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Results for "

Internalization

" in MedChemExpress (MCE) Product Catalog:

67

Inhibitors & Agonists

5

Fluorescent Dye

3

Biochemical Assay Reagents

19

Peptides

8

Inhibitory Antibodies

8

Natural
Products

1

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-144258
    PD-1/PD-L1-IN-14

    		PD-1/PD-L1 Inflammation/Immunology Cancer
    PD-1/PD-L1-IN-14 (compound 17) is a bifunctional inhibitor of PD-1/PD-L1 interactions, with an IC50 of 27.8 nM. PD-1/PD-L1-IN-14 (compound 17) inhibits PD-1/PD-L1 interactions and promotes dimerization, internalization, and degradation of PD-L1 .
    PD-1/PD-L1-IN-14
  • HY-139690
    CCG258747

    		Opioid Receptor 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-111793A
    NUCC-390 dihydrochloride
    2 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-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-118518
    Ronipamil

    		Calcium Channel Cardiovascular Disease Cancer
    Ronipamil is a calcium ion antagonist. Ronipamil increases the specific binding and internalization of human 125I-LDL in human skin fibroblasts (HSF) and the human hepatoma cell line Hep G2 .
    Ronipamil
  • HY-111793
    NUCC-390

    		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-144347
    HF51116

    		CXCR Infection Cancer
    HF51116 is a potent antagonist of CXCR4. HF51116 strongly antagonizes SDF-1α-induced cell migration, calcium mobilization, and CXCR4 internalization. HF51116 inhibits HIV-1 infection via CXCR4. HF51116 has the potential for the research of HIV-1 infection, hematopoietic stem cell mobilization, and cancer metastasis .
    HF51116
  • HY-162973
    PD-L1 ligand 1

    		PD-1/PD-L1 Ligands for Target Protein for PROTAC Cancer
    PD-L1 ligand 1 is a PROTAC target protein ligand. PD-L1 ligand 1 can be used as a PD-L1 degrader .
    PD-L1 ligand 1
  • HY-NP035
    Ovalbumin-FITC

    OVA-FITC

    		 Fluorescent Dye Biochemical Assay Reagents Others
    Ovalbumin-FITC is an ovalbumin conjugated to FITC (Ex=495 nm; Em=525 nm). Ovalbumin-FITC can be internalized by cells via endocytosis .
    Ovalbumin-FITC
  • HY-106481
    Bufrolin

    		GPR35 Histamine Receptor Inflammation/Immunology
    Bufrolin is a Cromoglycate (histamine release inhibitor) analog and a high potency agonist of GPR35. Bufrolin promotes interactions between β-arrestin-2 and either human GPR35a or rat GPR35. Bufrolin also serves as antiallergic mast cell stabilizer and inhibit an anti-inflammatory response inducible by the internalization peptide. Bufrolin acts as an anti-inflammatory agent to be used in research of delivering pharmacol linked with internalization peptide .
    Bufrolin
  • HY-163079
    AlF-PD-FAPI

    		FAP Cancer
    AlF-PD-FAPI has affinity for FAP , with the IC50 of 0.13 nM, and shows a specific uptake, high internalized fraction, and low cellular efflux in vitro. AlF-PD-FAPI can be used as FAP-targeting tracer .
    AlF-PD-FAPI
  • HY-P10085
    PKC-ε translocation inhibitor peptide

    		PKC Inflammation/Immunology
    PKC-ε translocation inhibitor peptide is a PKC-ε translocation inhibitor. PKC-ε translocation inhibitor peptide can regulate the rate of FcγR-mediated internalization of opsonized beads, has no effect of FcαR trafficking .
    PKC-ε translocation inhibitor peptide
  • 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-161604
    HBV/HDV-IN-1

    		HBV PD-1/PD-L1 Infection Inflammation/Immunology Cancer
    HBV/HDV-IN-1 (Compd 122) is a HBV, HDV and PD-1/PD-L1 inhibitor, with EC50 values of 8 nM for T cell activation and 35 nM for PD-L1 internalization .
    HBV/HDV-IN-1
  • HY-144793
    Deac-SS-Biotin

    		Others Cancer
    Deac-SS-Biotin is a potent antitumor agent. Deac-SS-Biotin uptakes into the cells through biotin-mediated internalization. Deac-SS-Biotin combined with DTT (Glutathione mimetic) can effectively inhibit microtubule assembly and displays greater antitumor activity .
    Deac-SS-Biotin
  • HY-W356117
    C6 NBD Glucosylceramide

    		Fluorescent Dye Others
    C6 NBD Glucosylceramide is a glucosylceramide fluorescent derivative (Ex=466 nm, Em=535 nm). C6 NBD Glucosylceramide can be used to study the metabolism and internalization of glucosylceramide and also for the determination of glucosyl ceramide synthase activity .
    C6 NBD Glucosylceramide
  • 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-P99192
    Emibetuzumab

