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transcriptional repressor

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40

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0005
    Curcumin
    Maximum Cited Publications
    123 Publications Verification

    Diferuloylmethane; Natural Yellow 3; Turmeric yellow

    Histone Acetyltransferase Epigenetic Reader Domain Keap1-Nrf2 Autophagy Mitophagy Influenza Virus Ferroptosis Apoptosis Infection Metabolic Disease Inflammation/Immunology Cancer
    Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
    Curcumin
  • HY-141644
    PY-60
    15+ Cited Publications

    Annexin A YAP Inflammation/Immunology
    PY-60 is a robust and specific activator of YAP transcriptional activity that targets annexin A2 (ANXA2) with a Kd of 1.4 µM. PY-60 directly binds to ANXA2 and antagonizes its normal cellular function of repressing YAP activity .
    PY-60
  • HY-B0239
    Chloramphenicol
    15+ Cited Publications

    Antibiotic Bacterial HIF/HIF Prolyl-Hydroxylase VEGFR Autophagy Apoptosis Beclin1 JNK Akt MMP Infection Cancer
    Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research .
    Chloramphenicol
  • HY-12422

    CDK Cancer
    Voruciclib is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL) .
    Voruciclib
  • HY-N0005R
    Curcumin (Standard)
    1 Publications Verification

    Diferuloylmethane (Standard); Natural Yellow 3 (Standard); Turmeric yellow (Standard)

    Reference Standards Histone Acetyltransferase Epigenetic Reader Domain Keap1-Nrf2 Autophagy Mitophagy Influenza Virus Ferroptosis Infection Neurological Disease Inflammation/Immunology Cancer
    Curcumin (Standard) is the analytical standard of Curcumin (HY-N0005). This product is intended for research and analytical applications. Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
    Curcumin (Standard)
  • HY-W698249

    Ferroptosis Bacterial Cardiovascular Disease Infection
    Ferrous gluconate is a highly water-soluble iron-containing agent with high bioavailability and bactericidal activity. As a non-heme iron, Ferrous gluconate is used for meat product fortification and improvement of iron deficiency anemia. Ferrous gluconate induces ferroptosis in E. coli through Fe 2+ infiltration, reactive oxygen species burst, lipid peroxidation and direct interaction with DNA. Ferrous gluconate also downregulates the SOS responsive transcriptional repressor LexA. In addition, Ferrous gluconate regulates multiple key pathways in E. coli such as fatty acid metabolism, iron-sulfur cluster assembly and pyruvate metabolism, and is applied in studies related to *E. coli* infection and iron deficiency anemia .
    Ferrous gluconate
  • HY-103038
    ML327
    5 Publications Verification

    c-Myc Autophagy Cancer
    ML327 is a blocker of MYC which can also de-repress E-cadherin transcription and reverse Epithelial-to-Mesenchymal Transition (EMT).
    ML327
  • HY-N0005S

    Diferuloylmethane-d6; Natural Yellow 3-d6; Turmeric yellow-d6

    Isotope-Labeled Compounds Keap1-Nrf2 Ferroptosis Autophagy Histone Acetyltransferase Epigenetic Reader Domain Mitophagy Influenza Virus Infection Metabolic Disease Inflammation/Immunology Cancer
    Curcumin-d6 (Diferuloylmethane-d6 ) is deuterium labeled Curcumin (HY-N0005). Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
    Curcumin-d6
  • HY-156190A

    Orphan Nuclear Receptor Cancer
    NR2F2-IN-1 (free base) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F2-IN-1 (free base) substantially inhibits COUP-TFII–driven NGFIA reporter expression. NR2F2-IN-1 (free base) directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation .
    NR2F2-IN-1 free base
  • HY-146185

    Molecular Glues Bcl-2 Family Cancer
    CCT373566 is a potent and orally active molecular glue degrader of transcriptional repressor BCL6, with an IC50 of 2.2 nM. CCT373566 shows strong antiproliferative efficacy in vitro and reduction in tumor growth in vivo .
    CCT373566
  • HY-B0239R

