pour la recherche uniquement
Réf. Catalogue: S4163
Structure chimique
| Cibles apparentées | HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease Tyrosinase HIV Protease DPP |
|---|---|
| Autre Antineoplastic and Immunosuppressive Antibiotics Inhibiteurs | Staurosporine (STS) Cyclosporin A Oligomycin A (MCH 32) Puromycin Dihydrochloride Nigericin sodium salt Geldanamycin (NSC 122750) Honokiol Streptozotocin (STZ) Sodium Monensin (NSC 343257) Hygromycin B |
| Lignées cellulaires | Type d'essai | Concentration | Temps d'incubation | Formulation | Description de l'activité | PMID |
|---|---|---|---|---|---|---|
| SW1353 | Function assay | 50 uM | Inhibition of IL-1-beta-induced MMP13 production in human SW1353 cells at 50 uM | 17267227 | ||
| K-12 BW25113 | Bactericidal assay | 24 hrs | Bactericidal activity against yafQ gene-deficient Escherichia coli K-12 BW25113 biofilm assessed as log reduction of viable cells after 24 hrs | 19307375 | ||
| K-12 BW25113 | Bactericidal assay | 24 hrs | Bactericidal activity against Escherichia coli K-12 BW25113 biofilm harboring pCA24N ptac::yafQ plasmid assessed as log reduction of viable cells after 24 hrs pretreated with 5 uM of IPTG for 4 hrs | 19307375 | ||
| K562 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human K562 cells after 72 hrs by flow cytometry, IC50 = 15 μM. | 19482476 | ||
| HepG2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 20 μM. | 19482476 | ||
| THP1 | Function assay | Selectivity index, ratio of IC50 for human THP1 cells to IC50 for Plasmodium falciparum, IC50 = 3.1 μM. | 19748781 | |||
| THP1 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human THP1 cells after 72 hrs by propidium iodide staining-based flow cytometry, IC50 = 20 μM. | 19748781 | ||
| K562 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human K562 cells after 72 hrs by flow cytometry, IC50 = 15 μM. | 19926173 | ||
| HepG2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 20 μM. | 19926173 | ||
| HepG2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, CC50 = 20 μM. | 21741131 | ||
| Neuro2a | Function assay | 1 uM | Decrease in 7-DHC levels in Dhcr7-deficient mouse Neuro2a cells at 1 uM by LC-MS/GC-MS analysis | 26789657 | ||
| HepG2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HepG2 cells measured after 72 hrs by MTT assay, CC50 = 20 μM. | 27155463 | ||
| HepG2 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay, CC50 = 20 μM. | 27654395 | ||
| CD | Antibacterial assay | 25 ug/ml | 72 hrs | Antibacterial activity against Rickettsia prowazekii str. Breinl infected in CD rat primary pulmonary vascular endothelial cells assessed as bacterial shape change at 25 ug/ml measured 72 hrs post infection by Hoechst 33258/phalloidin staining based fluor | 28089350 | |
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | |||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | |||
| skeletal myoblast cells | Cytotoxicity assay | DNDI: Cytotoxicity in Vitro, 72 hour, in rat skeletal myoblast cells, IC50 = 14.49 μM. | ChEMBL | |||
| Cliquez pour voir plus de données expérimentales sur la lignée cellulaire | ||||||
| Poids moléculaire | 512.94 | Formule | C22H24N2O8.1/2C2H6O.HCl.1/2H2O |
Stockage (À compter de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 24390-14-5 | Télécharger le SDF | Stockage des solutions mères |
|
|
| Synonymes | WC2031 | Smiles | CCO.CC1C2C(C3C(C(=O)C(=C(C3(C(=O)C2=C(C4=C1C=CC=C4O)O)O)O)C(=O)N)N(C)C)O.CC1C2C(C3C(C(=O)C(=C(C3(C(=O)C2=C(C4=C1C=CC=C4O)O)O)O)C(=O)N)N(C)C)O.O.Cl.Cl | ||
|
In vitro |
DMSO
: 100 mg/mL
(194.95 mM)
Water : 100 mg/mL Ethanol : Insoluble |
|
In vivo |
|||||
Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)
Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y a pas de formulation in vivo dans la section Solubilité.)
Résultats du calcul :
Concentration de travail : mg/ml;
Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter d'abord si la concentration dépasse la solubilité du DMSO du lot de médicament. )
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.
Note : 1. Veuillez vous assurer que le liquide est clair avant d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.
| Targets/IC50/Ki |
MMP
|
|---|---|
| In vitro |
Doxycycline hyclate 10% (DOXY) has significant toxicity effects on osteoblast cells compared to the control group with a mean cell viability of 84%. Doxycycline hyclate 10% (DOXY) results in a significantly higher alkaline phosphatase activity (approximately 56%) than the control in osteoblasts. Doxycycline hyclate 10% (DOXY) seems to slightly altered the morphology of the osteoblasts. |
| In vivo |
Doxycycline hyclate is an effective treatment for acute E. canis infection in dogs. Doxycycline hyclate (5 mg/kg, orally) decreases the collagenase activity in corneas obtained from rabbits. Doxycycline hyclate (5 mg/kg, orally) promotes corneal reepithelialization in the rabbit alkali-burn model, a result, perhaps, of the drug's ability to inhibit excessive collagenase activity. Doxycycline hyclate results in 43% of prophylaxis in orally treated mice, in contrast, the sustained-release doxycycline hyclate completely protects mice from infection and resultant pathology. Doxycycline hyclate results in bioavailability of 70%, Cmin of 1 mg/L, Cmax of 2.3 mg/L and elimination half-life of 7 hours in calves with immature rumen function. |
Références |
|
| Méthodes | Biomarqueurs | Images | PMID |
|---|---|---|---|
| Western blot | pATM / ATM HSP70 / HSP90 AKT / BCL6 / Cyclin E / HDAC2 / HDAC3 / NEMO / TYK2 / RIPK1 |
|
23282955 |
| Immunofluorescence | E-cadherin / Vimentin |
|
29285218 |
(données du https://clinicaltrials.gov, mis à jour le 2026-05-15)
| Numéro NCT | Recrutement | Conditions | Promoteur/Collaborateurs | Date de début | Phases |
|---|---|---|---|---|---|
| NCT06738407 | RECRUITING | Gonorrhea; Chlamydia; Syphilis; Sexually Transmitted Infections (STIs) |
Westat |
2026-02-27 | PHASE4 |
| NCT07688096 | NOT_YET_RECRUITING | Ehlers-Danlos Syndrome Hypermobility Type (hEDS); Ehlers-Danlos Syndrome (EDS); Joint Hypermobility; Joint Instability; Hypermobility Spectrum Disorder; Chronic Pain Syndrome; Musculoskeletal Pain; Sprain; Subluxation; Dislocation; Craniocervical Disfunction |
Manhattan Pain Medicine, PLLC |
2026-07-15 | PHASE1; PHASE2 |
| NCT04504123 | RECRUITING | Exudative Macular Degeneration; Wet Age-related Macular Degeneration |
University of Iowa |
2020-11-04 | PHASE2 |
| NCT04762134 | RECRUITING | Bacterial Sexually Transmitted Diseases |
Jonathan Troy Grennan |
2023-06-02 | |
| NCT04582383 | ACTIVE_NOT_RECRUITING | Acne |
University of Pennsylvania |
2022-03-30 | PHASE4 |
| NCT05112211 | RECRUITING | Thyroid Associated Ophthalmopathy |
Sun Yat-sen University |
2022-01-01 |