(2R)-2-[([1,1μ-Biphenyl]-4-ylsulfonyl)(1-methylethoxy)amino]-N-hydroxy-3-methyl-butanamide, (R)-N-Hydroxy-2-(N-isopropoxybiphenyl-4-ylsulfonamido)-3-methylbutanamide

Uses

ARP 101i inhibits α-MSH-stimulated melanogenesis by regulation of autophagy in melanocytes and also induces autophagy in various cancer cells.

Definition

ChEBI: N(2)-([biphenyl]-4-ylsulfonyl)-N-hydroxy-N(2)-isopropoxy-D-valinamide is a hydroxamic acid that is N-hydroxy-D-valinamide in which the alpha-amino group has been substituted by isopropoxy and [biphenyl]-4-ylsulfonyl groups. A selective matrix metalloproteinase-2 (MMP-2) inhibitor, it is one of the most potent inducers of autophagy. Its physiological roles include angiogenesis, cancer metastasis, embryogenesis, tissue remodeling in development, and wound healing. It has a role as an EC 3.4.24.24 (gelatinase A) inhibitor, an autophagy inducer, an antineoplastic agent and a melanin synthesis inhibitor. It is a hydroxamic acid and a D-valine derivative.

Biological Activity

ARP 101 is a MMP-2 selective inhibitor (Gelatinase A, EC 3.4.24.24; TBE-1; LG4A; MONA; Type IV Collagenase). ARP 101 has diverse physiological roles including wound healing, cancer metastasis, angiogenesis, tissue remodeling in development and embryogenesis. IC50 = 0.81 nM on MMP-2.