    Reference Standards Antibiotic Bacterial HIF/HIF Prolyl-Hydroxylase VEGFR Autophagy Apoptosis Beclin1 JNK Akt MMP Infection Cancer
    Chloramphenicol (Standard) is the analytical standard of Chloramphenicol. This product is intended for research and analytical applications. Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research .
    Chloramphenicol (Standard)
  • HY-124484

    Notch Cancer
    JI130 (JI051 derivative ) is a stabilizer for the Hes1-PHB2 interaction. JI130 inhibits the ability of Hes1 to repress transcription. JI130 significantly reduces the tumor growth in a murine pancreatic tumor model and has the potential for managing pancreatic cancer .
    JI130
  • HY-12422A

    CDK Cancer
    Voruciclib hydrochloride is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib hydrochloride potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL) .
    Voruciclib hydrochloride
  • HY-160638

    TET Protein Cancer
    NSC-311068 is TET1 inhibitor. NSC-311068 selectively suppress TET1 transcription and 5-hydroxymethylcytosine (5hmC) modification. NSC-311068 represses the level of TET1 expression and the global 5hmC level. NSC-311068 effectively inhibits cell viability in AML cells with high expression of TET1 .
    NSC-311068
  • HY-143653

    BCL6 Cancer
    BCL6-IN-6 is a potent inhibitor of transcriptional repressor B-cell lymphoma 6 (BCL6). BCL6-IN-6 significantly blocks the interaction of BCL6 with its corepressors and reactivates BCL6 target genes in a dose-dependent manner. BCL6-IN-6 has the potential for the research of diffuse large B-cell lymphoma (DLBCL) .
    BCL6-IN-6
  • HY-156190

    Orphan Nuclear Receptor Cancer
    NR2F2-IN-1 (CIA1) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F2-IN-1 substantially inhibits COUP-TFII-driven NGFIA reporter expression. NR2F2-IN-1 directly binds to the COUP-TFII ligand-binding domain and disrupts COUP-TFII interaction with transcription regulators, including FOXA1, thus repressing COUP-TFII activity on target gene regulation .
    NR2F2-IN-1
  • HY-136522

    Histone Demethylase Apoptosis Cancer
    S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice .
    S2116
  • HY-146184

    Molecular Glues Bcl-2 Family Cancer
    CCT373567 is a potent molecular glue degrader of transcriptional repressor BCL6, with an IC50 of 2.9 nM. CCT373567 exhibits antiproliferative activity .
    CCT373567
  • HY-176866

    HDAC Neurological Disease
    Rodin-A is an orally active, brain-penetrant and selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC50 value of 1.80 μM for the CoREST complex, 0.15 μM for HDAC1, and 0.43 μM for HDAC2. Rodin-A increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-A is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease .
    Rodin-A
  • HY-B0239S2

    JNK Apoptosis VEGFR MMP Bacterial Akt Autophagy HIF/HIF Prolyl-Hydroxylase Antibiotic Beclin1 Cancer
    Threo-Chloramphenicol-d6 is the deuterium labeled Chloramphenicol . Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research .
    Threo-Chloramphenicol-d6
  • HY-136523

    Histone Demethylase Apoptosis Cancer
    S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells .
    S2157
  • HY-N0005S1

    Diferuloylmethane-d3; Natural Yellow 3-d3; Turmeric yellow-d3

    Isotope-Labeled Compounds Autophagy Histone Acetyltransferase Keap1-Nrf2 Influenza Virus Mitophagy Epigenetic Reader Domain Ferroptosis Infection Metabolic Disease Inflammation/Immunology Cancer
    Curcumin-d3 (Diferuloylmethane-d3 ) is deuterium labeled Curcumin (HY-N0005). Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
    Curcumin-d3
  • HY-177756

    BCL6 Cancer
    BCL6-IN-11 (Compound 8) is an efficient inhibitor that induces partial degradation of BCL6 with its IC50 value for inhibiting the interaction between BCL6 and its co-inhibitory proteins (such as NCOR1) of 6 nM. BCL6-IN-11 can induce approximately 52% degradation of BCL6 after being treated with 5 μM concentration for 90 minutes, and thus is also classified as a partial degrader. BCL6-IN-11 can be used for the study of lymphoma .
    BCL6-IN-11
  • HY-P10488

