Home Microbiology Antineoplastic and Immunosuppressive Antibiotics Hämmare Doxycycline

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Doxycycline MMP Inhibitor

Kat.nr.: S5159

Doxycycline (Vibramycin, Doxytetracycline, Doxiciclina, Doxycyclinum) är ett antibiotikum som används vid behandling av ett antal typer av infektioner orsakade av Bacterial och protozoer. Doxycycline är också en ospecifik matrix metalloproteinase (MMP)-hämmare.
Doxycycline Antineoplastic and Immunosuppressive Antibiotics Hämmare Chemical Structure

Kemisk struktur

Molekylvikt: 444.43

Hoppa till

Kvalitetskontroll (Quality Control)

Batch: Renhet: >97.00%
  • Citerad i Nature Medicine för sin förstklassiga kvalitet
  • COA
  • Datablad
  • SDS
  • Citerad i Nature Medicine för sin förstklassiga kvalitet
  • COA
  • Datablad
  • SDS
  • Citerad i Nature Medicine för sin förstklassiga kvalitet
  • COA
  • Datablad
  • SDS
  • Citerad i Nature Medicine för sin förstklassiga kvalitet
  • COA
  • Datablad
  • SDS
  • Citerad i Nature Medicine för sin förstklassiga kvalitet
  • COA
  • Datablad
  • SDS
97.00

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Cellinjer Analystyp Koncentration Inkubationstid Formulering Aktivitetsbeskrivning PMID
Staphylococcus aureus 2 planktonic cells Bactericidal assay 24 hrs Bactericidal activity against methicillin-resistant Staphylococcus aureus 2 planktonic cells after 24 hrs by calgary biofilm device method, MBC=2μM. 29638121
THP1 Function assay Selectivity index, ratio of IC50 for human THP1 cells to IC50 for Plasmodium falciparum, IC50=3.1μM. 19748781
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells after 72 hrs by flow cytometry, IC50=15μM. 19482476
K562 Cytotoxicity assay 72 hrs Cytotoxicity against human K562 cells after 72 hrs by flow cytometry, IC50=15μM. 19926173
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50=20μM. 19482476
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, IC50=20μM. 19926173
THP1 Cytotoxicity assay 72 hrs Cytotoxicity against human THP1 cells after 72 hrs by propidium iodide staining-based flow cytometry, IC50=20μM. 19748781
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, CC50=20μM. 21741131
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, CC50=20μM. 22889559
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, CC50=20μM. 21852132
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, CC50=20μM. 24946216
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay, CC50=20μM. 25791675
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells incubated for 72 hrs by MTT assay, CC50=20μM. 25282267
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells measured after 72 hrs by MTT assay, CC50=20μM. 27155463
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay, CC50=20μM. 27654395
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
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
vascular endothelial cells 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
Hep2 Anti-Chlamydial assay 1 ug/ml 8 hrs Anti-Chlamydial activity against Chlamydia trachomatis Serovar LGV-L2 infected in Hep2 cells assessed as reduction in size and number of chlamydial inclusion at 1 ug/ml treated at 8 hrs post-infection and 24 hrs later re-infecting fresh Hep2 cells monolay 32227948
skeletal myoblast cells Cytotoxicity assay DNDI: Cytotoxicity in Vitro, 72 hour, in rat skeletal myoblast cells, IC50=14.49μM. ChEMBL
Klicka för att visa mer experimentella data för cellinjer

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Molekylvikt 444.43 Formel

C22H24N2O8

 Lagring (från mottagningsdatumet)
CAS-nr 564-25-0 Ladda ner SDF Lagring av stamlösningar

Synonymer Vibramycin, Doxytetracycline, Doxiciclina, Doxycyclinum Smiles 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

Löslighet (Solubility)

In vitro
Batch:

DMSO : 89 mg/mL (200.25 mM)
(Fuktkontaminerad DMSO kan minska lösligheten. Använd färk, vattenfri DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritetsräknare

