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MMP-2/MMP-9 Inhibitor I
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MMP-2/MMP-9 Inhibitor I图片
CAS NO:193807-58-8
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
MMP-2/MMP-9 Inhibitor I 是一种高选择性、口服活性和有效的 IV 型胶原酶(MMP-9 和 MMP-2)抑制剂,IC50 分别为 0.24 和 0.31 μM 分别用于 MMP-9 和 MMP-2 . MMP-2/MMP-9 Inhibitor I 在肿瘤生长和转移的动物模型中具有口服活性。 MMP-2/MMP-9 Inhibitor I可用于癌症研究。
Cas No.193807-58-8
别名胶原酶,Metalloproteinase-2/Metalloproteinase-9 Inhibitor I
化学名N-([1,1'-biphenyl]-4-ylsulfonyl)-D-phenylalanine
Canonical SMILESO=S(C(C=C1)=CC=C1C2=CC=CC=C2)(N[C@@H](C(O)=O)CC3=CC=CC=C3)=O
分子式C21H19NO4S
分子量381.4
溶解度≤25mM in DMSO
储存条件Store at 4℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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).