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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
35 Results for "
architecture
" in MedChemExpress (MCE) Product Catalog:
Products (35)
35 Results for "architecture" in MCE Product Catalog:
Cat. No.: HY-P10984
CAS No.: 206536-96-1
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FNIII14 is a β1-integrin inhibitory peptide. FNIII14 induces the conformational shift of β1-integrin from the active form to the inactive form, blocks integrin-mediated signaling pathways, disrupts the interaction between VLA-4 and fibronectin, inhibits the phosphorylation of FAK/Akt, suppresses cell adhesion, fibronectin fibril formation and chondrocyte proliferation, induces chondrocyte apoptosis and cartilage degeneration, upregulates the pro-apoptotic protein Bim, and binds to membrane-bound eEF1A. FNIII14 reversibly disrupts cell adhesion without reducing cell viability, accelerates adipocyte differentiation, and loosens tumor matrix architecture to enhance the permeability of nanotherapeutic agents. FNIII14 can be used in research related to neuroblastoma, pancreatic cancer, acute myeloid leukemia, colitis-associated colorectal cancer, osteoarthritis, and atherosclerosis .
Cat. No.: HY-P2788
CAS No.: 2493080-84-3
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Cat. No.: HY-145441
CAS No.: 2866211-93-8
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GEM–IB is the conjugate of gemcitabine (GEM)-5'-phosphate with ibandronate (IB). GEM–IB as a single agent or in combination with Docetaxel (DTX) demonstrates reduced tumor burden, preservation of the bone architecture, and improved the survival in a murine model of osteosarcoma (OS) .
Cat. No.: HY-B1337S2
CAS No.: 3035513-80-2
Choline-d6 chloride is the d6-labeled Choline chloride (HY-B1337). Choline chloride is an orally active methylxanthine derivative. Choline chloride exhibits weak antihistaminic and anticholinergic activities and potentiates the effects of histamine and acetylcholine. Choline chloride relaxes bronchial smooth muscle, dilates coronary and peripheral blood vessels, increases urine output and electrolyte excretion, stimulates locomotor activity in the central nervous system, and induces transient hypotension following a pressor phase. Choline chloride modulates sleep architecture by increasing wakefulness time and reducing slow-wave sleep, without altering the frequency or severity of nocturnal hypoxemia, apnea, or hypopnea events. Choline chloride is used in studies of bronchospasm, nocturnal asthma, and chronic asthma .
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Cat. No.: HY-P990955
CAS No.: 2839652-75-2
Synonyms: ADX-097
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Cat. No.: HY-174479
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Mouse Mef2c mRNA encodes the mouse myocyte enhancer factor 2C (Mef2c) protein, a transcription activator which binds specifically to the MEF2 element present in the regulatory regions of many muscle-specific genes. Mef2c controls cardiac morphogenesis and myogenesis, and is also involved in vascular development, neurogenesis and the development of cortical architecture.
Cat. No.: HY-184913
JHK-02-102-1 is a selective CDK5 degrader derived from the regorafenib kinase inhibitor scaffold. JHK-02-102-1 recruits CRL4CRBN E3 ubiquitin ligase to induce ternary complex formation between CDK5 and CRBN, triggering ubiquitin-proteasome system-dependent degradation. JHK-02-102-1 achieves selectivity redirection from CDK6 to CDK5 via subtle PROTAC architecture modifications .
Cat. No.: HY-178359
CAS No.: 2228278-95-1
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JAX-77 is a potent root architecture modulator. JAX-77 maintains primary root length while substantially increasing lateral root numbers, thereby optimizing the plant’s overall root system. JAX-77 is the key intermediate metabolite formed from the hydrolysis of JAX-44 (HY-178358) and can be converted to Indole-3-butyric acid (IBA) (HY-N0186). JAX-77 can be used for auxin biology and root development research .
Cat. No.: HY-179164S
CAS No.: 287484-43-9
Choline- 15N chloride is the 15N-labeled Choline chloride (HY-B1337). Choline chloride is an orally active methylxanthine derivative. Choline chloride exhibits weak antihistaminic and anticholinergic activities and potentiates the effects of histamine and acetylcholine. Choline chloride relaxes bronchial smooth muscle, dilates coronary and peripheral blood vessels, increases urine output and electrolyte excretion, stimulates locomotor activity in the central nervous system, and induces transient hypotension following a pressor phase. Choline chloride modulates sleep architecture by increasing wakefulness time and reducing slow-wave sleep, without altering the frequency or severity of nocturnal hypoxemia, apnea, or hypopnea events. Choline chloride is used in studies of bronchospasm, nocturnal asthma, and chronic asthma .
