ARP-100

Names

[ Name ]:
ARP-100

[Synonym ]:
MMP-2 Inhibitor III
ARP 100
N-(4-Biphenylylsulfonyl)-N-hydroxy-N-isopropoxyglycinamide
N-(biphenyl-4-ylsulfonyl)-N-hydroxy-N-(propan-2-yloxy)glycinamide
Acetamide, 2-[([1,1'-biphenyl]-4-ylsulfonyl)(1-methylethoxy)amino]-N-hydroxy-

Biological Activity

[Description]:

ARP-100 is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC50=12 nM). ARP-100 interacts with S1＇ pocket of MMP-2 and shows anti-invasive properties in an in vitro model of invasion on matrigel. ARP-100 shows the less inhibitory activity towards MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM), and MMP-9 (0.2 μM)[1][2].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> MMP

[Target]

MMP-2:12 nM (IC50)

MMP-9:0.2 μM (IC50)

MMP-3:4.5 μM (IC50)

MMP-1:>50 μM (IC50)

MMP-7:>50 μM (IC50)

[In Vitro]

ARP-100 (50 nM) shows a significant reduction in the total number of invasive elongations[1].

[References]

[1]. Rossello A, et al. New N-arylsulfonyl-N-alkoxyaminoacetohydroxamic acids as selective inhibitors of gelatinase A (MMP-2). Bioorg Med Chem. 2004 May 1;12(9):2441-50.

[2]. Tuccinardi T, et al. Amber force field implementation, molecular modelling study, synthesis and MMP-1/MMP-2 inhibition profile of (R)- and (S)-N-hydroxy-2-(N-isopropoxybiphenyl-4-ylsulfonamido)-3-methylbutanamides. Bioorg Med Chem. 2006 Jun 15;14(12):4260-76.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Molecular Formula ]:
C₁₇H₂₀N₂O₅S

[ Molecular Weight ]:
364.416

[ Exact Mass ]:
364.109283

[ PSA ]:
104.32000

[ LogP ]:
2.08

[ Index of Refraction ]:
1.589

Safety Information

[ HS Code ]:
2935009090

Customs

[ HS Code ]: 2935009090

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%