Chemical Name:N-[(2R)-2-[2-(Hydroxyamino)-2-oxoethyl]-4-methyl-1-oxopentyl]-3-methyl-L-valyl-N-(2-aminoethyl)-L-alaninamide
Purity: ≥95% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
ADAM-17 (TACE) and MMP inhibitor (Ki = 120 nM at ADAM-17). Sensitizes cancer stem cells to the lethal effects of 5-FU in vitro. Blocks shedding of TNF-α from cell membranes.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solubility
Soluble to 5 mg/ml in water and to 5 mg/ml in ethanol
Preparing Stock Solutions
The following data is based on the product molecular weight 415.54. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.41 mL
12.03 mL
24.07 mL
5 mM
0.48 mL
2.41 mL
4.81 mL
10 mM
0.24 mL
1.2 mL
2.41 mL
50 mM
0.05 mL
0.24 mL
0.48 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Mosset al (2007) Fluorescent substrates for the proteinases ADAM17, ADAM10, ADAM8, and ADAM12 useful for high-throughput inhibitor screening. Anal.Biochem. 366 144 PMID: 17548045
Wanget al (2016) A disintegrin and metalloproteinase domain 17 regulates colorectal cancer stem cells and chemosensitivity via notch1 signaling. Stem Cells Transl.Med. 5 331 PMID: 26744411