OM99-2 TFA

Names

[ Name ]:
OM99-2 TFA

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> Beta-secretase

Research Areas >> Neurological Disease

[Target]

Ki: 9.58 nM (memapsin 2)

[In Vitro]

Memapsin 2 (BACE) is an aspartyl protease known as beta-secretase that acts on the production of the beta-amyloid peptide in the human brain[4].

[References]

[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.

[2]. Zhao J, et al. Targeting Amyloidogenic Processing of APP in Alzheimer's Disease. Front Mol Neurosci. 2020;13:137. Published 2020 Aug 4.

[3]. Dash C, et al. Aspartic peptidase inhibitors: implications in drug development. Crit Rev Biochem Mol Biol. 2003;38(2):89-119.

[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.