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transcriptional regulation

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31

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-115728

    PROTACs Cancer
    PROTAC CDK9 degrader-4 is a highly potent and efficacious CDK9 degrader for targeting transcription regulation.
    PROTAC CDK9 degrader-4
  • HY-N6747

    c-Myc Autophagy Cancer
    Stauprimide is a staurosporine analog that promotes embryonic stem cell (ESC) differentiation. Stauprimide is a non-broad spectrum inhibitor that binds to the MYC transcription factor NME2 and blocks its nuclear localization in ESCs, which results in down-regulation of MYC transcription .
    Stauprimide
  • HY-12270
    T-5224
    Maximum Cited Publications
    90 Publications Verification

    AP-1 MMP Others
    T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription .
    T-5224
  • HY-P0312
    c-Myc Peptide TFA
    1 Publications Verification

    c-Myc Cancer
    c-Myc Peptide (TFA) is a synthetic peptide corresponding to the C-terminal amino acids (410-419) of human c-myc protein, and participates in regulation of growth-related gene transcription.
    c-Myc Peptide TFA
  • HY-168518

    PROTACs CDK Cancer
    PROTAC CDK9 degrader-9 (compound 29) is a highly selective and efficient CDK9 degrader based on PROTAC technology. PROTAC CDK9 degrader-9 can be used in anti-cancer research .
    PROTAC CDK9 degrader-9
  • HY-144175

    CDK Cancer
    CDK7-IN-12 is a potent inhibitor of CDK7. CDK7-IN-12 plays a key role in transcriptional regulation and cell cycle regulation. CDK7-IN-12 effectively inhibit malignant tumor proliferation in vitro and in vivo. CDK7-IN-12 has the potential for the research of cancer disease (extracted from patent WO2021249417A1, compound 43) .
    CDK7-IN-12
  • HY-174578

    mRNA Cancer
    Human MYB mRNA encodes a protein with three HTH DNA-binding domains that functions as a transcription regulator. MYB plays an essential role in the regulation of hematopoiesis.
    Human MYB mRNA
  • HY-120106

    HDAC Others
    BG14 is a chemical optical modulation of epigenetic regulation of transcription (COMET) probe. BG14 enables high-resolution optical control of epigenetic mechanisms using visible light and can photochromically inhibit human histone deacetylases (HDACs). BG14 can be used to study the dynamic regulation of the human genome .
    BG14
  • HY-174539

    mRNA Neurological Disease
    Human SOX2 mRNA encodes the human SRY-box transcription factor 2 (SOX2) protein, a member of the SRY-related HMG-box (SOX) family of transcription factors. SOX2 involves in the regulation of embryonic development and in the determination of cell fate. In addition, SOX2 is also required for stem-cell maintenance in the central nervous system and could regulate gene expression in the stomach.
    Human SOX2 mRNA
  • HY-12270R

    AP-1 MMP Others
    T-5224 (Standard) is the analytical standard of T-5224. This product is intended for research and analytical applications. T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription .
    T-5224 (Standard)
  • HY-103691

    Autophagy Apoptosis Cancer
    ARN5187 is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 shows lysosomotropic potency and cytotoxicity. ARN5187 induces apoptosis .
    ARN5187
  • HY-103691A
    ARN5187 trihydrochloride
    1 Publications Verification

    Autophagy Apoptosis Cancer
    ARN5187 trihydrochloride is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 trihydrochloride shows lysosomotropic potency and cytotoxicity. ARN5187 trihydrochloride induces apoptosis .
    ARN5187 trihydrochloride
  • HY-112721
    FDI-6
    5+ Cited Publications

    DNA/RNA Synthesis Cancer
    FDI-6 is an inhibitor of FOXM1. FDI-6 binds directly to FOXM1 protein, to displace FOXM1 from genomic targets in MCF-7 breast cancer cells, and induce concomitant transcriptional down-regulation.
    FDI-6
  • HY-E70625

    Casein Kinase Cancer
    Casein Kinase 2 (CK2) is a serine/threonine protein kinase that is highly conserved among eukaryotes and has roles in many different cellular processes, such as cell survival, cell cycle regulation, cell polarity, stress responses, transcription and translation .
    Casein Kinase 2
  • HY-14414
    GSK4112
    5+ 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 .
    GSK4112
  • HY-N0292
    Oleuropein
    5 Publications Verification

    Cytochrome P450 PPAR Apoptosis Cardiovascular Disease Inflammation/Immunology Cancer
    Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity . Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase .
    Oleuropein
  • HY-174547

    mRNA Metabolic Disease
    Human PDX1 mRNA encodes the human pancreatic and duodenal homeobox 1 (PDX1) protein, a transcriptional activator of several genes, including insulin, somatostatin, glucokinase, islet amyloid polypeptide, and glucose transporter type 2. PDX1 may be involved in the early development of the pancreas. It also plays a major role in glucose-dependent regulation of insulin gene expression.
    Human PDX1 mRNA
  • HY-143862

    PPAR Metabolic Disease
    Pparδ agonist 7 is a potent agonist of Pparδ. The peroxisome proliferator-activated receptor (PPAR) is a member of the intranuclear receptor transcription factor superfamily that plays a key role in the regulation of metabolic homeostasis, inflammation, cell growth and differentiation in vivo. Pparδ agonist 7 has the potential for the research of non-alcoholic fatty liver disease (NAFLD) (extracted from patent WO2019105234A1, compound TM4) .
    Pparδ agonist 7
  • HY-143863

