Bioactivity | BPHA is a potent and orally active MMP-2, MMP-9 and MMP-14 inhibitor with IC50s of 12 nM, 16 nM and 17 nM, respectively. BPHA does not inhibit MMP-1, -3, and -7 (the IC50s are 974, >1000, and 795 nM, respectively). BPHA has antiangiogenic and antitumor effects[1]. |
Invitro | BPHA does not inhibit typical serine proteinases (neutrophil elastase, plasmin, trypsin, and chymotrypsin), cysteine proteinases (cathepsins B and L), aspartic proteinase (HIV-1 protease), or metalloproteinase (aminopeptidase M)[1]. |
In Vivo | Daily oral administration of 200 mg/kg BPHA in mice results in potent inhibition of tumor-induced angiogenesis, primary tumor growth, and liver metastasis. The growth inhibition activity of BPHA is 48% and 45% in a B16-BL6 melanoma and F2 hemangio-endothelioma model, respectively[1]. |
Name | BPHA |
CAS | 193807-60-2 |
Formula | C21H20N2O4S |
Molar Mass | 396.46 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. R Maekawa, 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 Mar 15;59(6):1231-5. |