γ secretase

gamma-secretase modulator 1 is a modulator of γ secretase and can be used in studies about the treatment of Alzheimer's disease.

BMS-906024 (Osugacestat) is an orally available and selective inhibitor of γ-secretase, a small molecule Notch inhibitor.BMS-906024 has broad-spectrum antitumour activity against a variety of human cancer xenografts.BMS-906024 prevents the activation of all four Notch receptors, and is active against Notch1, -2, -3 and -4 receptors. BMS-906024 prevents the activation of all four Notch receptors, with IC50s of 1.6, 0.7, 3.4 and 2.9 nM for Notch1, -2, -3 and -4 receptors, respectively.

RO7185876 is a selective gamma secretase modulator, which can be used in the study of Alzheimer's disease.

3,5-Bis(4-nitrophenoxy)benzoic acid (Compound W) is a γ-secretase inhibitor that reduces the levels of released Aβ42 and notch-1 Aβ-like peptide 25 (Nβ25).

E2012 is a γ-secretase modulator (GSM). E2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat.

NGP555 is a modulator of γ-secretase.

Itanapraced (CHF5074), a γ-secretase modulator, reduces Aβ42/40 secretion (IC50: 3.6/18.4 μM).

RO4929097 (RG-4733), a γ secretase inhibitor (IC50: 4 nM), inhibits cellular processing of Aβ40 and Notch (EC50: 14/5 nM).

L-685458 (L-685,458) is a specific and potent inhibitor of A beta PP gamma-secretase activity with Ki of 17 nM.

Nirogacestat (PF 03084014) is a specific γ-secretase inhibitor (IC50: 6.2 nM, in a cell-free assay).

5β-Cholanic acid (5beta-Cholanic acid) is a potent γ-secretase modulator used in Alzheimer's disease research.

LY900009 is a small molecule inhibitor of Notch signalling via selective inhibition of the γ-secretase protein.

Fosciclopirox (CPX-POM), the phosphoryloxymethyl ester of CPX (Ciclopirox Prodrug, CPX-POM), selectively delivers the active metabolite, CPX, to the entire urinary tract following parenteral administration.

Gamma-secretase inhibitor-1 is a gamma-secretase modulator valuable for Alzheimer's disease [1].

Gamma-secretase modulator 2 is a potent, selective compound for the treatment of Alzheimer's disease, specifically designed to modulate γ-secretase activity. This modulation selectively attenuates the production of Aβ(1-42), addressing diseases associated with Aβ deposition in the brain, particularly Alzheimer's disease.

γ-Secretase modulator 4 is a potent γ-secretase modulator that reduces Aβ42 levels with IC50s of 0.017 μM in mice and 0.014 μM in humans.

gamma-Secretase Modulators serves as a useful treatment for Alzheimer's disease by inhibiting the production of Amyloid-β. Specifically, it acts as a gamma-Secretase Modulators with an IC50 value.

γ-Secretase modulator 10 (GSM-10) is a novel compound that modulates γ-secretase activity.

γ-Secretase modulator 12 (Compound 1a) is a selective compound that effectively reduces amyloid-β42 (Aβ42) levels with an IC50 of 0.39 μM, specifically designed for Alzheimer's disease research. Notably, γ-Secretase modulator 12 exhibits a favorable brain/plasma ratio (Kp, brain = 0.72) in mice [1].

γ-Secretase modulator 11 hydrochloride is a potent, orally active γ-secretase modulator (IC50: 0.029 μM). γ-Secretase modulator 11 hydrochloride significantly reduces brain Aβ42 levels and rescues the cognitive deficits exhibited by AD model mice. γ-Secretase modulator 11 hydrochloride has shown research potential in Alzheimer's disease.

Gamma-secretase modulator 5 (compound 22d) is a gamma-secretase modulator (GSM) that crosses the blood-brain barrier and inhibits the production of the aggregated amyloid β peptide Aβ42 (IC50: 60 nM). This compound is valuable for studying Alzheimer's disease.

γ-Secretase Modulator 14, a γ-secretase modulator, shows potential for use in Alzheimer's disease (AD) research (WO2013010904A1; compound 42) [1].

β-Secretase Inhibitor IV is a potent, cell-active inhibitor of BACE-1, with IC50 values of 15.6 nM and 16.3 nM at BACE-1 concentrations of 2 nM and 100 pM, respectively.

Gamma-secretase modulator 6 (Example 50) is a gamma-secretase modulator. It inhibits Aβ42 secretion in HEK cell lines stably expressing APP (Aβ amyloid precursor protein) with a pIC50 of 8.1. This compound is applicable in Alzheimer's disease research.