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Results for "

receptor internalization

" in MedChemExpress (MCE) Product Catalog:

29

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5

Biochemical Assay Reagents

8

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2

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1

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1

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-139690
    CCG258747

    		Opioid Receptor G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    CCG258747 is a selective GRK2 inhibitor (IC50=18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, >5500, and >550–fold, respectively).CCG258747 also blocks the internalization of the µ-opioid receptor. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure .
    CCG258747
  • HY-N1166
    Tephrosin
    2 Publications Verification

    Deguelinol I; Hydroxydeguelin

    		 EGFR Cancer
    Tephrosin is a natural rotenoid which has potent antitumor activities. Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors .
    Tephrosin
  • HY-174140
    CMKLR1 antagonist 3

    		Chemerin Receptor Metabolic Disease Inflammation/Immunology
    CMKLR1 antagonist 3 (Compound VU0514009) is a competitive chemokine-like receptor 1 (CMKLR1) antagonist (EC50=2 nM). CMKLR1 antagonist 3 prevents chemerin-9-induced arrestin recruitment and receptor internalization, significantly reducing Ca 2+ flux response in HEK293 cells. CMKLR1 antagonist 3 is promising for research of inflammatory diseases and metabolic syndrome .
    CMKLR1 antagonist 3
  • HY-116088
    W123

    		LPL Receptor Inflammation/Immunology
    W123, a FTY720 analog, is a competitive sphingosine 1-phosphate type 1 (S1P1) receptor antagonist. W123 is measured by GTPγS activation, MAPK recruitment, cell migration, and ligand-induced receptor internalization .
    W123
  • HY-172689
    DSPE-PEG1000-THRPPMWSPVWP

    		Liposome Cancer
    DSPE-PEG1000-THRPPMWSPVWP is a PEG compound which composed of DSPE and a transferrin receptor (TfR) peptide (THRPPMWSPVWP). THRPPMWSPVWP binds to the TfR and is subsequently internalized into TfR-expressing cells .
    DSPE-PEG1000-THRPPMWSPVWP
  • HY-172691
    DSPE-PEG5000-THRPPMWSPVWP

    		Liposome Cancer
    DSPE-PEG5000-THRPPMWSPVWP is a PEG compound which composed of DSPE and a transferrin receptor (TfR) peptide (THRPPMWSPVWP). THRPPMWSPVWP binds to the TfR and is subsequently internalized into TfR-expressing cells .
    DSPE-PEG5000-THRPPMWSPVWP
  • HY-172690A
    DSPE-PEG3400-THRPPMWSPVWP

    		Liposome Cancer
    DSPE-PEG3400-THRPPMWSPVWP is a PEG compound which composed of DSPE and a transferrin receptor (TfR) peptide (THRPPMWSPVWP). THRPPMWSPVWP binds to the TfR and is subsequently internalized into TfR-expressing cells .
    DSPE-PEG3400-THRPPMWSPVWP
  • HY-172690
    DSPE-PEG2000-THRPPMWSPVWP

    		Liposome Cancer
    DSPE-PEG2000-THRPPMWSPVWP is a PEG compound which composed of DSPE and a transferrin receptor (TfR) peptide (THRPPMWSPVWP). THRPPMWSPVWP binds to the TfR and is subsequently internalized into TfR-expressing cells .
    DSPE-PEG2000-THRPPMWSPVWP
  • HY-P3852
    Neurokinin Receptor (393-407), rat

    SPR393-407

    		 Neurokinin Receptor Neurological Disease Inflammation/Immunology
    Neurokinin Receptor (393-407), rat (SPR393–407) is a rat neurokinin 1 receptor (NK1R) fragment. NK1R is rapidly internalized by endocytosis and recycled to the plasma membrane when binding to substance P (SP). Neurokinin Receptor (393-407), rat can be used in the research of neurogenic inflammation .
    Neurokinin Receptor (393-407), rat
  • HY-164290
    Rhodady C10

    		Dynamin Infection Neurological Disease
    Rhodady C10 (Compound C10) is a dynamin I GTPase inhibitor. Rhodady C10 blocks receptor-mediated endocytosis (IC50: 7 μM). Dynamin is involved in clathrin-independent endocytosis, phagocytosis, and caveolae internalization .
    Rhodady C10
  • HY-111793A
    NUCC-390 dihydrochloride
    4 Publications Verification

