MMP activity is involved in many disease-related phenomena including cancer propagation, invasion and metastasis, rheumatoid arthritis, and areas of cardiovascular disease. Imaging MMP activity in vivo can provide insights into disease processes and assist in the development of novel therapeutics.
MMPSense mechanism of activation in the presence of matrix metalloproteases
MMPSense in vitro activation profile
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Specificity of activatable agent: figure shows in vitro activation of MMPSense in the presence of a range of MMPs and plasmin.
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About matrix metalloproteases |
MMPs are Zn2+-dependent neutral endopeptidases. Twenty four human MMP genes have already been identified and several MMP inhibitors are in clinical trials, emphasizing the significance of this group of enzymes. In normal tissue, MMPs are often involved in embryonic growth and tissue morphogenesis. These enzymes have been linked to the aggressiveness of tumors, to apoptopsis and angiogenesis, to degradation of extracellular matrix and basement membrane and to inflammation and degradation of cartilage in arthritis.
| MMPSense 680 |
| MMPSense 680 absorbance and emission spectra in PBS |
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| MW |
~450,000 g mol-1 |
| Fluorescence Excitation |
680 ±10 nm |
| Fluorescence Emission |
700 ±10 nm |
| Absorbance |
680 ±10 nm |
| Purity (determined by SE-HPLC, measuring absorbance at 680 nm) |
>95% |
| Appearance |
Clear blue solution |
1 Absorbance and fluorescence maxima in PBS.
Changes in protease activity are seen in a number of pathological states and disease-related events, including rheumatoid arthritis, cancer, atherosclerosis, angiogenesis and cardiovascular disease. For example, cathepsin B is known to be up-regulated in colon cancer and cathepsins B, C, D, G, K, L and S, plasmin, plasma kallikrein, uPA and CD10 are associated with the development and maintenance of arthritis.
ProSense mechanism of activation in the presence of cathepsins
ProSense protease in vitro activation profile
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Specificity of activatable agent: figure shows in vitro activation of ProSense in the presence of a range of cathepsins, Klk5 (kallikrein-related peptidase 5), uPA (urokinase plasminogen activator) and CD10.
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About cathepsins |
Cathepsins are globular endopeptidases, usually with a cysteine active site. More than 12 different cathepsins have been identified with different structures and specificities. They are primarily lysosomal enzymes, many of them becoming active at low pH. In normal tissue, they are involved in intra- and extra-cellular protein turnover e.g. osteoclastic bone resorption and antigen presentation by macrophages. In tumors they are involved in degradation of collagen and elastin and in initiation, metastasis and apotopsis. Cathepsin B levels have been correlated with the degree of malignancy. Cathpesin B and L levels are used to monitor tumor progression.
| ProSense 680, ProSense 680 Control |
| ProSense 680 absorbance and emission spectra in PBS |
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| MW |
~400,000 g mol-1 |
| Fluorescence Excitation |
680 ±10 nm |
| Fluorescence Emission |
700 ±10 nm |
| Absorbance |
680 ±10 nm |
| Purity (determined by SE-HPLC, measuring absorbance at 680 nm) |
>95% |
| Appearance |
Clear blue solution |
1 Absorbance and fluorescence maxima in PBS.
| ProSense 750, ProSense 750 Control |
| ProSense 750 absorbance and emission spectra in PBS |
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| MW |
~400,000 g mol-1 |
| Fluorescence Excitation |
750 ±10 nm |
| Fluorescence Emission |
780 ±10 nm |
| Absorbance |
750 ±10 nm |
| Purity (determined by SE-HPLC, measuring absorbance at 750 nm) |
>95% |
| Appearance |
Clear blue solution |
1 Absorbance and fluorescence maxima in PBS.
The products below are supplied in concentrated form for dilution in 1 x PBS (not supplied) prior to injection.
| Product |
Supplied concentration |
Recommended injection concentration |
Recommended injection volume for an ~25 gram mouse |
| MMPSense 680 |
20 nmol/1.5 ml in 1 x PBS |
2 nmol /150μl in 1 x PBS |
150 μl |
| ProSense 750 |
20 nmol/150 μl in 1 x PBS |
2 nmol /150μl in 1 x PBS |
150 μl |
| ProSense 680 |
20 nmol/150μl in 1 x PBS |
2 nmol /150μl in 1 x PBS |
150 μl |
Allow fluorescence agents to reach room temperature before injection.
Inject agents intravenously via the tail vein.
Use a small gauge (27G) needle and dispense slowly into the tail vein.
