Prinomastat hydrochloride
Based on 4 publication(s) in Google Scholar
Prinomastat hydrochloride (AG3340 hydrochloride) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat hydrochloride inhibits MMP-2, MMP-3, MMP-13 and MMP-9 with Kis of 0.05 nM, 0.3 nM, 0.03 nM and 0.26 nM, respectively. Prinomastat hydrochloride can cross blood-brain barrier. Antitumor avtivity.
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- Purity: 98.53%
- CAS No.: 1435779-45-5
- 화학식: C18H22ClN3O5S2
- 분자량:459.97
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Prinomastat hydrochloride
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Biological Activity
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MMP-9 5 nM (IC50) |
MMP-9 0.26 nM (Ki) |
MMP-2 0.05 nM (Ki) |
MMP-1 79 nM (IC50) |
MMP-13 6.3 nM (IC50) |
MMP-13 0.3 nM (Ki) |
collagenases 3 0.03 nM (Ki) |
Prinomastat (AG3340; 0.1-1 μg/mL; 4 days; C57MG/Wnt1 cells) inhibits Wnt1-induced MMP-3 production. Reversal of Wnt1-induced EMT and β-catenin transcriptional activity by Prinomastat[1].
Co-culture of L/Wnt3a cells and CT7 cells increases the Topflash activity in CT7 cells, and co-culturing both L/Wnt3a cells and MMP-3 overexpressing C57MG cells with CT7 cells increases the Topflash luciferase activity in CT7 cells beyond the level observed with L/Wnt3a cells, and these effects are all suppressed by Prinomastat (AG3340)[1].
Inhibition of entry of C57MG/Wnt1 cells into S phase by Prinomastat corresponds to a decrease in expression of cyclin D1 and Erk1/2 phosphorylation. The effect of Prinomastat on Wnt1-induced migration is then examined using an in vitro wound assay. As anticipated, the migration of C57MG/Wnt1 cells is increased by 1.8-fold when compared with C57MG cells.The effect of Wnt1 on the cellular distribution of vimentin is reversed by Prinomastat in C57MG/Wnt1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:C57MG/Wnt1 cells
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Concentration:0.1 µg/mL, 1 µg/mL
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Incubation Time:4 days
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Result:A significant decrease in MMP-3 promoter activity in C57MG/Wnt1 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1435779-45-5
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Appearance Solid
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분자량 459.97
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화학식 C18H22ClN3O5S2
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Color White to off-white
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SMILES
O=C([C@@H]1N(S(=O)(C2=CC=C(OC3=CC=NC=C3)C=C2)=O)CCSC1(C)C)NO.[H]Cl
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Synonyms
AG3340 hydrochloride; KB-R9896 hydrochloride
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Sci Adv
2023 Jan 20;9(3):eadd3867. PMID: 36662861 -
J Neuropathol Exp Neurol
Inhibiting Matrix Metalloproteinases Protects Evoked Electromyography Amplitudes and Muscle Tension in the Orbicularis Oris Muscle in a Rat Model of Facial Nerve Injury. [Abstract]2022 Sep 19;81(10):816-824. PMID: 35656867 -
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용액&용해도
H2O : 100 mg/mL (217.41 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (281 KB)
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SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
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Handling Instructions (2659 KB)
References
[1]. Sørensen MD, et al. Cyclic phosphinamides and phosphonamides, novel series of potent matrix metalloproteinase inhibitors with antitumour activity. Bioorg Med Chem. 2003 Dec 1;11(24):5461-84. [Content Brief]
[2]. Blavier L, et al. Stromelysin-1 (MMP-3) is a target and a regulator of Wnt1-induced epithelial-mesenchymal transition (EMT). Cancer Biol Ther. 2010 Jul 15;10(2):198-208. [Content Brief]
[3]. Shalinsky DR, et al. Broad antitumor and antiangiogenic activities of AG3340, a potent and selective MMP inhibitor undergoing advanced oncology clinical trials. Ann N Y Acad Sci. 1999 Jun 30;878:236-70. [Content Brief]
[4]. Ozerdem U, et al. The effect of prinomastat (AG3340), a potent inhibitor of matrix metalloproteinases, on a subacute model of proliferative vitreoretinopathy. Curr Eye Res. 2000 Jun;20(6):447-53. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 2.1741 mL | 10.8703 mL | 21.7405 mL | 54.3514 mL |
| 5 mM | 0.4348 mL | 2.1741 mL | 4.3481 mL | 10.8703 mL | |
| 10 mM | 0.2174 mL | 1.0870 mL | 2.1741 mL | 5.4351 mL | |
| 15 mM | 0.1449 mL | 0.7247 mL | 1.4494 mL | 3.6234 mL | |
| 20 mM | 0.1087 mL | 0.5435 mL | 1.0870 mL | 2.7176 mL | |
| 25 mM | 0.0870 mL | 0.4348 mL | 0.8696 mL | 2.1741 mL | |
| 30 mM | 0.0725 mL | 0.3623 mL | 0.7247 mL | 1.8117 mL | |
| 40 mM | 0.0544 mL | 0.2718 mL | 0.5435 mL | 1.3588 mL | |
| 50 mM | 0.0435 mL | 0.2174 mL | 0.4348 mL | 1.0870 mL | |
| 60 mM | 0.0362 mL | 0.1812 mL | 0.3623 mL | 0.9059 mL | |
| 80 mM | 0.0272 mL | 0.1359 mL | 0.2718 mL | 0.6794 mL | |
| 100 mM | 0.0217 mL | 0.1087 mL | 0.2174 mL | 0.5435 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.