    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 .
    cycFWRPW
  • HY-151471

    c-Myc Cancer
    Anticancer agent 84 is an anticancer agent. Anticancer agent 84 represses the transcription of c-MYC by stabilizing the G-quadruplex (G4) structure. Anticancer agent 84 can be used for the research of cancer .
    Anticancer agent 84
  • HY-162478

    Phosphatase Cancer
    GR-28 is an inhibitor for small C-terminal domain phosphatase 1 (SCP1). GR-28 inhibits the transcriptional activity of repressor element-1 silencing transcription factor (REST), inhibits the proliferation of glioblastoma cells (IC50 is 2.9 and 10.1 µM, for cells A172 and T98G) .
    GR-28
  • HY-E70128

    Others Others
    Leucyl aminopeptidase, Porcine is a metallopeptidase that cleave N-terminal residues from proteins and peptides. Leucyl aminopeptidase serves as transcriptional repressors to control pyrimidine, alginate and cholera toxin biosynthesis, as well as mediate site-specific recombination events in plasmids and phages .
    Leucyl aminopeptidase, Porcine
  • HY-P10543

    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 .
    SMRT peptide
  • HY-136774

    Bcl-2 Family Cancer
    BCL6-IN-5 is a potent BCL6 inhibitor exacted from patent WO2018215801A1, example 1n, has a pIC50 of 5.82 .
    BCL6-IN-5
  • HY-174568

    mRNA Inflammation/Immunology
    Human NFKB2 mRNA encodes the human nuclear factor kappa B subunit 2 (NFKB2) protein, a subunit of the transcription factor complex nuclear factor-kappa-B (NFkB). The NFkB complex is expressed in numerous cell types and functions as a central activator of genes involved in inflammation and immune function. NFKB2 can function as either a transcriptional activator or repressor depending on its dimerization partner.
    Human NFKB2 mRNA
  • HY-146564

    NF-κB Inflammation/Immunology
    R-HP210 acts on the NF-κB mediated tethered transrepression function (IC50=3.80 μM). R-HP210 represses the LPS-induced transcription of a variety of proinflammatory genes such as IL-1β, IL-6 and COX-2. R-HP210 does not induce the transactivation functions of Glucocorticoids (GCs) .
    R-HP210
  • HY-176867

    HDAC Neurological Disease
    Rodin-B is a selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC50 value of 0.50 μM for the CoREST complex, 0.27 μM for HDAC1, and 0.28 μM for HDAC2. Rodin-B increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-B is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease .
    Rodin-B
  • HY-146561

    Glucocorticoid Receptor NF-κB Inflammation/Immunology
    S-HP210 is a potent and selective glucocorticoid receptor (GR) with an IC50 value of 1.92 μM for NF-κB transrepression (TR). S-HP210 represses the LPS-induced transcription of a variety of proinflammatory genes such as IL-1β, IL-6 and COX-2. S-HP210 is nontoxic at effective doses against mouse fibroblasts 3T3 cells .
    S-HP210
  • HY-W698249R

    Reference Standards Ferroptosis Bacterial
    Ferrous gluconate (Standard) is the analytical standard of Ferrous gluconate. This product is intended for research and analytical applications. Ferrous gluconate is a highly water-soluble iron-containing agent with high bioavailability and bactericidal activity. As a non-heme iron, Ferrous gluconate is used for meat product fortification and improvement of iron deficiency anemia. Ferrous gluconate induces ferroptosis in E. coli through Fe 2+ infiltration, reactive oxygen species burst, lipid peroxidation and direct interaction with DNA. Ferrous gluconate also downregulates the SOS responsive transcriptional repressor LexA. In addition, Ferrous gluconate regulates multiple key pathways in E. coli such as fatty acid metabolism, iron-sulfur cluster assembly and pyruvate metabolism, and is applied in studies related to *E. coli* infection and iron deficiency anemia .
    Ferrous gluconate (Standard)
  • HY-135024B

