Search Result
Results for "
internalization
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-144258
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PD-1/PD-L1
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Inflammation/Immunology
Cancer
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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 .
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- HY-139690
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Opioid Receptor
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Cardiovascular Disease
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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 .
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- HY-111793A
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CXCR
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Neurological Disease
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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 .
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- HY-111793
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CXCR
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Neurological Disease
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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 .
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- HY-144347
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CXCR
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Infection
Cancer
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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 .
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- HY-N1166
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Deguelinol I; Hydroxydeguelin
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Tephrosin is a natural rotenoid which has potent antitumor activities. Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors .
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- HY-106481
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GPR35
Histamine Receptor
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Inflammation/Immunology
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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 .
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- HY-163079
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FAP
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Cancer
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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 .
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- HY-P10085
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PKC
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Inflammation/Immunology
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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 .
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- HY-144793
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Others
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Cancer
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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 .
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- HY-W356117
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Fluorescent Dye
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Others
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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 .
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- HY-116088
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LPL Receptor
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Inflammation/Immunology
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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 .
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- HY-15578
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McMMAF
4 Publications Verification
Maleimidocaproyl monomethylauristatin F
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Drug-Linker Conjugates for ADC
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Cancer
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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 .
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- HY-P99192
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LY2875358
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c-Met/HGFR
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Cancer
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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 .
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- HY-P99827
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TSR-022; GSK4069889
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Tim3
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Cancer
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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) .
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- HY-P5285
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Parasite
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Infection
Inflammation/Immunology
Cancer
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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 .
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- HY-161096
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ROR
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Cancer
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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 .
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- HY-145314
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Integrin
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Cancer
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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 .
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- HY-P3717
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Ephrin Receptor
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Cancer
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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 .
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- HY-139950
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Ras
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Cancer
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Rasarfin is a dual Ras and ARF6 inhibitor .
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- HY-P99412
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OSE-127
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Interleukin Related
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Cancer
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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 .
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- HY-124071
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Formyl Peptide Receptor (FPR)
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Inflammation/Immunology
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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 .
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- HY-W010907
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GPR35
ERK
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Neurological Disease
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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 .
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- HY-139413
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Toll-like Receptor (TLR)
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Cancer
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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 .
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- HY-D1602
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Fluorescent Dye
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Others
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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) .
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- HY-P3852
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SPR393-407
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Neurokinin Receptor
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Neurological Disease
Inflammation/Immunology
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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 .
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- HY-15578G
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Maleimidocaproyl monomethylauristatin F
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Drug-Linker Conjugates for ADC
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Cancer
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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 .
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- HY-P2336A
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Melanocortin Receptor
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Cancer
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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 .
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- HY-145287
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DNA/RNA Synthesis
Parasite
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Infection
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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 .
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- HY-151207
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Apoptosis
ADC Cytotoxin
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Cancer
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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 .
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- HY-160045
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Cholecystokinin Receptor
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Cancer
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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 .
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- HY-117665
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TPCS2a
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Others
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Cancer
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Fimaporfin (TPCS2a) is an endosomal/lysosomal-localizing photosensitizer .
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- HY-101265
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S1p receptor agonist 1
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LPL Receptor
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Inflammation/Immunology
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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.
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- HY-P2336
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Melanocortin Receptor
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Cancer
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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 .
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- HY-12005
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FTY720
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LPL Receptor
PAK
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Inflammation/Immunology
Cancer
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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 .
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- HY-P2106
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Arrestin
Apelin Receptor (APJ)
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Cardiovascular Disease
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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 .
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- HY-P99956
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VLS-101; MK-2140
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Antibody-Drug Conjugates (ADCs)
Apoptosis
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Cancer
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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 .
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- HY-D1746
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EDTA acetoxymethyl ester; Ethylenediaminetetraacetic acid acetoxymethyl ester
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Biochemical Assay Reagents
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Others
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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 .
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- HY-10968A
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LPL Receptor
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Neurological Disease
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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) .
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- HY-10968
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LPL Receptor
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Neurological Disease
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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) .
