| Description | BPHA (MMP-2/MMP-9 Inhibitor II) is a potent, selective and orally active inhibitor of MMP-2, MMP-9 and MMP-14 with IC50s of 12 nM, 16 nM and 17 nM, respectively.BPHA does not inhibit MMP-1, -3 and -7 (IC50s of 974, >1000 and 795 nM, respectively).BPHA has anti-angiogenic and BPHA has anti-angiogenic and anti-tumor activities. |
| In vivo | 在小鼠中，通过口服途径每天给予BPHA（200mg/kg）能有效抑制由肿瘤引起的血管生成、原发性肿瘤生长及肝脏转移。在B16-BL6黑色素瘤和F2血管内皮瘤模型中，BPHA分别显示出48%和45%的显著生长抑制活性。[1] |
| Target activity | MMP2:12 nM, MMP9:16 nM, MMP14:17 nM, MMP1:974 nM, MMP3:>1000 nM, MMP7:795 nM |
| Synonyms | MMP-2/MMP-9 Inhibitor II |
| molecular weight | 396.46 |
| Molecular formula | C21H20N2O4S |
| CAS | 193807-60-2 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Methanol: 22.5 mg/mL (56.8 mM) DMSO: 90.0 mg/mL (227.0 mM) |
| References | 1. Maekawa R, et al. Correlation of antiangiogenic and antitumor efficacy of N-biphenyl sulfonyl-phenylalanine hydroxiamic acid (BPHA), an orally-active, selective matrix metalloproteinase inhibitor. Cancer Res. 1999;59(6):1231-1235. 2. Kohri T, et al. Reduction of experimental laser-induced choroidal neovascularization by orally administered BPHA, a selective metalloproteinase inhibitor. Graefes Arch Clin Exp Ophthalmol. 2003;241(11):943-952. 3. Maki H, et al. Antiangiogenic and antitumor effect of BPHA, an orally-active matrix metalloproteinase inhibitor, in in vivo murine and human tumor model. Gan To Kagaku Ryoho. 1999;26(11):1599-1606. |