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MMP-2/MMP-9 Inhibitor II

Names

[ CAS No. ]:
193807-60-2

[ Name ]:
MMP-2/MMP-9 Inhibitor II

[Synonym ]:
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

Biological Activity

[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]:

Research Areas >> Cancer
Signaling Pathways >> Metabolic Enzyme/Protease >> MMP

[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.  

Chemical & Physical Properties

[ 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


Related Compounds

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