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- HY-P2106A
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Apelin Receptor (APJ)
Arrestin
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Cardiovascular Disease
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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 .
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- HY-W008947
-
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LPL Receptor
ERK
Akt
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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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 .
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- HY-101939
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LPL Receptor
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Neurological Disease
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RP-001 is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 induces internalization and polyubiquitination of S1P1. RP-001 has little activity on S1P2-S1P4 and only moderate affinity for S1P5 .
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- HY-101939A
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LPL Receptor
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Neurological Disease
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RP-001 hydrochloride is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 hydrochloride induces internalization and polyubiquitination of S1P1. RP-001 hydrochloride has little activity on S1P2-S1P4 and only moderate affinity for S1P5 .
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- HY-131683
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Others
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Others
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ES9-17 is an analog of ES9 (endosidin9), which is an inhibitor of clathrin heavy chain (CHC). ES9-17 is an inhibitor of clathrin-mediated endocytosis (CME), a major route for internalization of plasma membrane proteins and molecules from the extracellular environment in plants. ES9-17 inhibits the uptake of transferrin and FM4-64. ES9-17 also inhibits root growth of Arabidopsis seedings .
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- HY-12005R
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FTY720 (Standard)
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LPL Receptor
PAK
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Inflammation/Immunology
Cancer
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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 .
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- HY-158033
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LYTACs
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Cancer
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Biotin-εNle-CKCKC-γAbu-CKCKCG-NH2 (Compound 24, Cys modified with M6Pn) is a mannose-6-phosphate (M6Pn)-peptide conjugate capable of binding to targeted ligands of various proteins and successfully internalizing and degrading them through M6PR. Biotin-εNle-CKCKC-γAbu-CKCKCG-NH2 can be utilized in the research of lysosomal targeting chimeras (LYTACs) based on M6Pn .
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- HY-141832
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mGluR
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Neurological Disease
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mGluR5 modulator 1 is a mGluR5 positive allosteric modulator. mGluR5 modulator 1 can be used for the research of the schizophrenia and cognitive impairments .
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- HY-N6727
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Aspergillin
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Apoptosis
PKA
NF-κB
Bacterial
Fungal
Antibiotic
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Infection
Inflammation/Immunology
Cancer
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Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis . Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells . Gliotoxin is a potent NOTCH2 transactivation inhibitor, can effectively induce apoptosis of chronic lymphocytic leukemia (CLL) cells .
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- HY-108556A
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Protease Activated Receptor (PAR)
Apoptosis
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Cardiovascular Disease
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RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis .
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- HY-108556
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Protease Activated Receptor (PAR)
Apoptosis
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Cardiovascular Disease
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RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 inhibits angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 induces cell apoptosis .
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- HY-152240
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PD-1/PD-L1
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Cancer
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PD-1/PD-L1-IN-29 (S4-1) is a potent PD-1/PD-L1 inhibitor with an IC50 value of 6.1 nM. PD-1/PD-L1-IN-29 binds PD-L1 and disrupts PD-1/PD-L1 interactions, induces PD-L1 dimerization and internalization, improves its localization to the endoplasmic reticulum, and promotes PD-L1 entry into the endoplasmic reticulum. PD-1/PD-L1-IN-29 has anticancer activity .
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- HY-153360
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Drug-Linker Conjugates for ADC
Topoisomerase
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Cancer
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MC-GGFG-AM-(10Me-11F-Camptothecin) is a linker-payload conjugate used to synthesize ZW251. ZW251 an antibody-drug conjugate (ADC) targeting human GPC3. ZW251 consists of a humanized IgG1 antibody conjugated to a novel camptothecin-based topoisomerase 1 inhibitor, ZD06519, via a linker. The linker is the maleimide anchor and a glycyl glycyl phenylalanyl glycine (GGFG)-aminomethyl (AM) cleavable linker. ZW251 has high affinity with human and cynomolgus monkey GPC3. ZW251 displays rapid internalization in GPC3-expressing HCC cell lines, and bystander-mediated killing of GPC3 negative cancer cells .
