Mca-Lys-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 (fluorogenic substrate)

Sensitive fluorogenic substrate for most matrix metalloproteinase (MMP) enzymes, as follows [k_cat/K_m (M^-1s^-1) and K_m (µM), in parentheses]: MMP-1 (9.2 x 10⁴, 27); MMP-2 (6.9×10⁵, >30); MMP-3 (2.0×10⁴); MMP-7 (2.9×10⁵); MMP-8 (4.2×10⁵); MMP-9 (6.2×10⁵, >30); MMP-12 (1.3×10⁵, 130); MMP-13 (1.1×10⁶, 5.2); MMP-14 (1.3×10⁶, 7.9); mouse, rat, and monkey MMP-14; MMP-16; MMP-20; ADAM10 (1.1×10³); ADAM17/TACE (7.8×10⁵, 26), and BACE2 (internal data using Prod. No. BML-SE550). It is cleaved very poorly by neutrophil elastase, and not at all by trypsin. Can be used to measure cell-associated activity, or activity in cell-conditioned medium, or in biological fluids such as synovial fluid. Mca fluorescence is quenched by the Dpa group until cleavage separates them (MMPs cleave between Gly-Leu). Ex.: 328nm, Em.: 400nm, but it is possible to use Ex./Em. 320-340/393-420nm. This highly-quenched (98.4%) substrate is useful for inhibitor screening and kinetic analysis.