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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
408 Results for "
integrity
" in MedChemExpress (MCE) Product Catalog:
Products (408)
408 Results for "integrity" in MCE Product Catalog:
Cat. No.: HY-P12080
CAS No.: 176365-43-8
Target:
Research Areas:
Cardiovascular Disease Metabolic Disease Inflammation/Immunology
pUR4 is a recombinant peptide that acts as a fibronectin (FN) inhibitor. pUR4 binds to the N-terminal type I modules of fibronectin, inhibiting the polymerization of soluble fibronectin and its deposition into the extracellular matrix (ECM). pUR4 reduces β1 integrin activation by depleting ECM fibronectin and disrupting FN-β1 integrin coupling. pUR4 attenuates TNF-α-induced endothelial hyperpermeability, maintains endothelial monolayer integrity, and reduces TNF-α-induced cell morphological changes. pUR4 decreases neutrophil adhesion to cardiac endothelial cells, T cell interstitial migration, immune cell infiltration, collagen deposition, and fibroblast activation. pUR4 can be used in research on pathological vascular leakage, heart failure, inflammation, chronic kidney disease, liver fibrosis, and intestinal fibrosis .
Cat. No.: HY-W019704R
CAS No.: 1115-47-5
Cat. No.: HY-W709349S
Synonyms: D 9998-d6 hydrochloride
Cat. No.: HY-17001AR
CAS No.: 56995-20-1
Synonyms: D 9998 (Standard)
Research Areas:
Flupirtine (Standard) (D 9998 (Standard)) is the analytical standard of Flupirtine (HY-17001A). This product is intended for research and analytical applications. Flupirtine is an orally active, blood-brain barrier-crossing non-opioid analgesic and neuroprotective agent. Flupirtine is a neuronal potassium channel opener (Kv7 activator), a NMDA receptor antagonist and a GABA receptor activator. Flupirtine stabilizes blood-brain-barrier integrity, reduces oxidative stress and brain leukocyte infiltration, enhances angioneurogenesis, suppresses calcium influx, stabilizes neuronal resting membrane potential, and counteracts focal cerebral ischemia. Flupirtine exhibits analgesic, muscle relaxant properties, protects neurons from excitotoxic, ischemic, or cytokine-mediated death. Flupirtine functions as a non-opioid analgesic without antipyretic or antiphlogistic properties, shows no relevant affinity to opiate receptor. Flupirtine can be used for the research of focal cerebral ischemia, pain, Alzheimer’s disease, or multiple sclerosis .
Cat. No.: HY-183393
CAS No.: 1798292-13-3
NVP-BHS345 is an ATP-competitive TORC1/TORC2 inhibitor with an IC50 of 1 μM for both targets in yeast. NVP-BHS345 acutely inhibits TORC1/TORC2 kinase activity, even in genetically engineered TOR1 M2282T Saccharomyces cerevisiae strains. NVP-BHS345 also reduces the phosphorylation levels of Ser-232/Ser-233 sites in Sch9, Ypk1/Ypk2 and Rps6, and induces hyperphosphorylation of Slt2 and activation of the cell wall integrity pathway. NVP-BHS345 causes depolarization of the actin cytoskeleton, blocks fluid-phase endocytosis, prevents the accumulation of vacuolar lipophilic dyes, and regulates the phosphorylation levels of Ent1, Pan1, Prk1, Akl1 and other cellular proteins .
Cat. No.: HY-N20708
CAS No.: 89353-99-1
Target:
Cat. No.: HY-P10159
CAS No.: 1809102-71-3
Target:
Research Areas:
DJK-5 is an antimicrobial peptide that targets and degrades guanosine pentaphosphate and tetraphosphate (pppGpp and ppGpp). DJK-5 kills bacteria within dentinal tubules, dental plaque and preformed oral biofilms, delays biofilm recovery, reduces the abundance of extracellular polysaccharides and the structural integrity of biofilm matrices, and inhibits the formation and biomass accumulation of dental plaque biofilms. DJK-5 permeabilizes bacterial membranes, induces bacterial morphological changes, inhibits bacterial growth, and exerts a synergistic effect on bacterial biofilms when used in combination with traditional antibiotics and Colistin (HY-113678). DJK-5 exhibits protease resistance and broad-spectrum antibiofilm activity, though its activity decreases in fetal bovine serum. DJK-5 can be used in studies of pulpitis, mixed biofilm infections, skin abscesses, dental caries, infections associated with failed root canal therapy, and Pseudomonas aeruginosa biofilm-related respiratory tract infections .
