| CAS NO: | 193807-58-8 |
| 包装: | 5mg |
| 市场价: | 2758元 |
| Physical Appearance | A solid |
| Storage | Store at 4°C |
| M.Wt | 381.4 |
| Cas No. | 193807-58-8 |
| Formula | C21H19NO4S |
| Synonyms | Metalloproteinase-2/Metalloproteinase-9 Inhibitor I |
| Solubility | ≤25mM in DMSO |
| Chemical Name | N-([1,1'-biphenyl]-4-ylsulfonyl)-D-phenylalanine |
| Canonical SMILES | O=S(C(C=C1)=CC=C1C2=CC=CC=C2)(N[C@@H](C(O)=O)CC3=CC=CC=C3)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次半岛bd体育手机客户端 溶解度各有差异，仅做参考。若实验所需浓度过大至半岛bd体育手机客户端 溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
IC50: 310 and 240 nM for MMP-2 and MMP-9, respectively
MMP-2/MMP-9 Inhibitor I is a potent inhibitor of matrix metalloproteinase-2 (MMP-2) and MMP-9.
Matrix metalloproteinase (MMP), a typical metalloproteinase, requires zinc ion at its active sites. As many as 18 kinds of MMP have been identified and cloned and are collectively called the MMP family.
In vitro: MMP-2/MMP-9 inhibitor I was identified as a potent inhibitor of matrix metalloproteinase-2 (MMP-2) and MMP-9 with IC50 values of 310 and 240 nM, respectively. MMP-2/MMP-9 inhibitor I acted by binding zinc at the active site of these MMPs. MMP-2/MMP-9 inhibitor I was found to be able to block MMP-2/MMP-9-dependent invasion in cell culture model [1].
In vivo: Both hydroxamic acid and carboxylic acid analogs of MMP-2/MMP-9 inhibitor I were evaluated for their inhibitory activities in animal cancer models. Results showed that lung colonization of Lewis lung carcinoma cells was suppressed by these inhibitors significantly. In addition, antitumor activity was also observed in the human lung cancer model. Ma44 cells growed as a solid tumor on the peritoneum after being implanted ip, and mice bearing Ma44 eventually died within 3 to 4 weeks. Daily oral administration of compound 5l led to prolonged survival of Ma44-bearing mice [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Tamura, Y. ,Watamane, F.,Nakatani, T., et al. Highly selective and orally active inhibitors of type IV collagenase (MMP-9 and MMP-2): N-sulfonylamino acid derivatives. J. Med. Chem. 41(4), 640-649 (1998).
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