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Results for "

ligand-binding site

" in MedChemExpress (MCE) Product Catalog:

11

Inhibitors & Agonists

1

Fluorescent Dyes

3

Inhibitory Antibodies

1

Natural
Products

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0010
    Geniposidic acid
    5+ Cited Publications

    FXR Sirtuin TNF Receptor Interleukin Related Metabolic Disease
    Geniposidic acid is an orally active FXR modulator and SIRT6 activator. Geniposidic acid binds to the Ser332 and His447 sites on the FXR ligand-binding domain, thereby driving nuclear translocation, coactivator recruitment, and transcription of downstream bile acid and cholesterol metabolism-related genes. Geniposidic acid improves metabolic dysfunction-related fatty liver disease by activating the SIRT6 signaling pathway. Geniposidic acid inhibits inflammation and modulates gut microbiota to alleviate colitis. Geniposidic acid can be used in research on drug-induced liver injury, inflammatory bowel disease, metabolic dysfunction-related fatty liver disease, and metabolic dysfunction-related steatohepatitis .
    Geniposidic acid
  • HY-P9964

    11F8; IMC-11F8; LY3012211

    EGFR Cancer
    Necitumumab (11F8; IMC-11F8; LY3012211) is a human IgG monoclonal antibody directed against EGFR. Necitumumab binds to the EGF binding site of EGFR, blocks ligand binding, neutralizes ligand-induced EGFR phosphorylation and downstream signaling, induces EGFR internalization and degradation, and mediates antibody-dependent cellular cytotoxicity (ADCC) in EGFR-expressing cells. Necitumumab enhances antitumour activity in combination with Gemcitabine (HY-17026) and Cisplatin (HY-17394) in murine non-small-cell lung cancer xenograft models. Necitumumab can be used in research on cancers such as non-small cell lung cancer and colorectal cancer .
    Necitumumab
  • HY-P991224

    CCR Inflammation/Immunology Cancer
    CAP-100 is a monoclonal antibody that targets CCR7. CAP-100 neutralizes the ligand-binding site and signaling of CCR7. CAP-100 strongly inhibits CCR7-induced migration, extravasation, homing, and survival in chronic lymphocytic leukemia (CLL) samples. CAP-100 triggers potent tumor cell killing, mediated by host immune mechanism. CAP-100 shows a favorable toxicity profile on relevant hematopoietic subsets. CAP-100 is involved in research on anti-tumor and disease such as CLL .
    CAP-100
  • HY-B1403

    Estrogen Receptor/ERR Endocrinology
    Dienestrol is an orally active nonsteroidal estrogen. Dienestrol prevents the formation of implantation swellings in the uterus by inhibiting ovum discharge .
    Dienestrol
  • HY-160250

    Fluorescent Dye UGT Metabolic Disease
    UGT1A1-IN-1 is a UGT1A1 inhibitor and fluorescent probe (Ex=370 nm, Em=520 nm), with an IC50 of 1.33 μM and a Ki of 5.02 μM. UGT1A1-IN-1 is selectively glucuronidated by UGT1A1 at the bilirubin homologous binding site, and its PET effect is blocked along with this reaction, triggering fluorescence changes. UGT1A1-IN-1 can serve as a substitute for bilirubin to detect UGT1A1 activity and perform high-throughput screening of UGT1A1 modulators .
    UGT1A1-IN-1
  • HY-P991553

    TNF Receptor Apoptosis Inflammation/Immunology Cancer
    HeFi-1 is a mouse anti-CD30 IgG1 monoclonal antibody. HeFi-1 recognizes the ligand-binding site on CD30. HeFi-1 can inhibit the growth of tumor cells with high expression of CD30. HeFi-1 can induce eosinophil apoptosis. HeFi-1 can be used for researches on cancer or inflammation conditions such as anaplastic large-cell lymphoma (ALCL) and asthma .
    HeFi-1
  • HY-D2857

    Fluorescent Dye Metabolic Disease
    NBD-Stearic acid is a stearic acid labeled with a nitrobenzoxadiazole (NBD) fluorophore. NBD-Stearic acid can be used as a probe for fatty acid uptake or the the ligand binding sites of fatty acid and sterol carrier proteins (FABP)
    NBD-Stearic acid
  • HY-141551

    Estrogen Receptor/ERR Cancer
    GNE-274 is a structural analog of the ER degrader GDC-0927 and is a non-degrader. GNE-274 does not induce conversion of ER in breast cancer cell lines and functions as a partial ER agonist (partial ER agonist). GNE-274 increases the chromatin accessibility of ER-DNA binding sites, whereas GDC-0927 does not. GNE-274 is an effective ER ligand binding domain (LBD) inhibitor. GNE-274 can be used in cancer research.
    GNE-274
  • HY-180554

    Synaptic Vesicle Proteins Neurological Disease
    UCB1244283 is a synaptic vesicle glycoprotein 2A (SV2A) allosteric modulator. UCB1244283 binds to a secondary ligand-binding site in SV2A and enhances orthosteric ligand engagement when the orthosteric site is occupied, by stabilizing the occluded state and slowing ligand dissociation. UCB1244283 shows a clear protective effect against both tonic and clonic convulsions in sound-sensitive mice. UCB1244283 can be used for epilepsy research .
    UCB1244283
  • HY-183602

    DNA/RNA Synthesis Cancer
    FRC-303 is a CHD1 inhibitor with a Kd of 0.14 μM and an IC50 of 0.18 μM. FRC-303 binds to the H3K4me3 binding site of CHD1 tandem chromodomain, forms aromatic cage interactions and extended ligand contacts, acts as a methyl-lysine mimic, and occupies natural peptide ligand-binding regions. FRC-303 can be used for the research of prostate cancer .
    FRC-303
  • HY-181020

    Phosphodiesterase (PDE) p38 MAPK Akt mTOR ERK Cancer
    Deltafluorine is a phosphodiesterase delta (PDEδ) inhibitor with an IC50 of 27 nM, a KD of 148 nM. Deltafluorine covalently modifies the specific glutamate residue p.E88 in the ligand binding site of PDEδ, interfering with its chaperone function. Deltafluorine inhibits signaling through the MAPK and Akt-mTOR pathway, reduces ERK1/2 expression. Deltafluorine reduces tumor volume in an autochthonous mouse model of Kras-driven lung adenocarcinoma. Deltafluorine can be used for the research of lung adenocarcinoma .
    Deltafluorine

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