For research use only.

Licensed by Pfizer Catalog No.S1403 Synonyms: GAR-936

5 publications

Tigecycline Chemical Structure

Molecular Weight(MW): 585.65

Tigecycline is bacteriostatic and is a protein synthesis inhibitor by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation.

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Selleck's Tigecycline has been cited by 5 publications

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  • CHX blocked Pim-1 AUG isoform translocation from the cytosol to mitochondria and led to reduced pBADS112. Cox-2 was examined to assess the effect of tigecycline on mitochondrial translation. Cy-Cox-2: cytoplasmic Cox-2; Mt-Cox-2: mitochondrial Cox-2.

    Biochem J, 2016, 473(1):99-107. Tigecycline purchased from Selleck.

Purity & Quality Control

Choose Selective Antineoplastic and Immunosuppressive Antibiotics Inhibitors

Biological Activity

Description Tigecycline is bacteriostatic and is a protein synthesis inhibitor by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation.
In vitro

Tigecycline evades the Tet(A-E) efflux pumps, which account for most acquired resistance to tetracycline and minocycline in Enterobacteriaceae and Acinetobacter spp. Tigecycline binds to bacterial ribosomes that have been modified by the Tet(M) protein, a mechanism that compromises all available tetracyclines, and which is frequent in Gram-positive cocci and Neisseria spp. Tigecycline remains vulnerable to the chromosomally-encoded multidrug efflux pumps of Proteeae and Pseudomonas aeruginosa, and to Tet(X), a tetracycline-degrading mono-oxygenase found, albeit rarely, in Bacteroides spp. Tigecycline MICs for enterococci, staphylococci, and streptococci are mostly 0.06–0.25 mg/L, again with little or no skew to the distribution. Tigecycline is prone to oxidation, and MIC values, particularly for the most susceptible isolates, may be raised if the drug is added to broth that has become oxygenated during storage, or if drug-containing media are stored before inoculation. [1] Tigecycline is a poor substrate for tetracycline-specific efflux pumps, and it still attaches to ribosomes that have been modified by the Tet(M) protein. Tigecycline has demonstrated activity against a wide variety of gram-positive and gram-negative pathogens, including multidrug-resistant strains. Tigecycline is active against many gram-positive and -negative organisms, including methicillin-resistantStaphylococcus aureus, vancomycin-intermediate and -resistant enterococci, and extended-spectrum β-lactamase–producing Escherichia coli and Klebsiella pneumoniae. Tigecycline exhibits antibacterial activity against a wide spectrum of aerobic and anaerobic bacteria. [2] Tigecycline is a broad-spectrum, protein-inhibiting, antibacterial agent possessing activity against strains resistant to other chemotherapeutic agents. Tigecycline demonstrates in vitro activities against the GISA and the methicillin-resistant and methicillin-susceptible staphylococcal strains tested (MICs at which 90% of isolates tested are inhibited [MIC90s], 0.5 to 1 μg/ml). Tigecycline has MIC90s of 0.25 μg/ml for all of the S. pneumoniae strains and demonstrates similar activities against all of the S. pneumoniae strains tested. [3]

Methods Test Index PMID
Western blot
Cyclin D1 / CDK2 / p21 ; 

PubMed: 30247801     

MM cells were treated with tigecycline as above, and Western blot analysis was performed to assess the level of p21, cyclin D1 and CDK2. *P < 0.05, **P < 0.01, vs the respective control.

p62 / LC3-I / LC3-II ; 

PubMed: 30247801     

RPMI-8226, NCI-H929 and U266 cells were treated with 0, 10, 20, 40 μmol/L tigecycline for 48 h, the autophagy markers LC3 and SQSTM1/p62 were detected by Western blot analysis.

p-AMPKα / AMPKα / p-mTOR / mTOR / p-p70S6K / p70S6K / p-4E-BP-1 / 4E-BP1 ; 

PubMed: 30247801     

AMPK/mTOR pathway is implicated in tigecycline‐induced autophagy in MM cells. After treated with various concentrations of tigecycline for 48 h, the levels of AMPKa, mTOR, p70S6K, and 4E‐BP1, as well as the phosphorylation of these proteins were analysed by Western blot in MM cell lines RPMI‐8226 (A), NCI‐H929 (B) and U266 (C). Images shown were representatives of at least three independent experiments.

Cox-1 / Cox-2 / Cox-4 ; 

PubMed: 30082885     

Tigecycline decreases protein level (A) of Cox-1 and -2 without affecting protein and mRNA levels of Cox-4 in retinoblastoma cells and HREC.  

CDK2 / Cyclin E; 

PubMed: 26621850     

C, D. Western blot assay was performed to assess the cell cycle-related protein levels at 48 h in A375 and MV3 cells, respectively. Cells were treated with the indicated concentration or the indicated times of tigecycline; GAPDH was used as a control. 

E-cadherin / Vimentin ; 

PubMed: 26621850     

Western blot analysis of the EMT-related protein levels at 48 h in A375 and MV3 cells respectively. Cells were treated with the indicated concentration or the indicated times of tigecycline; GAPDH was used as a control. 

30247801 30082885 26621850
Growth inhibition assay
Cell viability; 

PubMed: 30247801     

Tigecycline induces growth inhibition in MM cells. A, After cultured with different concentrations of tigecycline for 24, 48 and 72 h, the cell viability of RPMI‐8226, NCI‐H929 and U266 cells was measured by CCK‐8 assay.

In vivo Tigecycline is bactericidal against methicillin-susceptible S. aureus (MSSA) in the rabbit osteomyelitis model and exhibits good, but not excellent, activity in Legionellapneumophila pneumonia in guinea pigs[1]. Tigecycline at 50 mg/kg twice daily was not toxic to mice. Tigecycline is effective in inhibiting NSCLC growth in vivo through decreasing proliferation and increasing apoptosis of tumor cells[4].


Cell Research:


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  • Cell lines: NSCLC cells
  • Concentrations: 1, 5, 10, 25, 50 μM
  • Incubation Time: 24 h or 3 days
  • Method:

    NSCLC cells were treated with DMSO (as control) or different concentrations of tigecycline for 3 days prior to 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium (MTS) and apoptosis assays. After 24 h of treatment with tigecycline, cells were harvested for the measurement of mitochondrial functions.

    (Only for Reference)
Animal Research:


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  • Animal Models: SCID mice
  • Dosages: 50 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (170.75 mM)
Water 100 mg/mL (170.75 mM)
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 585.65


CAS No. 220620-09-7
Storage powder
in solvent
Synonyms GAR-936
Smiles CN(C)C1C2CC3CC4=C(C(=C(NC(=O)CNC(C)(C)C)C=C4N(C)C)O)C(=O)C3=C(O)C2(O)C(=O)C(=C1O)C(N)=O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03034174 Unknown status -- Septic Shock|Antibiotic Resistant Infection|Critical Illness Medical University of Lublin January 15 2017 --
NCT02883036 Not yet recruiting Other: blood sampling Chronic Myeloid Leukemia Nanfang Hospital of Southern Medical University September 2016 --
NCT02931526 Unknown status Drug: Tigecycline Bacterial Infection|Critically Ill Zhujiang Hospital August 2016 --
NCT01840319 Completed -- Survival Status at Day 30 After the Last Intake Pfizer February 2013 --
NCT01560143 Completed Drug: Tigecycline Obesity Manjunath Prakash Pai|Pfizer|University of Michigan March 2012 Phase 4

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID