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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
115 Results for "
surface expression
" in MedChemExpress (MCE) Product Catalog:
Products (115)
115 Results for "surface expression" in MCE Product Catalog:
Cat. No.: HY-181967
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PROTAC PARP1 degrader-5 is a PARP1 PROTAC degrader with a DC50 of 0.12 μM. PROTAC PARP1 degrader-5 hijacks the ubiquitin-proteasome system via catalytic ternary complex formation to drive sustained PARP1 degradation. PROTAC PARP1 degrader-5 induces DNA damage, drives marginal cytosolic double-stranded DNA accumulation in tumor cells, and up-regulates PD-L1 surface expression in tumor cells. PROTAC PARP1 degrader-5 shows tumor growth inhibition activity in murine melanoma models when encapsulated in lipid nanoparticles. PROTAC PARP1 degrader-5 can be used for the research of cancer, such as melanoma .
Cat. No.: HY-184897
CAS No.: 312724-83-7
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YS-01 is an inhibitor of pendrin (SLC26A4) with pulmonary protective activity. YS-01 inhibits pendrin-mediated anion exchange activity, reduces pendrin expression, and suppresses the activation of NF-κB and the production of proinflammatory cytokines. YS-01 alleviates lipopolysaccharide-induced and ventilator-induced lung injury. YS-01 attenuates ovalbumin-induced airway hyperresponsiveness, inflammatory infiltration, epithelial thickening and goblet cell hyperplasia, and reduces eosinophil and neutrophil counts. YS-01 decreases MUC5AC transcription levels induced by IL-4, reverses the reduction of airway surface liquid volume, and inhibits the increase of apical SCN − concentration in epithelial cells. YS-01 can be used in studies related to lung injury and allergic asthma .
Cat. No.: HY-109061A
CAS No.: 2411549-88-5
Synonyms: YH25448 mesylate hydrate; GNS-1480 mesylate hydrate
Lazertinib (YH25448; GNS-1480) mesylate hydrate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate hydrate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate hydrate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate hydrate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate hydrate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
Cat. No.: HY-177204
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DSPE-PEG2000-WLSEAGPVVTVRALRGTGSW is a polypeptide targeting tenascin-X (Tenascin-X) that can be conjugated with liposomes and exosomes. DSPE-PEG2000-WLSEAGPVVTVRALRGTGSW specifically binds to Tenascin-X on the surface of cardiomyocytes, mediates receptor-dependent uptake of nanocarriers, enhances targeted drug delivery of cargo to cardiomyocytes, and increases drug accumulation in cardiac tissue. DSPE-PEG2000-WLSEAGPVVTVRALRGTGSW protects cardiomyocytes treated with LPS, alleviates oxidative stress, repairs mitochondrial function, inhibits ferroptosis and apoptosis, and downregulates the secretion of pro-inflammatory cytokines at the same time. DSPE-PEG2000-WLSEAGPVVTVRALRGTGSW improves cardiac injury and pathological morphology in mice with sepsis-induced cardiomyopathy, restores GPX4 expression, and promotes the internalization of cardiomyocyte-derived exosomes, making it suitable for related research on sepsis-induced cardiomyopathy, myocardial ischemia-reperfusion injury, and other conditions .
Cat. No.: HY-183905
CAS No.: 1401564-00-8
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KR-67607 is a selective 11β-HSD1 inhibitor, with an IC50 value of 4.8 nM against h11β-HSD1 and 7.1 nM against mouse 11β-HSD1. KR-67607 inhibits stress-induced Glucocorticoid receptor nuclear translocation, reduces cortisol levels, suppresses the expression of ROS and proinflammatory cytokines, and enhances Nrf-2-mediated antioxidant gene transcription. KR-67607 maintains trabecular meshwork structure and reverses elevated intraocular pressure. KR-67607 improves ocular antioxidant activity and mucus secretion, reverses ocular surface damage, and prevents ischemia-reperfusion induced ocular injury. KR-67607 can be used in research related to glaucoma and dry eye disease .
Cat. No.: HY-N4246
CAS No.: 382148-47-2
Cat. No.: HY-P99899
CAS No.: 2052591-32-7
Synonyms: PR-1498487
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Cat. No.: HY-181588
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NR4A agonist-2 is a selective pan-NR4A agonist designed based on Vidofludimus (HY-14908), with a Kd of 0.10 μM against NR4A1, and EC50 values of 0.098 μM, 0.092 μM and 0.09 μM against Nur77, Nurr1, NOR-1, respectively. NR4A agonist-2 exhibits 47-fold selectivity over DHODH, and shows no cytotoxic activity at concentrations up to 10 μM. By binding to a specific surface pocket in the ligand-binding domain of Nurr1, NR4A agonist-2 inhibits the formation of Nurr1 homodimers, activates response elements such as NBRE, NurRE, DR5, and then potently induces the expression of neuroprotective genes including BDNF, SOD2, thereby exerting neuroprotective activity. NR4A agonist-2 can be used in the research of neurodegenerative diseases such as Parkinson's disease, dementia and multiple sclerosis .