Cat. No.: HY-189412
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Antibacterial agent 376 is an antibacterial agent. Antibacterial agent 376 exhibits antibacterial efficacy against S. aureus and E. coli. Antibacterial agent 376 induces mild hepatic alterations, including slight inflammatory cell infiltration, moderate vacuolar degeneration, and moderate hepatocyte enlargement, while the overall liver architecture remains largely preserved. Antibacterial agent 376 induces mild renal alterations, including vascular congestion, limited inflammatory cell infiltration, and mild tubular degeneration, while the overall kidney structure remains intact. Antibacterial agent 376 causes a significant decrease in serum antioxidant markers GSH, GPx, and CAT, indicating the induction of oxidative stress in rats. Antibacterial agent 376 can be used for research on bacterial infections (Staphylococcus aureus and Escherichia coli) .
Cat. No.: HY-L125
2,810 compounds
Pulmonary fibrosis (PF), also known as diffuse interstitial pulmonary fibrosis, is a very common end-stage manifestation of several diseases, including idiopathic pulmonary fibrosis (IPF), pulmonary hypertension, and scleroderma, characterised by excessive matrix deposition and destruction of the lung architecture, finally leading to respiratory insufficiency. PF has become a global disease with significantly increased incidence rate, and the most common form of pulmonary fibrosis is idiopathic pulmonary fibrosis (IPF).
Lung fibrosis is a complex disease, a multitude of signal factors and signaling pathways is disrupted in this complex disease, such as TGF-β, Wnt, VEGF and PI3K–Akt. MCE offers a unique collection of 2,810 compounds with identified and potential anti-pulmonary fibrosis activity. MCE Anti-Pulmonary Fibrosis Compound Library is a useful tool for anti-pulmonary fibrosis drugs screening and other related research.
Cat. No.: HY-180556
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PI3K/mTOR-IN-20 is a selective dual PI3K/mTOR inhibitor. PI3K/mTOR-IN-20 demonstrates nanomolar antiproliferative effects with IC50s of 0.380 and 0.090 μM for MRC-5 and Mlg2908 cells. PI3K/mTOR-IN-20 reduces Ashcroft scores, hydroxyproline content, collagen deposition, and downregulates fibrosis-related proteins, while restoring lung architecture in a Bleomycin-induced pulmonary fibrosis model. PI3K/mTOR-IN-20 shows a favorable safety profile with steady weight recovery and no distinct liver or kidney toxicity. PI3K/mTOR-IN-20 can be used for fetal lung fibroblasts research .
Cat. No.: HY-L932V0
2,000,000 compounds
Macrocyclic compounds (≥12-atom cyclic small molecules/peptides) have unique physicochemical properties. They form preorganized conformations with high binding affinity/selectivity, target traditional small-molecule-inaccessible proteins, and bridge small-molecule drugs and biological agents. As key protein phosphorylation enzymes, kinases are linked to tumors, COPD, etc., and are critical therapeutic targets. Traditional small-molecule kinase inhibitors lack selectivity, causing off-target toxicity, low bioavailability, and acquired resistance. Macrocycles’ semi-rigid structure restricts conformations, boosts binding selectivity, optimizes pharmacokinetics, and makes macrocyclization a core kinase inhibitor optimization strategy.
Thousands of bioactive macrocycles were curated from ChEMBL. Via Transformer, macrocyclization was converted into a chemical language translation task, enabling end-to-end macrocycle generation from linear precursors with simplified inputs. Macformer achieves efficient, automated linear molecule macrocyclization via deep learning; generated macrocycles have diversity, novelty, biocompatibility, and cover broader chemical space.
MCE collected thousands of marketed/clinical kinase inhibitors, using their fragments for macrocyclization to generate derivatives. After evaluating synthetic accessibility and physicochemical properties, a million-scale virtual macrocyclic library was built for kinase-related virtual and AI-driven screening.
Cat. No.: HY-L932V
2,000,000 compounds
Macrocyclic compounds (≥12-atom cyclic small molecules/peptides) have unique physicochemical properties. They form preorganized conformations with high binding affinity/selectivity, target traditional small-molecule-inaccessible proteins, and bridge small-molecule drugs and biological agents. As key protein phosphorylation enzymes, kinases are linked to tumors, COPD, etc., and are critical therapeutic targets. Traditional small-molecule kinase inhibitors lack selectivity, causing off-target toxicity, low bioavailability, and acquired resistance. Macrocycles’ semi-rigid structure restricts conformations, boosts binding selectivity, optimizes pharmacokinetics, and makes macrocyclization a core kinase inhibitor optimization strategy.
Thousands of bioactive macrocycles were curated from ChEMBL. Via Transformer, macrocyclization was converted into a chemical language translation task, enabling end-to-end macrocycle generation from linear precursors with simplified inputs. Macformer achieves efficient, automated linear molecule macrocyclization via deep learning; generated macrocycles have diversity, novelty, biocompatibility, and cover broader chemical space.
MCE collected thousands of marketed/clinical kinase inhibitors, using their fragments for macrocyclization to generate derivatives. After evaluating synthetic accessibility and physicochemical properties, a million-scale virtual macrocyclic library was built for kinase-related virtual and AI-driven screening.
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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
