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193807-60-2

193807-60-2 structure
193807-60-2 structure
  • Name: MMP-2/MMP-9 Inhibitor II
  • Chemical Name: Nα-(4-Biphenylylsulfonyl)-N-hydroxy-D-phenylalaninamide
  • CAS Number: 193807-60-2
  • Molecular Formula: C21H20N2O4S
  • Molecular Weight: 396.460
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease MMP
  • Create Date: 2018-06-22 21:10:16
  • Modify Date: 2024-01-07 07:22:21
  • BPHA is a potent and orally active MMP-2, MMP-9 and MMP-14 inhibitor with 50s 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].

Name Nα-(4-Biphenylylsulfonyl)-N-hydroxy-D-phenylalaninamide
Synonyms Nα-(4-Biphenylylsulfonyl)-N-hydroxy-D-phenylalaninamide
Benzenepropanamide, α-[([1,1'-biphenyl]-4-ylsulfonyl)amino]-N-hydroxy-, (αR)-
Nα-(biphenyl-4-ylsulfonyl)-N-hydroxy-D-phenylalaninamide
Description BPHA is a potent and orally active MMP-2, MMP-9 and MMP-14 inhibitor with 50s 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].
Related Catalog
Target

MMP-2:12 nM (IC50)

MMP-9:16 nM (IC50)

MMP-14:17 nM (IC50)

MMP-1:974 nM (IC50)

MMP-3:>1000 nM (IC50)

MMP-7:795 nM (IC50)

In Vitro BPHA 不抑制典型的丝氨酸蛋白酶(中性粒细胞弹性蛋白酶、纤溶酶、胰蛋白酶和胰凝乳蛋白酶)、半胱氨酸蛋白酶(组织蛋白酶 B 和 L)、天冬氨酸蛋白酶(HIV-1 蛋白酶)或金属蛋白酶(氨肽酶 M)[1]< /sup>。
In Vivo antiangiogenic and antitumor effects, MMP-2, MMP-9, MMP-14, orally active小鼠每日口服 200 mg/kg BPHA 可有效抑制肿瘤诱导的血管生成、原发性肿瘤生长和肝转移。BPHA 在 B16-BL6 黑色素瘤和 F2 血管内皮瘤模型中的生长抑制活性分别为 48% 和 45%[1]。
References

[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.  

Density 1.3±0.1 g/cm3
Molecular Formula C21H20N2O4S
Molecular Weight 396.460
Exact Mass 396.114380
LogP 3.23
Index of Refraction 1.630