    PPAR Metabolic Disease
    Pparδ agonist 8 is a potent agonist of Pparδ. The peroxisome proliferator-activated receptor (PPAR) is a member of the intranuclear receptor transcription factor superfamily that plays a key role in the regulation of metabolic homeostasis, inflammation, cell growth and differentiation in vivo. Pparδ agonist 8 has the potential for the research of non-alcoholic fatty liver disease (NAFLD) (extracted from patent WO2021169769A1, compound TM2) .
    PPARδ agonist 8
  • HY-151379

    Histone Methyltransferase Cancer
    EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity (KD=13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours .
    EM127
  • HY-N0292R

    Cytochrome P450 Reference Standards PPAR Apoptosis Cardiovascular Disease Inflammation/Immunology Cancer
    Oleuropein (Standard) is the analytical standard of Oleuropein. This product is intended for research and analytical applications. Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity . Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase .
    Oleuropein (Standard)
  • HY-103484

    IKZF Family Cardiovascular Disease
    GATA4-NKX2-5-IN-1 (Compound 3) dose-dependently inhibits the GATA4–NKX2-5 transcriptional synergy with an IC50 of 3 μM. GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression .
    GATA4-NKX2-5-IN-1
  • HY-107916
    Thyrotropin
    1 Publications Verification

    TSH; Pretiron

    TSH Receptor PKC Apoptosis Metabolic Disease Inflammation/Immunology Endocrinology Cancer
    Thyrotropin (TSH, Pretiron) is a thyroid-stimulating hormone produced by thyrotrope cells in the anterior pituitary gland. Thyrotropin regulates the endocrine function of the thyroid. Thyrotropin induces transcriptional regulation of TH-gatekeeper genes in tanycytes through the Tshr/Gαq/PKC pathway. Thyrotropin prevents Apoptosis. Thyrotropin has an association of low levels with increased bone remodeling, reduced bone mass and a high fracture risk in mice. Thyrotropin is promising for research of skeletal remodeling, hyperthyroidism .
    Thyrotropin
  • HY-N1445
    Isoquercitrin
    5+ Cited Publications

    Isoquercetin; Quercetin 3-glucoside

    NF-κB NO Synthase Inflammation/Immunology Cancer
    Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway . Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies .
    Isoquercitrin
  • HY-P99925

    REGN421

    Notch Metabolic Disease Cancer
    Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
    Enoticumab
  • HY-N10612

    AMPK PPAR TRP Channel Mitochondrial Metabolism Metabolic Disease Cancer
    Petasin inhibits adipogenesis in cell 3T3-F442A with an IC50 of 0.95 μM. Petasin inhibits the expression of lipid synthesis factors ACC1, FAS and SCD1 by inhibiting transcription factors PPARγ and C/EBPα, as well as targeting TRPA1 and TRPV1 channels . Petasin inhibits mitochondrial complex I, thereby inhibiting tumor growth and metastasis. Petasin activates AMPK signaling pathway, participating in regulation of glucose and lipid metabolism. Petasin is orally active .
    Petasin
  • HY-156190

    Orphan Receptor Cancer
    NR2F6 modulator-2 (CIA1) is a potent and selective orphan nuclear receptor COUP-TFII (NR2F2) inhibitor. NR2F6 modulator-2 substantially inhibits COUP-TFII–driven NGFIA reporter expression. NR2F6 modulator-2 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-156190A

    Orphan 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-N1445R
    Isoquercitrin (Standard)
    1 Publications Verification

    Isoquercetin (Standard); Quercetin 3-glucoside (Standard)

    Reference Standards NF-κB NO Synthase Inflammation/Immunology Cancer
    Isoquercetin (Standard) is the analytical standard of Isoquercetin. This product is intended for research and analytical applications. Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway . Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies .
    Isoquercitrin (Standard)
  • HY-P10336

    Serpin Neurological Disease Endocrinology
    Serpinin is an agonist of the protease inhibitor Nexin-1 (PN-1). Serpinin upregulates the expression of PN-1 through the cAMP-PKA-Sp1 signaling pathway, promoting granule biogenesis in endocrine cells. Serpinin is used in research related to the regulation of secretory function . Serpinin is a selective agonist for β-adrenergic receptors. Serpinin interacts with β1-adrenergic receptors to activate the AC-cAMP-PKA pathway, which regulates myocardial systolic and diastolic function. pGlu-serpinin upregulates Bcl2 mRNA transcription and exerts neuroprotective effects .
    Serpinin
  • HY-N0086R

    6-Methyladenosine (Standard); N-Methyladenosine (Standard)

    Endogenous Metabolite Influenza Virus Reference Standards Infection
    N6-Methyladenosine (Standard) is the analytical standard of N6-Methyladenosine. This product is intended for research and analytical applications. N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities. In Vitro: N6-methyladenosine (m6A) is selectively recognized by the human YTH domain family 2 (YTHDF2) protein to regulate mRNA degradation. N6-methyladenosine (m6A), a prevalent internal modification in the messenger RNA of all eukaryotes, is post-transcriptionally installed by m6A methyltransferase (e.g., MT-A70) within the consensus sequence of G(m6A)C (70%) or A(m6A)C (30%). N6-methyladenosine (m6A)-containing RNAs are greatly enriched in the YTHDF-bound portion and diminished in the flow-through portion . N6-methyladenosine (m6A), the most abundant internal RNA modification, functions in diverse biological processes, including regulation of embryonic stem cell self-renewal and differentiation. N6-methyladenosine (m6A) is a large protein complex, consisting in part of methyltransferase-like 3 (METTL3) and methyltransferase-like 14 (METTL14) catalytic subunits .
    N6-Methyladenosine (Standard)

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