| Description | MMP-2/MMP-9-IN-1 is a potent, highly selective and orally bioavailable inhibitor of type IV collagenases (MMP-9 and MMP-2) with an IC50 of 0.24 and 0.3 1 μM for MMP-9 and MMP-2, respectively. activity, which can be used to study cancer. |
| In vitro | MMP-2/MMP-9 Inhibitor I被确认为一种强效的基质金属蛋白酶-2（MMP-2）和MMP-9抑制剂，其IC50值分别为310和240 nM。MMP-2/MMP-9 Inhibitor I通过结合这些MMPs的活性部位上的锌来发挥作用。研究发现，MMP-2/MMP-9 Inhibitor I能够阻断细胞培养模型中基于MMP-2/MMP-9的侵袭。[1] |
| In vivo | MMP-2/MMP-9 Inhibitor I的羟胺酸和羧酸类似物在动物癌症模型中的抑制活性被评估。结果显示，这些抑制剂显著抑制了Lewis肺癌细胞的肺部定植。此外，在人类肺癌模型中也观察到了抗肿瘤活性。Ma44细胞在被腹腔内植入后，以实体肿瘤的形式在腹膜上生长，携带Ma44的小鼠最终在3到4周内死亡。5l化合物的每日口服给药使携带Ma44的小鼠的存活时间延长。[1] |
| Target activity | MMP2:0.31 μM, MMP9:0.24 μM |
| molecular weight | 381.44 |
| Molecular formula | C21H19NO4S |
| CAS | 193807-58-8 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 180.0 mg/mL (471.9 mM) |
| References | 1. Tamura Y, et al. Highly selective and orally active inhibitors of type IV collagenase (MMP-9 and MMP-2): N-sulfonylamino acid derivatives. J Med Chem. 1998;41(4):640-649. |