OM99-2

OM99-2, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin 2 with a Ki value of 9.58 nM[1]. OM99-2 is significantly advanced the development of BACE1 inhibitor[2]. OM99-2 has the potential for the research of the Alzheimer's disease[3].

Cell permeable: no', 'Primary Target
human brain memapsin 2', 'Product does not compete with ATP.', 'Reversible: no', 'Target Ki: 1.6 nM against recombinant memapsin 2; 9.58 nM against recombinant pro-memapsin 2; 48 nM against cathepsin D

BACE1

[1] Ghosh AK, et al. Design of Potent Inhibitors for Human Brain Memapsin 2 (β-Secretase). J Am Chem Soc. 2000;122(14):3522-3523. DOI:10.1021/ja000300g
[2] Zhao J, et al. Targeting Amyloidogenic Processing of APP in Alzheimer's Disease. Front Mol Neurosci. 2020;13:137. Published 2020 Aug 4. DOI:10.3389/fnmol.2020.00137
[3] Dash C, et al. Aspartic peptidase inhibitors: implications in drug development. Crit Rev Biochem Mol Biol. 2003;38(2):89-119. DOI:10.1080/713609213
[4] Park H, et al. Determination of the active site protonation state of beta-secretase from molecular dynamics simulation and docking experiment: implications for structure-based inhibitor design. J Am Chem Soc. 2003;125(52):16416-16422. DOI:10.1021/ja0304493