The ADAM17 Fluorometric (also known as fluorimetric) Drug Discovery Kit is a complete assay system designed to screen ADAM17 (TACE) inhibitors using a quenched fluorogenic peptide: Mca-PLAQAV-Dpa-RSSSR-NH2. Mca fluorescence is quenched by the Dpa group until cleavage by proteases separates the two moieties. The assays are performed in a convenient 96-well microplate format. The kit is useful to screen inhibitors of ADAM17, a potential therapeutic target. The compound GM6001 is also included as a prototypic control inhibitor.
Product Details
| Alternative Name: | TACE, A disintegrin and metalloproteinase 17 |
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| Applications: | Fluorescent detection, HTS
Activity assay
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| Application Notes: | Designed to screen ADAM17 (TACE) inhibitors using a quenched fluorogenic peptide. |
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| Handling: | Avoid freeze/thaw cycles. |
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| Shipping: | Dry Ice |
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| Long Term Storage: | -80°C |
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| Contents: | 1 vial ADAM17 enzyme
1 vial Substrate (Mca-PLAQAV-Dpa-RSSSR-NH2)
1 vial CALIBRATION STANDARD
1 vial control inhibitor (GM6001)
1 bottle (20 ml) assay buffer
1 black 96-well microplate
Instructions |
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| Scientific Background: | TACE/ADAM17 (Tumor necrosis factor-α-converting enzyme; A Disintegrin And Metalloproteinase 17) is a soluble or membrane-bound metalloproteinase primarily responsible for activation of proTNF-α, while also targeting proteins such as fractalkine, amyloid precursor proteins, and CD40. ADAM17/TACE is involved in cancer, vascular disorders, and inflammatory diseases such as rheumatoid arthritis and focal ischemic injury. The catalytic domain of ADAM17/TACE is able to cleave proTNF-α and is used in inhibitor screening. |
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| UniProt ID: | P78536 |
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| Regulatory Status: | RUO - Research Use Only |
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General Literature References
Insulin-like growth factor-1 (IGF-1)-induced processing of amyloid-{beta} precursor protein (APP) and APP-like protein 2 is mediated by different metalloproteinases: K.T. Jacobsen, et al.; J. Biol. Chem.
285, 10223 (2010),
Abstract;
Novel TACE inhibitors in drug discovery: a review of patented compounds: P.R. Murumkar, et al.; Expert Opin. Ther. Pat.
20, 31 (2010),
Abstract;
The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors: K.E. Rosner, et al.; Bioorg. Med. Chem. Lett.
20, 1189 (2010),
Abstract;
ADAM17 as a therapeutic target in multiple diseases: J. Arribas & C. Esselens; Curr. Pharm. Des.
15, 2319 (2009),
Abstract;
Synthesis and activity of quinolinylmethyl P1’ alpha-sulfone piperidine hydroxamate inhibitors of TACE: C. Zhang, et al.; Bioorg. Med. Chem. Lett.
19, 3445 (2009),
Abstract;
Inhibition of tumor necrosis factor-alpha-converting enzyme by a selective antagonist protects brain from focal ischemic injury in rats: X. Wang, et al.; Mol. Pharmacol.
65, 890 (2004),
Abstract;
Membrane-anchored CD40 is processed by the tumor necrosis factor-alpha-converting enzyme. Implications for CD40 signaling: C. Contin, et al.; J. Biol. Chem.
278, 32801 (2003),
Abstract;
Design, synthesis and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo: C.-B. Xue, et al.; J. Med. Chem.
44, 2636 (2001),
Abstract;
Tumor necrosis factor-alpha-converting enzyme (ADAM17) mediates the cleavage and shedding of fractalkine (CX3CL1): K.J. Garton, et al.; J. Biol. Chem.
276, 37993 (2001),
Abstract;
TNF-alpha convertase enzyme from human arthritis-affected cartilage: isolation of cDNA by differential display, expression of the active enzyme, and regulation of TNF-alpha: I.R. Patel, et al.; J. Immunol.
160, 4570 (1998),
Abstract;
Cloning of a disintegrin metalloproteinase that processes precursor tumour-necrosis factor-alpha: M.L. Moss, et al.; Nature
385, 733 (1997),
Abstract;
