- 商品介绍
- 规格参数
- 包装参数
General description
This compound is a cell-permeable, selective, and reversible thiopyrimidone MMP-9 allosteric inhibitor that binds specifically to the non-catalytic site of MMP-9 at the PEX domain with a Kd = 2.1 µM and thereby disrupts MMP-9 homodimerization and its cross-talk with CD44 and the EGFR-MAPK signaling pathway. It does not bind to the PEX domain of MMP-2 or MT1-MMP and it is shown to decrease MMP-9 mediated cell migration in COS-1 cells at 100 µM. Also, it inhibits cell migration and invasion of HT-1080 and MDA-MB-435 human cancer cells in a dose-dependent manner from 0.1 to 100 µM, without altering MMP-9 expression or proteolytic activity in HT-1080 cells. In addition, it attenuates both primary tumor growth and metastasis in vivo in a mouse model without obvious toxicity (20 mg/kg, 6 days/week, i.v. and i.t.).
Packaging
Packaged under inert gas
Other Notes
Dufour, A., et al. 2011. Cancer Res.71, 4977.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | yellow-white |
| solubility | DMSO: 50 mg/mL, light yellow |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | O=C(CSC(NC(CCC)=C1)=NC1=O)NC2=CC=C(OC(F)F)C=C2 |
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¥ 1082.93
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¥ 1048.84
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¥ 638.71
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¥ 805.47
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¥ 782.57
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¥ 4110.85
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¥ 1066.63
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¥ 619.92
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¥ 298.24
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¥ 165230.53
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¥ 75435.65
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