| CAS | 323577-36-2 |
| Sequence | Mca-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys(Dnp)-OH |
| Sequence Single | Mca-RPPGFSAFK(Dnp)-OH |
| Molecular Formula | C66H81N15O19 |
| Molecular Weight | 1388.46 |
| Synonyms | Substrate V |
| Technology | Synthetic |
| Storage | -20°C, avoid light, cool and dry place |
| Application | Cancer Research|Cardiovascular System & Diseases|Inflammation Research |
| Description | Mca-(Ala7,Lys(Dnp)9)-Bradykinin also called substrate V, Mca-RPPGFSAFK(Dnp), is a very sensitive internally quenched fluorescent substrate for endothelin-converting enzyme-1 (ECE-1) a membrane-bound zinc metallopeptidase that is related to neprilysin in amino acid sequence. The kcat/Km value for the hydrolysis by ECE-1 was 1.9 x 10⁷ M-1s-1 and 1.7 x 10⁶ M-1s-1 for the hydrolysis by neprilysin. This FRET substrate was hydrolyzed rapidly by stromelysin 1 (MMP-3) with kcat/Km= 218000 M⁻¹s⁻¹ and very slowly by gelatinase B (MMP-9) (kcat/Km= 10100 M-1s-1). There was no hydrolysis by MMP-1 and MMP-2. Mca-(Ala7,Lys(Dnp)9)-Bradykinin has also found use as substrate for insulin-degrading enzyme (IDE) and ACE2. |
| References | 1. 2, 5-diketopiperazines (cyclic dipeptides) in beef: identification, synthesis, and sensory evaluation. M.Z.Chen et al., J. Food Sci., 74, C100 (2009) 2. Immunocapture-based fluorometric assay for the measurement of insulin-degrading enzyme activity in brain tissue homogenates. J.M.Miners et al., J. Neurosci. Methods, 169, 177 (2008) |