Cat. No.: HY-P5832
CAS No.: 836606-84-9
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Cat. No.: HY-L211
86 compounds
Hormones are a class of biologically active substances secreted by endocrine gland cells, which are transported through the circulatory system to various parts of the body, and precisely act on specific target organs or cells, playing a crucial role in regulating the growth, development, metabolism, and reproduction of organisms. The mechanisms of hormone action are diverse and complex. Some hormones (such as corticosteroids, vitamin D, and thyroid hormones) can enter the cell interior and interact with receptors in the nucleus, thereby regulating gene expression and affecting cell function. Other hormones (such as growth hormone and thyrotropin-releasing hormone) bind directly to receptors on the cell surface, exerting their effects by regulating enzyme activity or influencing the state of ion channels. Additionally, hormones play a key role in the study of endocrine and metabolic diseases, and are closely related to the development of diseases such as diabetes and thyroid diseases.
MCE has included 86 human hormone compounds, which is of great significance for the study of human metabolic pathways, and can also be used to build a metabonomics database.
Cat. No.: HY-177414
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BB-1701 is an anti-HER2 antibody-drug conjugate (ADC). BB-1701 consists of a humanized anti-HER2 antibody (Trastuzumab) (HY-P9907), a linker (Mal-PEG2-VCP), and a microtubule inhibitor (Eribulin) (HY-13442), with the drug-linker conjugate of the ADC being Mal-PEG2-VCP-Eribulin (HY-128870). BB-1701 exhibits potent cytotoxicity against various cancer cells, shows a remarkable bystander effect, and induces immunogenic cell death (upregulated cell surface expression of calreticulin, release of ATP/HMGB1, macrophage infiltration) and apoptosis. BB-1701 potently inhibits tumor growth in T-DM1/T-DXd-resistant tumor models. BB-1701 can be used in studies related to breast cancer, gastric cancer, non-small cell lung cancer, and heterogeneous mixed tumors .
Cat. No.: HY-N4246R
CAS No.: 382148-47-2
Cat. No.: HY-177300
CAS No.: 1402802-45-2
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TLR7/8 agonist 13 is an orally active dual agonist of TLR7 (lowest effective concentrations (LEC) [hTLR7] = 1.6 μM) and TLR8 (LEC [hTLR8] = 1.6 μM). TLR7/8 agonist 13 exhibits agonistic activity against human peripheral blood mononuclear cells (hPBMCs) (LEC [hPBMC] = 0.5 μM). TLR7/8 agonist 13 induces endogenous IFNα, activating myeloid dendritic cells and monocytes toward a TH1 phenotype in mice and cynomolgus monkeys. TLR7/8 agonist 13 reduces viral load and HBV surface antigen expression in a mouse model of chronic AAV-HBV infection. TLR7/8 agonist 13 has the potential to indirectly induce IFNγ, which may promote HBV antigen-specific CD8 T cell-mediated responses. TLR7/8 agonist 13 can be used to study hepatitis B virus .
Cat. No.: HY-165613
CAS No.: 656831-18-4
Synonyms: Dipalmitoyl-S-glyceryl-cysteine; S-[2,3-Bis(palmitoyloxy)propyl]cysteine
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Pam2Cys (Dipalmitoyl-S-glyceryl-cysteine; S-[2,3-Bis(palmitoyloxy)propyl]cysteine) is a TLR2 agonist and immunostimulant. Pam2Cys binds to TLR2 to activate dendritic cells and trigger the TLR2-dependent NF-κB signaling pathway. Pam2Cys also induces dendritic cell maturation by upregulating the expression of cell surface MHC II molecules. Pam2Cys activates innate immune signaling pathways, drives pro-inflammatory and antimicrobial responses, enhances the expression of macrophage activation markers, increases phagocytic activity, induces the release of IL-12 and pro-inflammatory cytokines, and polarizes macrophages into a pro-inflammatory, antimicrobial phenotype without interfering with IL-10-induced macrophage polarization. Pam2Cys also serves as the lipid moiety in synthetic lipopeptide vaccines and possesses self-adjuvant properties. Pam2Cys enhances the immunogenicity of conjugated peptide segments and induces cellular and humoral immune responses. However, it does not activate CD4 T cells in mouse splenocyte cultures when used alone. Pam2Cys activates pulmonary TLR2 signaling pathways, triggers innate immune responses, recruits neutrophils and macrophages, induces the secretion of various cytokines, alleviates symptoms and damages associated with influenza A virus infection in mice without impairing adaptive immunity. Pam2Cys can be used in studies related to tuberculosis and influenza A virus infection .
Cat. No.: HY-L917
5,619 compounds
RNA is crucial for the regulation of numerous cellular processes and functions. With the in-depth study of disease mechanisms, processes such as RNA expression, splicing, translation, and stability regulation have become new targets for disease intervention. RNA has provided new therapeutic modalities for metabolic diseases, genetic disorders, and cancer patients, resulting in several innovative drugs.
MCE R&D team collected small molecules targeting RNA from the PDB, R-BIND, ROBIN, and internal database as the positive dataset, and non-targeting RNA small molecules from ROBIN as the negative dataset. Based on the GeminiMol pre-trained model, we encoded the molecules and calculated over 1700 molecular descriptors using Mordred as inputs for the model. Subsequently, we employed 13 deep learning models to learn from the data. All of which yielded good training results, with AUROCs greater than 0.75. Ultimately, we selected the Finetune model to screen HY-L901P, which exhibited the best classification performance, achieving an AUROC of 0.82 and a prediction accuracy of 0.76. We then applied filtering based on StaR rules (with at least two of the following properties: cLogP ≥ 1.5, Molar Refractivity ≥ 4, Relative Polar Surface Area ≤ 0.3) to obtain a library containing approximately 5,000 small molecule compounds targeting RNA. This library serves as a valuable tool for screening small molecules that interact with RNA.
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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
