| Description | Ilomastat (GM6001) (GM6001, Galardin) is a broad spectrum matrix metalloprotease (MMP) inhibitor. |
| In vivo | 局部应用GM6001 (400 μg/ml) 可预防严重碱伤后的角膜溃疡。[3] 在兔模型中，支架置入后，GM6001 显著抑制内膜增生和内膜胶原含量，并在不影响增殖率的情况下增加支架动脉的腔内面积。[4] |
| Target activity | MMP1:0.4 nM(Ki), MMP2:0.5 nM(Ki), MMP26:0.36 nM(Ki), MMP9:0.2 nM(Ki), MMP8:0.1 nM(Ki) |
| Synonyms | Galardin, GM6001, 伊洛马司他 |
| molecular weight | 388.46 |
| Molecular formula | C20H28N4O4 |
| CAS | 142880-36-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 38.9 mg/mL (100 mM) |
| References | 1. Grobelny D, et al. Biochemistry, 1992, 31(31), 7152-714. 2. Leppert D, et al. J Immunol,1995, 154(9), 4379-4389. 3. Schultz GS, et al. Invest Ophthalmol Vis Sci, 1992, 33(12) 3325-3331. 4. Li C, et al. J Am Coll Cardiol, 2002, 39(11), 1852-1858. 5. Luan F, Yu Z, Yin L, et al. Accurate detection of matrix metalloproteinase-2 activity in clinical gastric cancer tissues using a fluorescent probe[J]. Analytical Methods. 2019, 11(11): 1516-1521. 6. Xia J, Sun S, Wu X, et al. Enzyme-activated anchoring of peptide probes onto plasma membranes for selectively lighting up target cells[J]. Analyst. 2020 7. Xia J, Sun S, Wu X, et al. Enzyme-activated anchorage of peptide probes on plasma membrane for selectively lighting up target cells. Analyst. 2020 8. Yin L, Sun H, Zhao M, et al. Rational Design and Synthesis of a Metalloproteinase-Activatable Probe for Dual-Modality Imaging of Metastatic Lymph Nodes in Vivo[J]. The Journal of organic chemistry. 2019 May 17;84(10):6126-6133. 9. Yin L, Sun H, Zhang H, et al. Quantitatively Visualizing Tumor-related Protease Activity In Vivo Using A Ratiometric Photoacoustic Probe[J]. Journal of the American Chemical Society. 2019 Feb 20;141(7):3265-3273. |
| Citations | 1. Sun Y, Lyu B, Yang C, et al. An enzyme-responsive and transformable PD-L1 blocking peptide-photosensitizer conjugate enables efficient photothermal immunotherapy for breast cancer. Bioactive Materials. 2023, 22: 47-59. 2. Yin L, Sun H, Zhang H, et al. Quantitatively Visualizing Tumor-related Protease Activity In Vivo Using A Ratiometric Photoacoustic Probe. Journal of the American Chemical Society. 2019 Feb 20;141(7):3265-3273. 3. Yin L, Sun H, Zhao M, et al. Rational Design and Synthesis of a Metalloproteinase-Activatable Probe for Dual-Modality Imaging of Metastatic Lymph Nodes in Vivo. The Journal of Organic Chemistry. 2019 May 17;84(10):6126-6133 4. Xia J, Sun S, Wu X, et al. Enzyme-activated anchoring of peptide probes on plasma membrane for selectively lighting up target cells. Analyst. 2020 5. Luan F, Yu Z, Yin L, et al. Accurate detection of matrix metalloproteinase-2 activity in clinical gastric cancer tissues using a fluorescent probe. Analytical Methods. 2019, 11(11): 1516-1521 6. Cheng Z, Jin Y, Li J, et al.Fibronectin-targeting and metalloproteinase-activatable smart imaging probe for fluorescence imaging and image-guided surgery of breast cancer.Journal of Nanobiotechnology.2023, 21(1): 1-16. |