Cat. No.: HY-P1615
CAS No.: 1006388-38-0
Synonyms: UPARANT
Cat. No.: HY-P2302
CAS No.: 136661-76-2
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Research Areas:
Cat. No.: HY-159607
CAS No.: 2755761-78-3
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PRT3789 is a selective SMARCA2 PROTAC degrader (DC50 in HeLa cell: 0.72 nM for SMARCA2, 14 nM for SMARCA4). PRT3789 forms a stable ternary complex with Von Hippel-Lindau (VHL) E3 ligase, induces polyubiquitination at SMARCA2-specific lysine residues, and drives proteasome-dependent SMARCA2 degradation. PRT3789 disrupts SWI/SNF chromatin remodeling complex integrity, induces dissociation of specific subunits, suppresses oncogenic gene expression, reduces chromatin accessibility, and upregulates antigen processing/presentation-related gene expression. PRT3789 induces synthetic lethality, inhibits proliferation and colony formation, and drives tumor growth inhibition and regression in SMARCA4-deficient contexts. PRT3789 can be used for the research of SMARCA4-mutated solid tumors, non-small cell lung cancer, endometrial cancer, colorectal cancer, bladder cancer, esophageal cancer, ovarian cancer, and gastric cancer .
Cat. No.: HY-17539
CAS No.: 1421919-75-6
Research Areas:
KPT-276 is an orally active and blood-brain barrier-penetrant selective XPO1/CRM1 inhibitor. KPT-276 blocks XPO1-mediated nuclear export function and promotes nuclear retention of various tumor suppressor proteins. KPT-276 induces apoptosis and G1 cell cycle arrest in tumor cells, and downregulates c-MYC, CDC25A, and BRD4. KPT-276 reduces immune cell proliferation through nuclear accumulation of cell cycle inhibitors, rescues TDP-43 cytoplasmic mislocalization, and restores axon growth and growth rate in mutant PFN1 motor neurons. KPT-276 maintains axonal cytoskeletal integrity and mitochondrial function, and inhibits tumor growth. KPT-276 can be used for research on glioblastoma, non-Hodgkin lymphoma, amyotrophic lateral sclerosis, multiple myeloma, and non-small cell lung cancer .
Target:
Research Areas:
Bis-PEG4-NHS ester is a crosslinking reagent and amine-reactive modulator .Bis-PEG4-NHS ester reacts with primary amine groups on liposome surfaces via amide bond formation to covalently attach dibenzylcyclooctyne groups, with a hydrophilic PEG4 spacer reducing steric hindrance for subsequent click chemistry .Bis-PEG4-NHS ester enables site-specific antibody coupling to liposome surfaces via copper-free strain-promoted alkyne-azide cycloaddition click chemistry without disrupting liposome structure in minimal organic solvent volumes .Bis-PEG4-NHS ester undergoes hydrolysis during annealing to form -COOH groups that interact with PbI and FAI to enhance perovskite structural integrity, passivate defects, and modulate nucleation kinetics to regulate crystal growth .Bis-PEG4-NHS ester enhances device efficiency and long-term stability when used as an antisolvent additive for p-i-n perovskite solar cells .
Cat. No.: HY-L915
422 compounds
Lysine is the second most common target residue used in the design of TCIs and related covalent ligands. Its appeal lies in its abundance in human proteins, which is approximately three times higher than that of cysteine (5.8% vs. 1.9%). This significantly increases the number of proteins suitable for covalent targeting, especially given that many human proteins lack ligandable cysteine residues. Moreover, it has been suggested that functional lysines have a lower probability of being replaced by mutation, as they often play a crucial role in catalysis by acting as bases or nucleophiles. Additionally, lysines are essential for maintaining the structural integrity of proteins and for regulating post-translational modifications (PTMs). Consequently, targeting lysine has garnered significant interest in recent years.
Through careful selection, we constructed a structural filter containing over 110 electrophilic groups. By analyzing the electrophilic fragments selected by the structural filter, we removed any molecules with trivial or undesirable structural features. Ultimately, we obtained 445 fragment molecules which can target lysine residue and can be used for fragment-based covalent drug discovery.
