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T-26c

Catalog No. T5361 CAS 869296-13-9

T-26c is highly potent and selective matrix metalloproteinase-13 (MMP-13) inhibitor (IC50: 6.75 pM).

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T-26c, CAS 869296-13-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 41.00
2 mg	In stock	$ 58.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 155.00
25 mg	In stock	$ 263.00
50 mg	In stock	$ 447.00
100 mg	In stock	$ 646.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 100%

Purity: 99.11%

Biological Description

Chemical Properties

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Description	T-26c is highly potent and selective matrix metalloproteinase-13 (MMP-13) inhibitor (IC50: 6.75 pM).
Targets&IC50	MMP13:6.75 pM （cell free)
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.
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.
Kinase Assay	The MMP assay buffer consisted of 50 mM Tris–HCl (pH 7.5), 10 mM CaCl2, 150 mM NaCl, and 0.05% Brij-35. The pro-MMPs were activated by preincubation with 1 mM aminophenylmercuric acetate (APMA) in assay buffer at 37 °C for 2 h (MMP-1, 2, 7, 8, 10, and 13) or 18 h (MMP-3 and 9). The TACE assay buffer consisted of 25 mM Tris–HCl (pH 9.0), 2.5 mM ZnCl2, and 0.005% Brij-35. The pro-MMPs were activated by preincubation with 1 mM aminophenylmercuric acetate (APMA) in assay buffer at 37 °C for 2 h (MMP-1, 2, 7, 8, 10, and 13) or 18 h (MMP-3 and 9). Enzyme inhibition assays were performed in an assay buffer containing enzymes and fluorescence peptide (Cy3-PLGLK(Cy5Q)AR-NH2 for MMPs, Cy3-PLAQAV(Cy5QL-2,3-diaminopropionic acid)-RSSSR-NH2 for TACE) in the presence of the various concentrations of inhibitors. Following incubation at 37 °C for 40 min, the reaction was terminated by addition of EDTA (pH 8.0). The increase in fluorescence as measured by Farcyte spectrofluorimeter. Enzyme activity (%) was determined as following equation: Enzyme activity (%) = (X - C)/(T - C) × 100, where X = the fluorescence count with inhibitor, T = the fluorescence count without inhibitor and C = the fluorescence count with EDTA. IC50 values of inhibitors were obtained with iterative fitting package.
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.

Molecular Weight	479.51
Formula	C24H21N3O6S
CAS No.	869296-13-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 12 mg/mL (25.03 mM)

H2O: Insoluble

References and Literature

1. Nara H, et al. Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site. Bioorg Med Chem. 2014 Oct 1;22(19):5487-505.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Inhibitor Library Anti-Pancreatic Cancer Compound Library Bioactive Compound Library Angiogenesis related Compound Library Immunology/Inflammation Compound Library Bioactive Compounds Library Max Anti-Fibrosis Compound Library NO PAINS Compound Library Protease Inhibitor Library

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Keywords

T-26c 869296-13-9 Proteases/Proteasome MMP T26c Inhibitor Matrix metalloproteinases T 26c inhibit inhibitor

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