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Doxycycline MMP Inhibitor

Name: Doxycycline
Brand: Selleck Chemicals
SKU: S5159
Availability: InStock
Rating: 5 (60 reviews)

Cat.No.S5159

Doxycycline (Vibramycin, Doxytetracycline, Doxiciclina, Doxycyclinum) is an antibiotic that is used in the treatment of a number of types of infections caused by bacteria and protozoa. Doxycycline is also a nonspecific matrix metalloproteinase (MMP) inhibitor.

Chemical Structure

Molecular Weight: 444.43

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: >97%

Related Targets	Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite Reverse Transcriptase HIV HCV Protease SARS-CoV HIV Protease Influenza Virus β-lactamase Integrase HBV CMV Neuraminidase HCV HSV RSV Enterovirus Thioredoxin Reductase 3C-Like Protease Ribosomal Peptidyl Transferase HPV
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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	444.43	Formula	C₂₂H₂₄N₂O₈	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	564-25-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	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

Solubility

In vitro
Batch:

DMSO : 89 mg/mL ( (200.25 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.100mg/ml (2.48mM)	Taking the 1 mL working solution as an example, add 50 μL of 22 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	1%DMSO 1 1%PEG300 2 98%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.060mg/ml (0.14mM)	Taking the 1 mL working solution as an example, add 10 μL of 6mg/ml clarified DMSO stock solution to 10 μL of PEG300, mix evenly to clarify it; add 980 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.250mg/ml (7.31mM)	Taking the 1 mL working solution as an example, add 50 μL of 65 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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^[1]. 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^[2].
In vivo	Doxycycline successfully reduces tumor growth in vivo (inhibited pancreatic cancer cell growth)^[2].
References	https://pubmed.ncbi.nlm.nih.gov/23741339/ https://pubmed.ncbi.nlm.nih.gov/19846942/

Applications

Methods	Biomarkers	Images	PMID
Western blot	pATM / ATM HSP70 / HSP90 AKT / BCL6 / Cyclin E / HDAC2 / HDAC3 / NEMO / TYK2 / RIPK1		23282955
Immunofluorescence	E-cadherin / Vimentin		29285218

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
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

Tech Support

Handling Instructions

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