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Results for "

transmembrane domain

" in MedChemExpress (MCE) Product Catalog:

22

Inhibitors & Agonists

8

Peptides

31

Recombinant Proteins

1

Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-129527

    iGluR Neurological Disease
    GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity .
    GNE-9278
  • HY-107506

    mGluR Neurological Disease
    Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation .
    Ro 67-4853
  • HY-P1985A

    Notch Cardiovascular Disease Cancer
    Notch 1 TFA (Notch homolog 1, translocation-associated) can encode a member of the NOTCH family of proteins. Members of this Type I transmembrane protein family share structural characteristics including an extracellular domain consisting of multiple epidermal growth factor-like (EGF) repeats, and an intracellular domain consisting of multiple different domain types .
    Notch 1 TFA
  • HY-119165

    γ-secretase Neurological Disease
    GSM-1 is a potent γ-secretase modulator. GSM-1 directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1) .
    GSM-1
  • HY-P2508

    Mucin Cancer
    MUC1, mucin core is the region of the MUC1 mucin core. MUC1 is a type I transmembrane glycoprotein, and is overexpressed and aberrantly glycosylated in carcinoma cells. MUC1, mucin core protein binds to domain 1 of ICAM-1 .
    MUC1, mucin core
  • HY-156095

    Wnt Cancer
    F7H is a Frizzled receptor FZD7 antagonist (IC50: 1.25 μM). Frizzled receptors (FZDs) influence Wnt signaling, mediating embryonic development and tissue homeostasis. F7H is a potent ligand for the FZD7 transmembrane domain (TMD) .
    F7H
  • HY-117903A

    Smo Hedgehog Cancer
    MRT-92 is a Smoothened (Smo) antagonist (Ki=0.7 nM) with anticancer activity. MRT-92 inhibits Hedgehog signaling pathway and rodent cerebellar granule cell proliferation by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor (IC50=0.4 nM). MRT-92 can be used in the study of cerebellar glioma .
    MRT-92
  • HY-145416

    Bacterial Infection
    G247 is a specific MsbA inhibitor. G247 acts as a transmembrane domains (TMDs) wedge, symmetrically increasing nucleotide-binding domains (NBDs) separation and preventing conformational transition of MsbA. G247 suppresses ATPase activity by increasing inter-NBD distance .
    G247
  • HY-P10416

    Q14 peptide

    Deubiquitinase Mitophagy Others Neurological Disease
    Q14 is a polypeptide derived from the USP30 (ubiquitin specific peptidase 30) transmembrane (TM) domain with the ability to inhibit the deubiquitination activity of USP30 (IC50=57.2 nM). Q14 reduces USP30 activity by inhibiting the interaction between the USP30 transmembrane domain and its catalytic domain. Q14 peptide contains the LC3 interaction region (LIR) motif, which enables it to bind to the LC3 and accelerate the formation of autophagosomes, thereby promoting mitophagy. Q14 can be used in the study of neurodegenerative diseases as well as mitochondrial quality control and cell metabolism .
    Q14
  • HY-162040

    P-glycoprotein Cancer
    P-gp inhibitor 17 (compound 2g) is a P-gp inhibitor directly interacted with the transmembrane domain of P-gp. P-gp inhibitor 17 can be used for P-gp-mediated multidrug-resistant in tumor cells study .
    P-gp inhibitor 17
  • HY-111163

    Apoptosis Cancer
    NSC49652 is a reversible, orally active p75 neurotrophin receptor (p75 NTR, also known as NGFR, TNFRSF16, and CD271) agonist. NSC49652 targets the transmembrane domain of p75 NTR. NSC49652 induces apoptosis and affects the viability of melanoma cells .
    NSC49652
  • HY-158185

    GABA Receptor Others
    Isocycloseram is an isoxazoline insecticide and acaricide widely recognized as an allosteric modulator of GABA-gated chloride channels. Isocycloseram is active against Lepidopteran, Hemiptera, Coleoptera, Thysanoptera and Diptera pests. Isocycloseram targets the invertebrate Rdl GABA receptor, but the G335M mutation in the third transmembrane domain of the Rdl GABA receptor may mediate resistance .
    Isocycloseram
  • HY-117833