    		 CXCR Neurological Disease
    NUCC-390 dihydrochloride is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 dihydrochloride induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046) . NUCC-390 dihydrochloride promotes nerve recovery of function after neurodegeneration in vivo .
    NUCC-390 dihydrochloride
  • HY-111793
    NUCC-390
    4 Publications Verification

    		 CXCR Neurological Disease
    NUCC-390 is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046) . NUCC-390 promotes nerve recovery of function after neurodegeneration in vivo .
    NUCC-390
  • HY-124071
    ACT-389949

    		Formyl Peptide Receptor (FPR) Inflammation/Immunology
    ACT-389949 is a first-in-class, potent and selective and agonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX), with an EC50 of 3 nM for FPR2/ALX internalization into monocytes. ACT-389949 has potential for the treatment of inflammatory disorders .
    ACT-389949
  • HY-139413
    β-D-Glucan

    		Toll-like Receptor (TLR) Cancer
    β-D-glucan is a natural non-digestible polysaccharide and high biocompatibility that can be selectively recognized by recognition receptors such as Dectin-1 and Toll-like receptors as well as being easily internalized by murine or human macrophages, which is likely to attribute to a target delivery . β-d-glucan is an enteric delivery vehicle for probiotics .
    β-D-Glucan
  • HY-160045
    AP1153 aptamer sodium

    		Cholecystokinin Receptor Cancer
    AP1153 aptamer sodium is a DNA aptamer that specifically binds to the cholecystokinin receptor CCKBR (Kd: ~15 pM), but does not activate CCKBR-related signaling pathways. AP1153 aptamer sodium is internalized by pancreatic ductal adenocarcinoma (PDAC) cells in a receptor-mediated manner. AP1153 aptamer sodium can bioconjugate to the surface of fluorescent nanoparticles to facilitate nanoparticle delivery to PDAC tumors in vivo .
    AP1153 aptamer sodium
  • HY-P3717
    Targefrin

    		Ephrin Receptor Cancer
    Targefrin is a potent EphA2-targeting agent, acts as an antagonist. Targefrin binds EphA2-LBD with 21 nM dissociation constant and an IC50 value of 10.8 nM. Targefrin induces cellular receptor internalization and degradation in several pancreatic cancer cell lines .
    Targefrin
  • HY-101265
    Icanbelimod

    S1p receptor agonist 1

    		 LPL Receptor Inflammation/Immunology
    Icanbelimod (S1p receptor agonist 1) is a potent and orally active S1P receptor agonist, exhibits an activity of inducing S1P1 internalization (EC50=9.83 nM). Icanbelimod has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). Icanbelimod is extracted from patent WO2015039587A1, Compound 2.
    Icanbelimod
  • HY-P2106
    Elabela(19-32)
    4 Publications Verification

    		 Arrestin Apelin Receptor (APJ) Cardiovascular Disease
    Elabela(19-32) is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart .
    Elabela(19-32)
  • HY-P10429
    RCP168

    		CXCR Infection
    RCP168 is a highly selective and affinity CXCR4 receptor antagonist (IC50=5 nM). RCP168 has a stronger ability than natural chemical factors to inhibit the entry of HIV-1 (human immunodeficiency virus type 1) into host cells via CXCR4 receptors. RCP168 inhibits HIV-1 infection by blocking viral binding sites or inducing receptor internalization. RCP168 can be used to analyze the interaction between CXCR4 receptor and other chemical factor receptors .
    RCP168
  • HY-P2106A
    Elabela(19-32) TFA
    4 Publications Verification

    		 Apelin Receptor (APJ) Arrestin Cardiovascular Disease
    Elabela(19-32) TFA is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) TFA activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) TFA induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart .
    Elabela(19-32) TFA
  • HY-P2336A
    CCZ01048 TFA
    2 Publications Verification

    		 Melanocortin Receptor Cancer
    CCZ01048 TFA, a α-MSH analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 TFA shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 TFA is a promising candidate for PET imaging of malignant melanoma .
    CCZ01048 TFA
  • HY-P2336
    CCZ01048

    		Melanocortin Receptor Cancer
    CCZ01048, a α-melanocyte-stimulating hormone (α-MSH) analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 is a promising candidate for PET imaging of malignant melanoma .
    CCZ01048
  • HY-167862
    UCM-05194