    LY2875358

    		 c-Met/HGFR Cancer
    Emibetuzumab (LY2875358) is a humanized bivalent MET antibody (IgG4 type). Emibetuzumab shows high neutralization and internalization activities, resulting in inhibition of both HGF-dependent and HGF-independent MET pathway activation and tumor growth. Emibetuzumab can be used in study of cancer .
    Emibetuzumab
  • HY-P4096
    HAP-1

    		Bacterial Inflammation/Immunology
    HAP-1 is a synovial-targeted transduction peptide. HAP-1 facilitates specific internalization of protein complexes into human and rabbit synovial cells. HAP-1 fused to an antimicrobial peptide, (KLAK)2, to generate a proapoptotic peptide DP2 .
    HAP-1
  • HY-P99827
    Cobolimab

    TSR-022; GSK4069889

    		 Tim3 Cancer
    Cobolimab (TSR-022) is an anti-TIM-3 monoclonal antibody. Cobolimab mediates the internalization of TIM3 with an IC50 value of 0.4464 nM. Cobolimab has potential application in solid tumors and non-small cell lung cancer (NSCLC) .
    Cobolimab
  • HY-P5285
    Lunasin

    		Parasite Infection Inflammation/Immunology Cancer
    Lunasin is a bioactive peptide with antioxidant, anti-inflammatory, anticancer and anti-aging properties. Lunasin can be isolated from soybean. Lunasin also has an epigenetic mechanism of action associated with histone acetylation. Lunasin can be internalized into cells and inhibit Oncosphere formation in cancer cells .
    Lunasin
  • HY-161096
    Antitumor agent-127

    		ROR Cancer
    Antitumor agent-127 (compound 1) is a parent macrocyclic peptide. Antitumor agent-127 displays nanomolar cell-based binding to ROR1 and relatively good internalization in 786-O and MDA-MB-231 tumor cell lines .
    Antitumor agent-127
  • HY-100677
    VUF11207

    		CXCR Endocrinology
    VUF11207 (Compound 29) is a CXCR7 agonist and a high-potency CXCR7 (pKi of 8.1) ligand that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7 .
    VUF11207
  • HY-139950
    Rasarfin
    1 Publications Verification

    		 Ras Cancer
    Rasarfin is a dual Ras and ARF6 inhibitor .
    Rasarfin
  • HY-145314
    TC113

    		Integrin Cancer
    TC113 is a c(RGDyK)-Based conjugate of Gemcitabine (GEM). TC113 could be internalized by A549 cells through integrin αvβ3. TC113 shows potent antiproliferative properties against WM266.4 and A549 cells .
    TC113
  • 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-P99412
    Lusvertikimab

    OSE-127

    		 Interleukin Related Cancer
    Lusvertikimab (OSE-127) is a humanized IL7R monoclonal antibody. Lusvertikimab is not internalized by target cells and prevents IL7R heterodimerization and subsequent downstream signaling. Lusvertikimab has anti-leukemic efficacy and has the potential for B cell precursor acute lymphoblastic leukemia (BCP-ALL) research .
    Lusvertikimab
  • 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-W010907
    Pamoic acid disodium
    2 Publications Verification

    		 GPR35 ERK Neurological Disease
    Pamoic acid disodium is a potent GPR35 agonist with an EC50 value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively. Pamoic acid disodium potently recruits β-arrestin2 to GPR35 and has an antinociceptive effect .
    Pamoic acid disodium
  • HY-117665
    Fimaporfin

    TPCS2a

    		 Fluorescent Dye Cancer
    Fimaporfin (TPCS2a) is a photosensitizer that localizes to endosomes/lysosomes with an excitation wavelength of 420 nm and an emission wavelength between 640 and 680 nm .
    Fimaporfin
  • 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-D1602
    BODIPY FL-DHPE

    		Fluorescent Dye Others
    BODIPY FL DHPE is a green-fluorescent phospholipid probe. BODIPY FL DHPE labels lipid 1,2-dihexadecanoyl-sn-glycero-phosphoethanolamine (DHPE), labeled liposomes can be internalized by membrane fusion. BODIPY FL DHPE can be used for investigations of membrane surface and membrane fusion. (λex=505 nm, λem=511 nm) .
    BODIPY FL-DHPE
  • 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-15578G
    McMMAF

    Maleimidocaproyl monomethylauristatin F

    		 Drug-Linker Conjugates for ADC Cancer
    McMMAF GMP is a GMP grade McMMAF (HY-15578). McMMAF is a protective group (maleimidocaproyl)-conjugated MMAF, which is a potent tubulin polymerization inhibitor. McMMAF can be used as a agent-linker for antibody-drug conjugates (ADC). McMMAF is uncleavable, and must be internalized and degraded within a cell, releasing cysteine-McMMAF as the active agent .
    McMMAF
  • HY-P2336A
    CCZ01048 TFA