    VAP-1 Inflammation/Immunology
    PXS-4681A is a potent, selective, irreversible and orally active semicarbazide-sensitive amine oxidase (SSAO; VAP-1) inhibitor with a Ki of 37 nM. PXS-4681A shows highly selectivity over related amine oxidases, ion channels, and seven-transmembrane domain receptors. PXS-4681A has anti-inflammatory effects .
    PXS-4681A
  • HY-P10495

    Transmembrane Glycoprotein Others Cancer
    GPR110 peptide agonist P12 is a peptide that acts as a GPR110 agonist. GPR110 peptide agonist P12 can significantly enhance the initial rate of GPR110 stimulated G protein GTPγS binding. GPR110 peptide agonist P12 mimics the action of natural ligands, causing the extracellular domain (ECD) of the GPR110 to dissociate from the seven transmembrane domains (7TM), exposing the β-strand-13/stalk region at the N-terminus of the 7TM domain, which acts as an agonist to activate G protein signaling. GPR110 peptide agonist P12 can be used in the study of developmental disorders and cancers related to GPR110 .
    GPR110 peptide agonist P12
  • HY-P10716

    GLP Receptor Metabolic Disease
    Exendin-P5 is a selective agonist that targets the GLP-1R. Exendin-P5 promotes rapid activation of G proteins by transient interactions with the transmembrane domain of GLP-1R, enhancing its potency in G protein-mediated signaling and accelerating cAMP production. This mechanism suggests the potential application of Exendin-P5 in the study of metabolic diseases .
    Exendin-P5
  • HY-103565

    mGluR Neurological Disease
    AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
    AMN082
  • HY-P5472

    Transmembrane Glycoprotein Others
    Tumour-associated MUC1 epitope is a biological active peptide. (This sequence is the hallmark of MUC1 mucin. MUC1 is a highly glycosylated type I transmembrane glycoprotein with a unique extracellular domain consisting of a variable number of tandem repeats (VNTR) of this 20 amino acid peptide. It is overexpressed on the cell surface of many human adenocarcinomas and hematological malignancies, including multiple myeloma and B-cell lymphoma, making MUC1 broadly applicable target for immunotherapeutic strategies.)
    Tumour-associated MUC1 epitope
  • HY-150407

    Ligands for Target Protein for PROTAC Autophagy Others Neurological Disease Cancer
    TSPO ligand-1 is the ligand of AUTAC4 (HY-134640) that can be used in the synthesis of PROTACs. TSPO ligand-1 is a mitochondrial outer membrane transmembrane structural domain protein can bind to AUTAC4 and regulate mitochondrial autophagy to promote targeted mitochondrial renewal. TSPO ligand-1 is also involved in the transport of cholesterol from the outer to inner mitochondrial membrane and serves as a sensitive biomarker of brain injury and neurodegeneration .
    TSPO ligand-1
  • HY-157214

    STING Molecular Glues Cancer
    NVS-STG2 is a molecular glue that targets STING and activates STING-mediated immune signaling. NVS-STG2 induces higher-order oligomerization of human STING by binding to pockets between adjacent STING dimer transmembrane domains, effectively acting as a molecular glue. NVS-STGI enhances the activity of cGAMP by inducing the formation of more abundant and larger oligomers. NVS-STG2 produces antitumor activity in animal models .
    NVS-STG2
  • HY-111161

    nAChR Parasite Infection
    GSK575594A is a modulator of the nicotinic acetylcholine receptor (nAChR) in Ascaris suum. GSK575594A enhances muscle contractions induced by acetylcholine (ACh) by binding to the allosteric binding site between subunits within the transmembrane domain of nAChR. At a concentration of 3 μM, GSK575594A significantly increased the contraction induced by ACh in Ascaris suum (Emax increased from 1.19 g to 1.51 g). GSK575594A may be used in research within the field of antiparasitic studies .
    GSK575594A
  • HY-103565A

    mGluR Neurological Disease
    AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
    AMN082 free base
  • HY-P1925A
    GO-203 TFA
    2 Publications Verification

    PI3K Reactive Oxygen Species Apoptosis Cancer
    GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembrane potential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice .
    GO-203 TFA

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