants. XL177A is mainly used in studies related to colorectal cancer, neuroblastoma, and coronavirus infections .

HY-14414

GSK4112 10+ Cited Publications SR6452	REV-ERB Apoptosis	Metabolic Disease
GSK4112 (SR6452) is a Rev-erbα agonist with an EC₅₀ value of 0.4 μM. GSK4112 can be used as a chemical tool to probe the function of Rev-erbα in transcriptional repression, regulation of circadian biology, and metabolic pathways .

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-N0642

α-L-Rhamnose monohydrate	Drug Derivative Calcium Channel	Metabolic Disease
α-L-Rhamnose monohydrate is a neutral sugar present in plants, animals, viruses and bacteria. α-L-Rhamnose monohydrate is a ligand for α-L-rhamnose-recognizing lectin sites, trigger intracellular signaling pathways. α-L-Rhamnose monohydrate induces rhaE and rhaA expression as a specific carbon source in Aspergillus nidulans, while glucose inhibits its cellular uptake. α-L-Rhamnose monohydrate induces rapid and transient increases in intracellular free Ca ²⁺ concentration in normal human dermal fibroblasts .

HY-119506

KL044 1 Publications Verification	Cryptochrome	Metabolic Disease
KL044, a stabilizer of the clock protein cryptochrome (CRY) , is a potent chemical probe with a pEC₅₀ value of 7.32, leading to the extension of the circadian period and repression of Per2 activity .

HY-U00442

CTX1	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
CTX1 is a p53 activator that overcomes HdmX-mediated p53 repression. CTX1 exhibits potent anti-cancer activity in a mouse acute myeloid leukemia (AML) model system .

HY-132822

Ivospemin SBP-101	Drug Derivative	Cancer
Ivospemin (SBP-101) is an antineoplastic spermine analog. Ivospemin has shown efficacy in slowing pancreatic and ovarian tumor progression in vitro and in vivo. Ivospemin shows modest induction of polyamine catabolism, but stronger repression of ornithine decarboxylase activity. Ivospemin is promising for research of cancers .

HY-125232

MS645 1 Publications Verification	Epigenetic Reader Domain	Cancer
MS645 is a bivalent BET bromodomains (BrD) inhibitor with a K_i of 18.4 nM for BRD4-BD1/BD2. MS645 spatially constrains bivalent inhibition of BRD4 BrDs resulting in a sustained repression of BRD4 transcriptional activity in solid-tumor cells .

HY-160821A

N-Acetylmannosamine 6-phosphate sodium salt ManNAc-6P sodium salt	Endogenous Metabolite	Others
N-Acetylmannosamine 6-phosphate sodium salt is a NanR modulator and an intermediate in the sialic acid pathway. N-Acetylmannosamine 6-phosphate sodium salt disrupts the binding of NanR to the promoter regions of nanAT and nanE, and prevents NanR-mediated transcriptional repression of these loci. N-Acetylmannosamine 6-phosphate sodium salt acts as a key precursor for sialic acid biosynthesis, participating in this process via Neu5Ac-9-P synthase. N-Acetylmannosamine 6-phosphate sodium salt can be used in research related to GNE myopathy .

HY-17663

KMR-206	PARP STAT STING IFNAR	Cancer
KMR-206 is a PARP7 inhibitor with an IC₅₀ of 13.7 nM. KMR-206 relieves AHR-mediated transcriptional repression and enhances CYP1A1 expression in the presence of TCDD. KMR-206 induces the STING-dependent IFN-β signaling pathway and increases the levels of STAT1, pSTAT1 and nuclear PARP7 in cancer cells. KMR-206 reduces the viability of lung adenocarcinoma cells, enhances radiation-induced immunogenic signals, and induces the production of immunogenic signals in glioblastoma cancer stem cells. KMR-206 destabilizes FRA1 to increase IRF1 levels and promotes the IRF3-CBP/p300 interaction. KMR-206 can be used in studies related to lung adenocarcinoma and glioblastoma .

HY-122235

MRL-24	PPAR	Cardiovascular Disease
MRL-24 is a PPARγ agonist. MRL-24 can be used in metabolic disease related research .

