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Application: Study enzyme kinetics and screen small molecule inhibitors of ADAMTS4 for drug discovery and high throughput screening (HTS) applications.
Background: ADAMTS4 (A disintegrin and metalloproteinase with thrombospondin motifs 4), also known as aggrecanase-1, is a member of the ADAMTS proteinase family but lacks the C-terminal domain and it is the only member of the family that does not undergo glycosylation. Its TSR (thrombospondin type 1 motif) is essential for its function, by binding to the extracellular matrix proteins. ADAMTS4 can be found in several tissues, such as the ovary, retina, breast, brain and others, and it is involved in cleaving CSPGs (chondroitin sulfate hyaluronan-binding proteoglycans), such as aggrecan, neurocan and versican. It can be inhibited by TIMP3 (metalloproteinase inhibitor 3), and dysfunction can result in osteoarthritis. In addition, it can be a biomarker for adult cardiac injury, as it becomes expressed under those conditions and contributes to fibrosis. In a rat model, inhibition of ADAMST4 resulted in improved cardiac responses and lower accumulation of collagen. The development of ADAMST4 inhibitors can thus open new therapeutic avenues in cardiology.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.Compounds that are fluorescent may interfere with the results, depending on their spectral excitation and emission properties.It is recommended that the compound alone is tested to determine any potential interference of the compound with the assay results.The presence of strong acids or bases, ionic detergents and high salt should be avoided.
Description: The ADAMTS4 Fluorogenic Assay Kit is designed to measure ADAMTS4 (A disintegrin and a metalloproteinase with thrombospondin motifs 4) protease activity for screening and profiling applications. The assay kit comes in a convenient 96-well format, with enough recombinant ADAMTS4, fluorogenic substrate, and assay buffer for 100 enzyme reactions
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed
Uniprot: O75173
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Vistnes M., et al., 2023 Cardiovasc Res 119(10):1915-1927.
Khanan R., et al., 2022 Sci Rep 12:9898.
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