Doxycycline (hyclate)

SKU: orb1307744

Description

Doxycycline hyclate is a broad-spectrum tetracycline antibiotic and matrix metalloproteinase (MMP) inhibitor. It is widely used in research for its antibacterial and antitumor properties, as well as a key regulator in Tet-On/Tet-Off inducible gene expression systems for both in vitro and in vivo studies.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 24390-14-5
• MW: 512.90
• Purity: >99.99% (May vary between batches)
• Formula: C₂₂H₂₄N₂O₈·HCl·1/2C₂H₆O·1/2H₂O
• SMILES: O.Cl.Cl.CCO.C[C@@H]1[C@H]2[C@H](O)[C@H]3[C@H](N(C)C)C(=O)C(C(N)=O)=C(O)[C@@]3(O)C(=O)C2=C(O)c2c(O)cccc12.C[C@@H]1[C@H]2[C@H](O)[C@H]3[C@H](N(C)C)C(=O)C(C(N)=O)=C(O)[C@@]3(O)C(=O)C2=C(O)c2c(O)cccc12
• Target: Antibiotic,ribosome,MMP,Antibacterial
• Solubility: DMSO:250 mg/mL (487.42 mM);H2O:13.89 mg/mL (27.08 mM)

Bioactivity

• Target IC50:
  chlamydial isolates:0.497 μg/mL|Pancreatic Cancer cells (96 h):50.02 μM|Pancreatic Cancer cells (72 h):99.64 μM|NCI-H446 cells:1.70 μM|Pancreatic Cancer cells (48 h):987.5 μM|A549 cells:1.06 μM
• In Vivo:
  METHODS: To detect anti-tumor activity in vivo, Doxycycline (50 mg/kg) was administered intraperitoneally once daily for fifteen days to BALB/c mice harboring human mammary carcinoma tumor 4T1. RESULTS: Doxycycline delayed tumor growth and reduced the number of tumor-associated macrophages and blood vessels. METHODS: To assay antimicrobial activity in vivo, Doxycycline (40 mg/kg) was administered intraperitoneally to BALB/c mice exposed to B. pseudomallei 1026b twice daily for two weeks. RESULTS: Doxycycline-treated mice survived 100% of the time, and no B. pseudomallei DNA was amplified from the lungs or spleens of the majority of the surviving mice.
• In Vitro:
  METHODS: Twenty-two tumor cells were treated with Doxycycline for 48 h. Cell viability was measured by MTT. RESULTS: Lung cancer cells were more sensitive to Doxycycline than most other cell lines. NCI-H446 and A549 cells were sensitive to Doxycycline with IC50s of 1.70 μM and 1.06 μM, respectively. METHODS: Human pancreatic cancer cells PANC-1 were treated with Doxycycline (10-40 μg/mL) for 8-24 h. The cell cycle was detected by Flow Cytometry. RESULTS: Doxycycline caused the cells to arrest in the G1-S phase of the cell cycle.
• Cell Research:
  Doxycycline is diluted in culture medium at a concentration of 10 μg/mL. All in vitro treatments are performed in SMC cultures at 90% confluence, when ECM synthesis in SMC starts to be evident. Doxycycline (20 nM) is diluted in culture medium at a concentration of 10 μg/mL (20 nM), at which no toxicity or variation in primary cultured SMC proliferation has been reported, as well as in other cell lines and the incubation time is 48 h. SMC-C and SMC-Ch are seeded at equal cell density in 6-well plates and, when confluence reaches 90%, 1 mL culture medium is added to each well containing 3.7×104 Bq L-[5-3H]-proline (9.62×1011 Bq/mmol). After 48 h incubation, cells are lysed with 0.5 mL 0.5 mol/L NaOH for 1 h. The resulting solution is neutralized with an equal amount of 0.5 mol/L HCl, and 50 μL are used to measure total proteins with the Bradford method. One volume of 10% TCA is added to the remaining 250 μL and centrifuged at 13,000 g for 15 min at 4°C. The resulting precipitate is dissolved in 100 μL 0.2 mol/L NaOH, and then neutralized with 1 mol/L HCl. The solution is incubated with collagenase buffer (Tris-HCl, pH 7.6 20 mM, and CaCl2 250 mM final concentration) and 10 units of collagenase at 37°C overnight. Then, 150 μL 10% TCA are added and centrifuged at 13000 g for 15 min at 4°C. The resulting supernatant is added to 4 mL of scintillation fluid and the radioactivity is measured in a liquid scintillation counter LS 600 TA.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Doxycycline, Doxycycline (hyclate), Doxycycline hyclate, Doxycycline Hydrochloride, Doxycycline hydrochloride hemiethanolate hemihydrate, anti-proliferative activity, antibacterial activity, Antibiotic, Bacterial, 293T, 16S ribosome, 30S ribosome, MMP, LNT-229, inhibit, Matrix metalloproteinases, MCF 12A, Inhibitor, hyclate, G55, SVG, WC-2031, WC2031, WC 2031, U343

Compound Identifiers

PubChem CID

54686183