HY-W014004

m-Carboxycinnamic acid bishydroxamide CBHA	HDAC Apoptosis	Others Cancer
m-Carboxycinnamic acid bishydroxamide (CBHA) is a histone deacetylase inhibitor. m-Carboxycinnamic acid bishydroxamide modulates histone acetylation sites, alters DNA methylation and epigenetic status, increases global histone acetylation, alleviates transcription repression, and facilitates chromatin remodelling. m-Carboxycinnamic acid bishydroxamide can be used for the research of cloned embryo development and epigenetic regulation .

HY-138794A

(Rac)-XL177A	Deubiquitinase	Cancer
(Rac)-XL177A is the racemic isomer of XL177A (HY-138794). XL177A is a covalent USP7 inhibitor that blocks the deubiquitinase activity of USP7. XL177A destabilizes non-canonical PRC1 complexes or KDM6A and reduces chromatin deposition of H2AK119Ub, thereby relieving the repression of neuronal differentiation programs. Meanwhile, XL177A also regulates the ELOF1-UVSSA-USP7-nuclear β-catenin axis, decreasing the transcription levels of related proteins and the accumulation of nuclear β-catenin. XL177A exerts antiviral effects by reducing the expression levels of coronavirus receptors, and exhibits inhibitory activity against APC-mutated colorectal cancer cells, neuroblastoma, and coronaviruses including SARS-CoV-2 variants. XL177A is mainly used in studies related to colorectal cancer, neuroblastoma, and coronavirus infections .

HY-122959

Kihadanin B	Akt PPAR	Metabolic Disease
Kihadanin B is a citrus limonoid that can be purified from the peels of immature Citrus unshiu. Kihadanin B suppresses adipogenesis through repression of the Akt-FOXO1-PPARγ axis in 3T3-L1 adipocytes .

HY-132822A

Ivospemin hydrochloride SBP-101 hydrochloride	Drug Derivative	Cancer
Ivospemin (SBP-101) hydrochloride is an antineoplastic spermine analog. Ivospemin hydrochloride has shown efficacy in slowing pancreatic and ovarian tumor progression in vitro and in vivo. Ivospemin hydrochloride shows modest induction of polyamine catabolism, but stronger repression of ornithine decarboxylase activity. Ivospemin hydrochloride is promising for research of cancers .

HY-P10543

SMRT peptide	BCL6	Cancer
SMRT peptide is one of the co-repressors of BCL6 BTB domain interaction. SMRT peptide binds to the BTB domain of BCL6 and enhances the transcriptional repression function of BCL6. SMRT peptide can be used to study protein-protein interactions .

HY-14353

GSK-9772	LXR	Neurological Disease Inflammation/Immunology
GSK-9772 is a Liver X Receptor (LXR) modulator of the N-phenyl tertiary amine class (NPTAs) with high affinity for LXR β ligand (IC₅₀=30 nM). GSK-9772 has anti-inflammatory activity by binding to LXR, specifically by interacting with the region associated with the transcriptional repression function of the receptor, thereby inhibiting the expression of pro-inflammatory genes. GSK-9772 can be used in the study of inflammatory and neurodegenerative diseases .

HY-P10566

BCOR(498-514), biotinylated	BCL6	Cancer
BCOR(498-514), biotinylated is the minimal BCL6 binding domain with an K_D value of 1.32 µM. BCOR(498-514), biotinylated blocks BCL6-mediated transcriptional repression and kills lymphoma cells .

HY-162796

TS-2	Apoptosis G-quadruplex c-Myc	Cancer
TS-2 is a fluorescent ligand of c-Myc G4 with anticancer activity. TS-2 inhibits the growth of cancer cells and induces apoptosis of cancer cells by targeting the c-MYC oncogene promoter G4, causing transcriptional repression of the c-Myc oncogene .

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-180944

BE2012	REV-ERB	Neurological Disease
BE2012, SR8278 (HY-14415) derivative, is a potent and selective REV-ERBα/β Antagonist with EC₅₀ values of 0.285 and 0.346 μM. BE2012 binds to the ligand-binding domain (LBD) of REV-ERB, preventing the receptor from recruiting co-inhibitory factors and thereby releasing the transcriptional repression on downstream target genes. BE2012 can upregulate the expression of myogenic transcription factors Myf5 and Myod, promoting muscle regeneration and repair in acute muscle injury micemodels .

Cat. No.	Product Name	Target	Research Area

HY-P1939

Cyclo(L-Leu-L-Pro) Cyclo(L-prolyl-L-leucyl)	Fungal Bacterial Influenza Virus	Infection
Cyclo(L-Leu-L-Pro) is a cyclic dipeptide with broad-spectrum antibacterial, antiviral and antifungal activities. Its biological activity is highly dependent on the stereoconfiguration and is widely present in microbial metabolites. Cyclo(L-Leu-L-Pro) efficiently and specifically inhibits the production of aflatoxin by Aspergillus flavus. The cis configuration of Cyclo(L-Leu-L-Pro) (cis-cyclo(L-Leu-L-Pro)) has broad-spectrum antibacterial activity against multi-drug resistant bacteria and significantly inhibits the influenza A virus H3N2 .

HY-P10543

SMRT peptide	BCL6	Cancer
SMRT peptide is one of the co-repressors of BCL6 BTB domain interaction. SMRT peptide binds to the BTB domain of BCL6 and enhances the transcriptional repression function of BCL6. SMRT peptide can be used to study protein-protein interactions .

HY-P4272

Tetraproline	Peptides	Others
Tetraproline is a fragment sequence in tristetraprolin (TTP). Recruitment of the 4EHP-GYF2 cap-binding complex to tetraproline motifs of tristetraprolin promotes repression and degradation of mRNAs with AU-rich elements .

HY-P10566

BCOR(498-514), biotinylated	BCL6	Cancer
BCOR(498-514), biotinylated is the minimal BCL6 binding domain with an K_D value of 1.32 µM. BCOR(498-514), biotinylated blocks BCL6-mediated transcriptional repression and kills lymphoma cells .

HY-P10111

Histone H3K9me3 (1-15) H3(1-15)K9me3	Peptides	Inflammation/Immunology Cancer
Histone H3K9me3 (1-15) (H3(1-15)K9me3) is a histone posttranslational modification (PTM) that has emerged as hallmark of pericentromeric heterochromatin. Trimethylation of histone H3 at lysine 9 is associated with gene repression, prevents transcription factor binding .

α-L-Rhamnose monohydrate	Structural Classification other families Classification of Application Fields Metabolic Disease Plants Disease Research Fields Saccharides Monosaccharides Source Classification Cancer	Drug Derivative Calcium Channel
α-L-Rhamnose monohydrate is a neutral sugar present in plants, animals, viruses and bacteria. α-L-Rhamnose monohydrate is a ligand for α-L-rhamnose-recognizing lectin sites, trigger intracellular signaling pathways. α-L-Rhamnose monohydrate induces rhaE and rhaA expression as a specific carbon source in Aspergillus nidulans, while glucose inhibits its cellular uptake. α-L-Rhamnose monohydrate induces rapid and transient increases in intracellular free Ca ²⁺ concentration in normal human dermal fibroblasts .

Kihadanin B	Other Terpenoids Terpenoids Dictamnus dasycarpus Turcz. Rutaceae Plants Source Classification	Akt PPAR
Kihadanin B is a citrus limonoid that can be purified from the peels of immature Citrus unshiu. Kihadanin B suppresses adipogenesis through repression of the Akt-FOXO1-PPARγ axis in 3T3-L1 adipocytes .

Cat. No.	Compare	Product Name	Species	Source	Image

HY-P704059

	Rev Protein, HIV-1 group M subtype C (GST) rev; Protein Rev; ART/TRS; Anti-Repression transactivator; Regulator of expression of viral proteins	Virus	E. coli
	Rev Protein, HIV-1 group M subtype C (GST) is the recombinant virus-derived Rev protein, expressed by E. coli, with N-GST tag.

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Repression

Inhibitors & Agonists

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