193807-60-2

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	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.