    		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-145287
    S-MGB-234

    		DNA/RNA Synthesis Parasite Infection
    S-MGB-234 is a minor groove binder of Animal African Trypanosomiasis (AAT). S-MGB-234 displays excellent in vitro activities against the principal causative organisms of AAT; Trypanosoma congolense, and Trypanosoma vivax. S-MGB-234 does not show cross-resistance with the current diamidine agents and are not internalized via the transporters used by diamidines .
    S-MGB-234
  • HY-151207
    Anticancer agent 81

    		Apoptosis ADC Cytotoxin Cancer
    Anticancer agent 81 (Compound 37b3) is an anticancer agent and can induce tumor cell cycle arrest and apoptosis. Anticancer agent 81 can be used as a payload to conjugate with Trastuzumab (HY-P9907) to obtain the antibody–agent conjugate (ADC) T-PBA. T-PBA maintained its mode of target and internalization ability of Trastuzumab .
    Anticancer agent 81
  • 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-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-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-10968A
    CYM5442 hydrochloride

    		LPL Receptor Neurological Disease
    CYM5442 hydrochloride is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 hydrochloride is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 hydrochloride activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 hydrochloride can easily penetrate the central nervous system (CNS) .
    CYM5442 hydrochloride
  • HY-10968
    CYM5442
    1 Publications Verification

    		 LPL Receptor Neurological Disease
    CYM5442 is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 can easily penetrate the central nervous system (CNS) .
    CYM5442
  • HY-P2106
    Elabela(19-32)
    3 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-P99956
    Zilovertamab vedotin

    VLS-101; MK-2140

    		 Antibody-Drug Conjugates (ADCs) Apoptosis Cancer
    Zilovertamab vedotin (VLS-101) is a novel antibody-drug conjugate comprising the humanized monoclonal antibody zilovertamab and and the anti-microtubule cytotoxin monomethyl vedotin. Zilovertamab vedotin binding to tumor cell ROR1 results in rapid internalization, trafficking to lysosomes, antibody–agent conjugate cleavage, and monomethyl vedotin release. Zilovertamab vedotin induces apoptosis. Zilovertamab vedotin can be used in research of cancer .
    Zilovertamab vedotin
  • HY-P10439
    CVRARTR

    		PD-1/PD-L1 Cancer
    CVRARTR is an antagonist for programmed cell death ligand-1 (PD-L1) with KD of 281 nM. CVRARTR induces the internalization of PD-L1 and downregulates PD-L1 on the cell surface. CVRARTR restores cytokine secretion and T cell proliferation in cell CT26. CVRARTR exhibits antitumor efficacy against in CT26 homograft mouse model .
    CVRARTR
  • HY-145287A
    S-MGB-234 TFA

    		DNA/RNA Synthesis Parasite Infection
    S-MGB-234 TFA is a minor groove binder used for African Animal Trypanosomiasis (AAT). S-MGB-234 exhibits excellent in vitro activity against the primary pathogens of AAT: Trypanosoma congolense and Trypanosoma vivax. S-MGB-234 TFA does not show cross-resistance with current diamidine active molecules and is not internalized via the transporters used by diamidines .
    S-MGB-234 TFA
  • HY-D1746
    EDTA-AM

    EDTA acetoxymethyl ester; Ethylenediaminetetraacetic acid acetoxymethyl ester

    		 Biochemical Assay Reagents Others
    EDTA-AM (ethylenediaminetetraacetic acid, acetoxymethyl ester) is the membrane-permeant form of the metal chelator EDTA (HY-Y0682). Live cells passively load EDTA-AM by incubating with EDTA-AM. Once internalized, cytoplasmic esterase decomposes AM esters, releasing the active ligand EDTA, which isolates metal ions within the cell. EDTA-AM induces an arrest of mitotic progression and chromosome decondensation .
    EDTA-AM
  • HY-P2106A
    Elabela(19-32) TFA
    3 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-132260
    Naratuximab emtansine

    IMGN529; Debio 1562

    		 Antibody-Drug Conjugates (ADCs) Apoptosis Cancer
    Naratuximab emtansine (IMGN529) is a CD37-targeted ADC consisting of a humanized IgG1 mAb coupled to the microtubule disruptor DM1. Naratuximab emtansine has high affinity and specificity for CD37, allowing ADC internalization, processing and intracellular release of DM1. Due to its ability to disrupt microtubule assembly, DM1 can subsequently induce cell cycle arrest and apoptosis .
    Naratuximab emtansine
  • HY-W008947
    SEW​2871
    4 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

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