MMP-9-IN-1 |
رقم الكتالوجGC38929
One-Click Copy Product Info
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MMP-9-IN-1 هو مثبط محدد للبروتيناز المعدني المصفوفي 9 (MMP-9) ، والذي يستهدف بشكل انتقائي مجال hemopexin (PEX) لـ MMP-9 ، ولكن ليس MMPs الأخرى
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 502887-71-0
Sample solution is provided at 25 µL, 10mM.
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MMP-9-IN-1 is a selective inhibitor of matrix metalloproteinase-9 (MMP-9)，it works by targeting the plasma ceruloplasmin (PEX) domain of MMP-9, with a Kd value of 2.1μM[1]. MMPs consist of a pro-peptide sequence, a catalytic (CAT) metalloproteinase domain, a hinge region or linker peptide, and a hemopexin (PEX) domain, among which the PEX domain is particularly important[2]. MMP-9 plays key roles in various physiological and pathological processes, including extracellular matrix remodeling, tissue repair, inflammatory responses, and tumor invasion and metastasis[3]. Therefore, MMP-9-IN-1 is often used in related research areas such as cancer, inflammatory diseases, and neurodegenerative diseases[4-6].
In vitro, treatment of HT-1080 and MDA-MB-435 cells with 10μM MMP-9-IN-1 for 9 days significantly inhibits cell proliferation, migration and invasion without affecting cell viability[1]. Treatment of BMSCs with 10μM MMP-9-IN-1 for 72h significantly inhibited MMP-9 activity but no significant effect on the proliferation[7].
In vivo, C57BL6/J mice were intraperitoneally injected with MMP-9-IN-1 three days after ovariectomy (2mg/kg twice a week, for 8 weeks), MMP-9-IN-1 increased osteogenic differentiation protein expression, histone acetylation, promoted citric acid and acetyl-CoA secretion in BMSCs and restored osteogenic matrix formation in osteoblasts[7].
References:
[1] Dufour, A., Sampson, N. S., Li, J., Kuscu, C., Rizzo, R. C., Deleon, J. L., Zhi, J., Jaber, N., Liu, E., Zucker, S., & Cao, J. (2011). Small-molecule anticancer compounds selectively target the hemopexin domain of matrix metalloproteinase-9. Cancer research, 71(14), 4977–4988.
[2] Okusha, Y., Eguchi, T., Sogawa, C., Okui, T., Nakano, K., Okamoto, K., & Kozaki, K. I. (2018). The intranuclear PEX domain of MMP involves proliferation, migration, and metastasis of aggressive adenocarcinoma cells. Journal of cellular biochemistry, 119(9), 7363–7376.
[3] Farina, A. R., & Mackay, A. R. (2014). Gelatinase B/MMP-9 in Tumour Pathogenesis and Progression. Cancers, 6(1), 240–296.
[4] Das, S., Amin, S. A., & Jha, T. (2021). Inhibitors of gelatinases (MMP-2 and MMP-9) for the management of hematological malignancies. European journal of medicinal chemistry, 223, 113623.
[5] Rashid, Z. A., & Bardaweel, S. K. (2023). Novel Matrix Metalloproteinase-9 (MMP-9) Inhibitors in Cancer Treatment. International journal of molecular sciences, 24(15), 12133.
[6] Alford, V. M., Kamath, A., Ren, X., Kumar, K., Gan, Q., Awwa, M., Tong, M., Seeliger, M. A., Cao, J., Ojima, I., & Sampson, N. S. (2017). Targeting the Hemopexin-like Domain of Latent Matrix Metalloproteinase-9 (proMMP-9) with a Small Molecule Inhibitor Prevents the Formation of Focal Adhesion Junctions. ACS chemical biology, 12(11), 2788–2803.
[7] Da, W., Jiang, W., & Tao, L. (2024). ROS/MMP-9 mediated CS degradation in BMSC inhibits citric acid metabolism participating in the dual regulation of bone remodelling. Cell death discovery, 10(1), 77.
| Cell experiment [1]: | |
Cell lines | human HT-1080, and MDA-MB-435 cancer cell lines |
Preparation Method | Human HT-1080, and MDA-MB-435 cancer cell lines were maintained in DMEM (Invitrogen) containing 10% fetal calf serum. Cells (5 × 103 ) were added to a 96-well plate in the presence or absence of MMP-9-IN-1(10μM) for 9 days. Cell proliferation, migration, invasion and cytotoxicity weredetermined using the CellTiter-Glo™ Luminescent Assay. |
Reaction Conditions | 10μM; 9 days |
Applications | MMP-9-IN-1 significantly inhibits cell proliferation, migration and invasion without affecting cell viability. |
| Animal experiment [2]: | |
Animal models | SPF grade C57BL6/J mice |
Preparation Method | Ten week-old female SPF grade C57BL6/J mice were randomly divided into 4 groups (6 mice in each group): control group (CON), sham operation group (Sham), ovariectomy group (OVX) and ovariectomy+MMP-9 inhibitor group (OVX + MMP-9-IN-1. Mice in the sham-operated group underwent dorsal skin excision and periovarian fat excision, while mice in the OVX group underwent bilateral oophorectomy after anaesthesia with an animal anaesthesia machine (oxygen flow was 0.5L/min, isoflurane inhalation concentration was 1%-3%). The OVX + MMP-9-IN-1 group was intraperitoneally injected with MMP-9-IN-1 three days after ovariectomy (2mg/kg, twice a week, for 8 weeks), and the other mice were injected with the same dose of phosphate-buffered saline (PBS). After 8 weeks of feeding, the mice were sacrificed by cervical dislocation, and the limbs were collected. Metabolite determination was carried out using ultrahigh-performance liquid chromatography–tandem mass spectrometry. Cells were harvested for Western blot. |
Dosage form | 2mg/kg, twice a week, for 8 weeks; i.p. |
Applications | MMP-9-IN-1 increased osteogenic differentiation protein expression, histone acetylation, promoted citric acid and acetyl-CoA secretion in BMSCs and restored osteogenic matrix formation in osteoblasts. |
References: | |
| Cas No. | 502887-71-0 | SDF | |
| Canonical SMILES | O=C(NC1=CC=C(OC(F)F)C=C1)CSC2=NC(CCC)=CC(N2)=O | ||
| Formula | C16H17F2N3O3S | M.Wt | 369.39 |
| الذوبان | DMSO: 125 mg/mL (338.40 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7072 mL | 13.5358 mL | 27.0717 mL |
| 5 mM | 541.4 μL | 2.7072 mL | 5.4143 mL |
| 10 mM | 270.7 μL | 1.3536 mL | 2.7072 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)