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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
254 Results for "
internalization
" in MedChemExpress (MCE) Product Catalog:
Products (254)
254 Results for "internalization" in MCE Product Catalog:
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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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1 Cited Publications
Synonyms: Oxophenylarsine; PhAsO; Arsenosobenzene
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Phenylarsine oxide (PAO), an inhibitor of endocytosis, inhibits PTPε with an IC50 of 18 μM. Phenylarsine oxide (PAO) inhibits oxygen consumption and decreases cellular ATP content overlap with those used to inhibit protein internalization .
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Opioid Receptor G Protein-coupled Receptor Kinase (GRK) Mas-related G-protein-coupled Receptor (MRGPR)
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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 (MOR). CCG258747 attenuates IgE mediated anaphylaxis by inhibiting GRK2 and FcεRI signaling pathway but activates mast cells via MRGPRX2 and MRGPRB2. CCG258747 can be used to study diseases related to overexpression of GRK2 (such as heart failure, opioid tolerance) .
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1 Cited Publications
Cat. No.: HY-148152A
Purity: 98.15%
PSMA I&S TFA is a PSMA-targeted imaging agent. PSMA I&S TFA undergoes PSMA-mediated internalization into PSMA-expressing cells, with uptake into PSMA-positive tissues competitively inhibited by a potent PSMA inhibitor. PSMA I&S TFA can be used for the research of prostate cancer .
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1 Cited Publications
Cat. No.: HY-D1375
CAS No.: 2183440-44-8
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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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1 Cited Publications
Cat. No.: HY-P11143A
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Cardiovascular Disease Neurological Disease Inflammation/Immunology
Halcinonide (SQ-18566) is an orally active Smoothened (Smo) agonist. Halcinonide activates the Hedgehog signaling pathway by binding to Smo and promoting its internalization and expression, thereby activating Gli transcription factors. Halcinonide not only stimulates cell proliferation, increases the expression of cyclin D2/CDK6 and inhibits the degradation of caspase-3, but also suppresses Bcl-2/Bax-mediated apoptosis, oxidative stress and inflammatory responses. Halcinonide activates RxRγ to upregulate the expression of myelin genes, thereby reducing cerebral infarction and improving behavioral deficits. Halcinonide has been used in studies related to multiple sclerosis and ischemic stroke .
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Patritumab deruxtecan (HER3-DXd) is an antibody-drug conjugate (ADC) targeting HER3, consisting of the anti-HER3 IgG1 antibody Patritumab (HY-P99275), a cleavable tetrapeptide linker, and the membrane-permeable topoisomerase I (Topoisomerase Ⅰ) inhibitor DXd (HY-13631D). After binding to membrane-localized HER3, Patritumab deruxtecan is internalized into lysosomes, where the linker is cleaved to release DXd. DXd enters the nucleus to induce DNA damage and cell death, and exerts a bystander effect via transmembrane diffusion. Patritumab deruxtecan reduces the viability of HER3-positive cells and induces features of immunogenic cell death including CALR membrane exposure, ATP and HMGB1 release, and can be used in studies related to HER3-positive breast cancer and non-small cell lung cancer .
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1 Cited Publications
Cat. No.: HY-P1206
CAS No.: 174688-78-9
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CH 275 is a peptidic somatostatin analog that acts as an agonist of SST1 (IC50 = 30.9 nM, Ki = 52 nM). The IC50 values of CH 275 for sst3, sst4, sst2, and sst5 are 345 nM, >1 μM, >10 μM, and >10 μM, respectively. CH 275 binds to SSTR1 via the IAmp9-Asp137 ion pair interaction and the hydrophobic interaction between the isopropyl group of IAmp9 and Leu107, and reduces the extracellular acidification rate. CH 275 induces weak sst1 internalization, exerts immunosuppressive effects on macrophages, and decreases macrophage viability, MCP-1 expression/secretion, and IL-8 secretion, but does not alter proMMP-9 secretion or IL-8 mRNA levels. CH 275 reduces hippocampal β-amyloid levels and alleviates plaque pathology without inducing hippocampal microglial activation. CH 275 is used in research on Alzheimer's disease, Parkinson's disease, and depression .
Cat. No.: HY-P99778
CAS No.: 946415-62-9
Synonyms: MORAb-004
Cat. No.: HY-P99192
CAS No.: 1365287-97-3
Synonyms: LY2875358
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Cat. No.: HY-P5362
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Cat. No.: HY-P5285
CAS No.: 496823-34-8
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FAPI-34 is a SPECT imaging agent targeting FAP. FAPI-34 specifically binds to FAP, is highly internalized by FAP-expressing cells, accumulates in FAP-expressing tumor lesions, and shows low uptake in normal tissues except the kidneys. FAPI-34 is applicable for tumor-related research .
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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 .
Cat. No.: HY-P9990
CAS No.: 2407378-48-5
Synonyms: BIIB059
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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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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
