T-26c

SKU: orb1301853

Description

T-26c is a highly potent and selective small molecule inhibitor of matrix metalloproteinase-13 (MMP-13), exhibiting an IC50 value of 6.75 pM. It is a valuable research tool for studying MMP-13's role in osteoarthritis, cancer, and fibrosis in both in vitro and in vivo experimental models.

Research Area

Protein Biochemistry

Key Properties

• CAS Number: 869296-13-9
• MW: 479.51
• Purity: 100.00%
• Formula: C₂₄H₂₁N₃O₆S
• SMILES: COc1cccc(CNC(=O)c2nc(=O)c3c(COCc4ccc(cc4)C(O)=O)csc3[nH]2)c1
• Target: MMP
• Solubility: H2O:Insoluble;DMSO:12 mg/mL (25.03 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.09 mM)

Bioactivity

• Target IC50:
  MMP13:6.75 pM （cell free)
• In Vivo:
  Oral administration of the disodium salt formulations of T-26c to guinea pigs resulted in significant increases in AUC (8357 ng·h/mL) and Cmax (1445 ng/mL) compared with those of the free acid T-26c (AUC = 6478 ng·h/mL and Cmax = 911 ng/mL). The compound was well absorbed in all species at the oral dose of 10–20 mg/kg.
• In Vitro:
  T-26c was the highly potent and selective MMP13 inhibitor with an IC50 value of 6.9 pM and more than 2600-fold selectivity over the other related metalloenzymes. Furthermore, the inhibitor was shown to be active in bovine nasal cartilage explants assay. T-26c significantly inhibited the breakdown of collagen (87.4% inhibition at 0.1 μM) in IL-1b and oncostatin M stimulated cartilage.
• Cell Research:
  Bovine nasal septum cartilage was sliced, and the slices were maintained in the medium of a 1:1 (v/v) mixture of Dulbecco's modified Eagle's MEM and Ham's F-12 medium (DMEM/F-12) containing 10 % fetal calf serum overnight. After confirming that the slices were not contaminated, they were cultured in DMEM/F-12 medium containing 20 μg/mL gentamycin, 50 μg/mL streptomycin, and 50 U/mL penicillin (culture medium) for 2 days at 37 °C. The cartilage slices were cut into small cubes (ca. 1mm3) and transferred individually into wells of a 96 well plate with 100 μL of culture medium. For the collagen degradation assay, the medium was supplemented with 10 ng/mL IL-1β and 50 ng/mL oncostatin M in the presence or absence of compounds. The cartilage was incubated for 2 weeks. The supernatants were harvested and replaced with fresh medium containing identical test compounds every 7 days. Supernatants of day 7 and day 14 were collected and stored at -20 °C until assay. At the end of the culture, the remaining cartilage was completely digested with papain. Hydroxyproline release in the media from each explant was determined as a measure of collagen degradation by use of chloramine T and p-dimethylaminobenzaldehyde. The percentage of inhibitory activity against collagen degradation was calculated as follows: % of inhibition = [(% of collagen degradation with IL-1b and OSM) - (% of collagen degradation with IL-1β, OSM, and test sample)]/[(% of collagen degradation with IL-1β and OSM) - (% of collagen degradation without additives)] × 100.

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

MMP, MMP-13, inhibit, Matrix metalloproteinases, Inhibitor, T 26c, T26c, T-26c

Compound Identifiers

PubChem CID

11525848