    		Endogenous Metabolite Neurological Disease
    UCM-05194 is a selective LPA1 receptor agonist with activity to improve neuropathic pain. UCM-05194 is a LPA1 agonist that exhibits potent and selective properties in its pharmacologically similar properties. UCM-05194 triggers LPA1-mediated cellular effects and leads to internalization of the receptor, resulting in functional inactivation in primary sensory neurons. UCM-05194 effectively reduces pain perception in in vivo models. UCM-05194 can be used to conduct research on progressive systemic diseases .
    UCM-05194
  • HY-P99189
    Cixutumumab

    IMC-A12; NSC742460

    		 IGF-1R Cancer
    Cixutumumab (IMC-A12) is a human anti-IGF-1R monoclonal antibody with high affinity that inhibits ligand-dependent receptor activation and downstream signaling. Cixutumumab also mediates the internalization and degradation of IGF-IR. Cixutumumab shows broad-spectrum anti-tumour activity and can be used in studies of cancers such as lung cancer, malignancies, leukaemia, non-small cell lung cancer and prostate cancer .
    Cixutumumab
  • HY-W008947
    SEW​2871
    Maximum Cited Publications
    7 Publications Verification

    		 LPL Receptor ERK Akt Neurological Disease Metabolic Disease Inflammation/Immunology
    SEW2871 is an orally active, potent, highly selective S1P1 (sphingosine-1-phosphate type 1 receptor) agonist, with an EC50 of 13.8 nM. SEW2871 activates ERK, Akt, and Rac signaling pathways and induces S1P1 internalization and recycling. SEW2871 reduces lymphocyte numbers in blood. SEW2871 can be used for the research of diabetes, Alzheimer’s disease, liver fibrosis, and inflammatory responses .
    SEW​2871
  • HY-120421
    SW116 free base

    		Sigma Receptor Cancer
    SW116 free base is a selective fluorescent ligand for sigma-2 receptor with a Ki of 14 nM. SW116 free base exhibits in methanol a maximal excitation wavelength of 333 nM, and a maximal emission wavelength of 506 nM. SW116 free base can be internalized into MDA-MB-435 cells, and reach 50% maximum fluorescent intensity in 24 minutes. SW116 free base can be as a fluorescent probe used in cancer research .
    SW116 free base
  • HY-12005R
    Fingolimod hydrochloride (Standard)

    FTY720 (Standard)

    		 Reference Standards LPL Receptor PAK Inflammation/Immunology Cancer
    Fingolimod (hydrochloride) (Standard) is the analytical standard of Fingolimod (hydrochloride). This product is intended for research and analytical applications. Fingolimod hydrochloride (FTY720), an analog of sphingosine, is a potent sphingosine 1-phosphate (S1P) receptors modulator. Fingolimod hydrochloride is phosphorylated by sphingosine kinases, particularly by SK2, and then binds S1PR1, 3, 4, and 5. Fingolimod hydrochloride induces the internalization of S1P1, and consequently, inhibits S1P activity. Fingolimod hydrochloride also is a pak1 activator .
    Fingolimod hydrochloride (Standard)
  • HY-P991243
    MP-RM-1

    		EGFR PI3K Akt Cancer
    MP-RM-1 is a selective murine monoclonal antibody inhibitor targeting human epidermal growth factor receptor 3 (ErbB-3). MP-RM-1 blocks the activation of ErbB-3 induced by neuregulin 1 (NRG-1β) and promotes the internalization and degradation of ErbB-3, inhibiting downstream signaling pathways such as PI3K-Akt. MP-RM-1 is promising for research of ErbB-3 highly expressed solid tumors such as breast cancer, melanoma, and prostate cancer .
    MP-RM-1
  • HY-119234
    CX4338

    		CXCR Inflammation/Immunology
    CX4338 is a CXCL8-mediated chemokine inhibitor with the activity of inhibiting CXCR2-mediated cell migration. CX4338 selectively inhibits CXCR2-mediated β-arrestin-2 recruitment and receptor internalization while enhancing CXCR2-mediated MAPK activation. CX4338 also inhibited CXCL8-induced chemotaxis, showing efficacy in CXCR2-overexpressing cells and human neutrophils. In vivo, CX4338 significantly reduced LPS-induced neutrophil numbers in mouse bronchoalveolar lavage fluid. The mechanism of action of CX4338 is to selectively inhibit CXCR2-mediated β-arrestin-2 activation, which is sufficient to inhibit CXCL8-mediated chemotaxis .
    CX4338

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