Synonyms: 18α-Glycyrrhizic acid Magnesium hydrate; 18α-GA Magnesium hydrate; 18α-Licorice-saponin H2 Magnesium hydrate
Target:
SOD PPAR Carnitine Palmitoyltransferase (CPT) HIV Reactive Oxygen Species (ROS) Keap1-Nrf2 Heme Oxygenase (HO) NOD-like Receptor (NLR) Interleukin Related Pyroptosis Autophagy NF-κB TNF Receptor
Research Areas:
Magnesium isoglycyrrhizinate hydrate (18α-Glycyrrhizic acid Magnesium hydrate; 18α-GA Magnesium hydrate; 18α-Licorice-saponin H2 Magnesium hydrate) is a derivative of glycyrrhizic acid with oral activity. Magnesium isoglycyrrhizinate hydrate exhibits antioxidant, anti-inflammatory, hepatoprotective and cardioprotective activities. Magnesium isoglycyrrhizinate hydrate protects against ethanol-induced alcoholic liver disease in rats by upregulating the expression levels of SOD, GSH, PPAR-α and CPT-1 . Magnesium isoglycyrrhizinate hydrate shows cytotoxicity against T lymphocytes and inhibits HIV-1 replication in these cells . Magnesium isoglycyrrhizinate hydrate alleviates oxidative stress by reducing the levels of ROS, Nrf2, HO-1 and p-P65, and alleviates pyroptosis by downregulating the expression levels of NLRP3, GSDMD-N, P20 and c-IL-1β. Magnesium isoglycyrrhizinate hydrate inhibits autophagy, colonic fibrosis and myocardial fibrosis, and regulates intestinal barrier integrity. Magnesium isoglycyrrhizinate hydrate can be used in research related to alcoholic liver disease, HIV-1 infection, hepatotoxicity, acute liver failure, inflammatory bowel disease and myocardial fibrosis .
Cat. No.: HY-B0819
CAS No.: 14816-18-3
Target:
Insecticide Cholinesterase (ChE) Cytochrome P450 Autophagy Reactive Oxygen Species (ROS) Apoptosis Bcl-2 Family Caspase COX Keap1-Nrf2 TNF Receptor Interleukin Related Bacterial
Research Areas:
Phoxim is an organophosphorus pesticide and an orally active inhibitor of cholinesterase and CYP3A, which induces neurotoxicity in Caenorhabditis elegans and causes nephrotoxicity characterized by glomerular atrophy and interstitial fibrosis. Phoxim induces inhibition of the autophagy pathway. Phoxim induces dopaminergic neuron degeneration and exacerbates Aβ-induced paralysis. Phoxim damages enterocytes and disrupts intestinal barrier integrity. Phoxim induces ROS accumulation. Phoxim induces mitochondrial apoptosis, involving upregulation of Bad, Bax, caspase-3, and caspase-9 and downregulation of Bcl-2. Phoxim inhibits mitochondrial functional enzymes (COX, Ca 2+-Mg 2+-ATPase, SDH). Phoxim upregulates Nrf2 mRNA expression in the jejunal mucosa. Phoxim increases TNF-α and decreases IL-6 and IL-8 in the intestinal mucosa. Phoxim alters gut microbial composition by increasing total bacteria and Escherichia coli and reducing Lactobacillus. Phoxim enhances energy metabolism in silver carp by upregulating key glycolytic and gluconeogenic enzymes. Phoxim is used in research on neurodegenerative diseases, nephrotoxicity, intestinal oxidative stress and barrier dysfunction, and bacterial sepsis .
Cat. No.: HY-P11242
Research Areas:
Cat. No.: HY-30234B
CAS No.: 17162-20-8
Target:
Research Areas:
Infection Neurological Disease Inflammation/Immunology Endocrinology
Clemizole sulfate is an orally active, blood-brain barrier permeable TRPC5 inhibitor, with an IC50 value of 1.05-1.34 μM against mouse TRPC5. Clemizole sulfate blocks TRPC1:TRPC5, TRPC3, TRPC4, TRPC6, TRPC7, hERG, hKCNQ1/hKCNE1 and hKv1.5 channels, and activates TRPA1; it modulates 5HT-2B and HTR2A receptors; it inhibits HCV RNA replication, CrtN enzymatic activity, oxidative stress, neuroinflammation, cell apoptosis and bacterial virulence; it maintains blood-brain barrier (BBB) integrity; it enhances DNA repair capacity; it improves cell viability; and it alters cardiac electrophysiological properties. Clemizole sulfate can be used in the research of Dravet syndrome, hepatitis C virus infection, Staphylococcus aureus skin infection, Cisplatin (HY-17394)-induced nephrotoxicity, STXBP1-related diseases, traumatic brain injury and xeroderma pigmentosum type C .
Cat. No.: HY-30234S
CAS No.: 1251554-64-9
Cat. No.: HY-N6911A
CAS No.: 83896-44-0
Synonyms: 18α-GA; Isoglycyrrhizinic acid; 18α-Glycyrrhizic acid
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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