Massa Koncentration Volym Molekylvikt
Utspädningsräknare Molekylviktsräknare

In vivo
Batch:

In vivo-formuleringsräknare (Klar lösning)

Steg 1: Ange information nedan (Rekommenderas: Ett extra djur för att ta hänsyn till förluster under experimentet)

mg/kg g μL

Steg 2: Ange in vivo-formuleringen (Detta är endast räknaren, inte formuleringen. Vänligen kontakta oss först om det inte finns någon in vivo-formulering i löslighetsavsnittet.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Beräkningsresultat:

Arbetskoncentration: mg/ml;

Metod för att bereda DMSO-stamlösning: mg substans förlöst i μL DMSO ( Stamlösningskoncentration mg/mL, Vänligen kontakta oss först om koncentrationen överskrider DMSO-lösligheten för denna batch av substansen. )

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedanμL PEG300, blanda och klarna, tillsätt sedanμL Tween 80, blanda och klarna, tillsätt sedan μL ddH2O, blanda och klarna.

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedan μL Majsolja, blanda och klarna.

Obs: 1. Se till att vätskan är klar innan du tillsätter nästa lösningsmedel.
2. Se till att tillsätta lösningsmedlet/lösningsmedlen i ordning. Du måste se till att lösningen som erhålls i föregående tillsats är en klar lösning innan du fortsätter att tillsätta nästa lösningsmedel. Fysiska metoder som vortex, ultraljud eller varmt vattenbad kan användas för att underlätta upplösningen.

Verkningsmekanism (Mechanism of Action)

In vitro

100 ng/mL-5 µg/mL Doxycycline can significantly alter the metabolic profile of the cell, as well as reduce the proliferative rate, though the effect size depends upon the particular cell line used.

This compound arrests cells in G1-S phase of the cell cycle in PANC-1 cells and induces the expression of p53 and its downstream target p21. It down-regulates antiapoptotic genes and induces proapoptotic genes. This chemical also induces apoptosis through a Fas/Fas-ligand dependent pathway in Jurkat T lymphocytes.
In vivo

Doxycycline successfully reduces tumor growth in vivo (inhibited pancreatic cancer cell growth).
Referenser

Applikationer (Applications)

Metoder Biomarkörer Bilder PMID
Western blot AKT / BCL6 / Cyclin E / HDAC2 / HDAC3 / NEMO / TYK2 / RIPK1 HSP70 / HSP90 pATM / ATM
S5159-WB1
26142707
Immunofluorescence E-cadherin / Vimentin
S5159-IF1
29285218

Klinisk prövningsinformation (Clinical Trial Information)

(data från https://clinicaltrials.gov, uppdaterad den 2024-05-22)

NCT-nummer Rekrytering Tillstånd Sponsor/Samarbetspartners Startdatum Faser
NCT05972772 Not yet recruiting
Infectious Disease|Therapeutics
Lao-Oxford-Mahosot Hospital Wellcome Trust Research Unit|Mahidol Oxford Tropical Medicine Research Unit
 March 20 2024 Phase 2|Phase 3
NCT06007534 Recruiting
Post-exposure Prophylaxis|Sexually Transmitted Diseases|Doxycycline
Assistance Publique - Hôpitaux de Paris
 October 25 2023 Not Applicable
NCT04762134 Recruiting
Bacterial Sexually Transmitted Diseases
Jonathan Troy Grennan|Canadian Institutes of Health Research (CIHR)|British Columbia Centre for Disease Control
 June 2 2023 Phase 4
NCT05853120 Recruiting
Sexually Transmitted Diseases
Emory University|Centers for Disease Control and Prevention
 May 31 2023 Phase 4
NCT05382208 Recruiting
Emphysema|HIV
Weill Medical College of Cornell University|National Heart Lung and Blood Institute (NHLBI)|University of California Los Angeles|University of Iowa|University of Michigan
 August 22 2022 Phase 2
NCT05492019 Recruiting
Parkinson Disease
Bangabandhu Sheikh Mujib Medical University Dhaka Bangladesh
 July 1 2022 Phase 2