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Cat. No. |
Product Name |
Type |
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- HY-W356117
-
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Fluorescent Dyes/Probes
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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 .
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- HY-D1602
-
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Fluorescent Dyes/Probes
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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) .
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- HY-D1746
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EDTA acetoxymethyl ester; Ethylenediaminetetraacetic acid acetoxymethyl ester
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Fluorescent Dyes/Probes
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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 .
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- HY-15578G
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Maleimidocaproyl monomethylauristatin F (GMP)
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Fluorescent Dye
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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 .
|
Cat. No. |
Product Name |
Type |
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- HY-139413
-
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Biochemical Assay Reagents
|
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 .
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- HY-15578G
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Maleimidocaproyl monomethylauristatin F (GMP)
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Biochemical Assay Reagents
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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 .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P4098
-
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Peptides
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Others
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SynB1 is a cell penetrating polypeptide, internalized by, or is associated with lipid vesicle (LV). SynB1 can be used to lipid vesicle-mediated delivery to cells .
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- HY-P10155
-
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Peptides
|
Others
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VT5 is a β-sheet amphipathic peptide consisting of 26 amino acids. VT5 has the ability to form β-sheets for cellular internalization .
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- HY-P10085
-
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PKC
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Inflammation/Immunology
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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 .
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- HY-P4096
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Peptides
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Inflammation/Immunology
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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 .
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- HY-P5285
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Parasite
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Infection
Inflammation/Immunology
Cancer
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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 .
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- HY-P3717
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Ephrin Receptor
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Cancer
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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 .
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- HY-P3852
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SPR393-407
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Neurokinin Receptor
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Neurological Disease
Inflammation/Immunology
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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 .
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- HY-P2336A
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Melanocortin Receptor
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Cancer
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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 .
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- HY-P2336
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Melanocortin Receptor
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Cancer
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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 .
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- HY-P2106
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Arrestin
Apelin Receptor (APJ)
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Cardiovascular Disease
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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 .
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- HY-P2106A
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Apelin Receptor (APJ)
Arrestin
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Cardiovascular Disease
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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 .
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- HY-P6020
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Peptides
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Others
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HBpep-SA is a cell membrane-permeable peptide condensate that phase separates to form stable droplets at pH values below 6.5. HBpep-SA is able to directly and efficiently deliver a variety of macromolecules, ranging from therapeutic peptides as small as 726 Da to large enzymes as large as 430 kDa, and the loaded condensates remain stable under near-physiological and serum conditions until internalized by cells. HBpep-SA can be used for intracellular delivery of large numbers of macromolecules and as a vector for mRNA-based vaccines .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99778
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MORAb-004
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Inhibitory Antibodies
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Cancer
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Ontuxizumab (MORAb-004) is a humanized IgG1/κ anti-endosialin (TEM-1 or CD248) monoclonal antibody with antitumor effects. Ontuxizumab can be used for the research of cancer .
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- HY-P99192
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LY2875358
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c-Met/HGFR
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Cancer
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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 .
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- HY-P99827
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TSR-022; GSK4069889
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Tim3
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Cancer
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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) .
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- HY-P99412
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OSE-127
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Interleukin Related
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Cancer
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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 .
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- HY-P99306
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DS 1024; Sym 004
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Inhibitory Antibodies
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Cancer
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Modotuximab (Anti-Human EGFR Recombinant Antibody) is an IgG1κ-type chimeric antibody targeting human EGFR protein. Modotuximab contains a portion of Futuximab that binds to two independent, non-overlapping epitopes on EGFR. Modotuximab promotes cross-linking of EGFR on the cell surface and promotes EGFR cellular internalization and degradation. Modotuximab has antitumor activity in vivo .
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- HY-P99956
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VLS-101; MK-2140
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Antibody-Drug Conjugates (ADCs)
Apoptosis
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Cancer
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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 .
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- HY-P99189
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IMC-A12; NSC742460
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Inhibitory Antibodies
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Cancer
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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 .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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