    Phenylacetyl Coenzyme A tetrasodium

    Others Metabolic Disease
    Phenylacetyl Coenzyme A (Phenylacetyl Coenzyme A) tetrasodium is an effector molecule of the TetR family transcriptional repressor PaaR. Phenylacetyl Coenzyme A tetrasodium changes the conformation of PaaR, causing it to dissociate from DNA and initiate transcription. Phenylacetyl Coenzyme A tetrasodium is promising for research of microbial metabolism .
    Phenylacetyl CoA tetrasodium
  • HY-103038R

    Reference Standards c-Myc Autophagy Cancer
    ML327 (Standard) is the analytical standard of ML327 (HY-103038). This product is intended for research and analytical applications. ML327 is a blocker of MYC which can also de-repress E-cadherin transcription and reverse Epithelial-to-Mesenchymal Transition (EMT).
    ML327 (Standard)
  • HY-165540

    Bacterial DNA/RNA Synthesis Infection
    BDM31343 is an Ethionamide (HY-B0276) synergist. BDM31343 inhibits the transcriptional repressor EthR in Mycobacterium tuberculosis, thereby relieving the inhibition of the EthA activator by Ethionamide, and enhancing the efficacy of Ethionamide. BDM31343 effectively inhibits the binding of EthR to DNA, with its IC₅₀ being 3.3 μM. BDM31343 can be used in the research of anti-Mycobacterium tuberculosis .
    BDM31343
  • HY-179498

    FOXO PTEN ROCK Epigenetic Reader Domain PI3K Akt Apoptosis Cancer
    ROCK2-IN-13 is a selective ROCK2 inhibitor. ROCK2-IN-13 reduces nuclear expression by disrupting the interaction of ROCK2 with transcriptional co activators p300> and PGC 1α, repressing oncogenic transcription. ROCK2-IN-13 activates FOXO1 driven PTEN expression, leading to suppression of the PI3K/Akt pathway, induction of G2/M cell cycle arrest, and promotion of apoptosis. ROCK2-IN-13 ablates the nuclear transcriptional function of ROCK2 that sustains oncogenic signaling and restores the tumor suppressive PTEN/FOXO1 axis. ROCK2-IN-13 can be used for prostate cancer reseach .
    ROCK2-IN-13
  • HY-183326

    IDMF

    Keap1-Nrf2 Inflammation/Immunology
    Isosorbide di-(methyl fumarate) (IDMF), topical DMF (HY-17363) derivative, is an NRF2/ARE pathway activator. Isosorbide di-(methyl fumarate) downregulates ANCR targets, modulates epithelial differentiation, represses proinflammatory cytokine genes, IL-17A- and TNF-induced keratinocyte genes, psoriatic skin lesion-specific genes, and immune response genes. Isosorbide di-(methyl fumarate) stimulates oxidative stress response gene transcription, reduces erythema and scaling in Imiquimod (HY-B0180)-induced psoriasiform lesions. Isosorbide di-(methyl fumarate) exhibits no genotoxicity or radiation sensitivity in skin fibroblasts, is nonirritating and nonsensitizing in rodent models. Isosorbide di-(methyl fumarate) can be used for the research of psoriasis vulgaris .
    Isosorbide di-(methyl fumarate)
  • HY-182014

    LXR Cardiovascular Disease Metabolic Disease
    TLC-2716 is an orally available, gut- and liver-restricted inhibitor against LXRα and LXRβ, with EC50 values of 7 nM and 15 nM, respectively. TLC-2716 represses LXRα/β transcriptional activity, downregulates genes involved in lipogenesis, lipid absorption and lipoprotein metabolism, and preserves peripheral reverse cholesterol transport. TLC-2716 reduces lipid accumulation, suppresses inflammation and fibrotic gene expression, enhances triglyceride-rich lipoprotein clearance, and improves glucose homeostasis and insulin sensitivity. TLC-2716 lowers serum and hepatic triglycerides, plasma cholesterol and other atherogenic lipid profiles in experimental models and humanized liver mice. TLC-2716 can be used for the research of dyslipidemia and related cardiometabolic disorders .
    TLC-2716

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