gamma secretase

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

gamma-secretase inhibitior-1 is a gamma-secretase modulator that is useful to 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.

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.

gamma-secretase modulator 5 (compound 22d) is a gamma-secretase modulator (GSMs) that crosses the blood-brain barrier and exhibits an inhibitory effect on the production of the aggregated amyloid β peptide Aβ42 (IC50: 60 nM). gamma-secretase modulator 5 can be used in the study of Alzheimer's disease. The gamma-secretase modulator 5 can be used to study Alzheimer's disease.

gamma-secretase modulator 3 is a gamma-secretase modulator.

YO-01027 (DBZ) is a potent γ-secretase inhibitor.

GSM-1 is a modulator of γ-Secretase.

DAPT (LY-374973) is a γ-secretase inhibitor that inhibits total Aβ and Aβ42 (IC50=115/200 nM) and is orally active. DAPT is also a Notch inhibitor. DAPT induces cell differentiation, autophagy and apoptosis.

Sulindac sulfide (cis-Sulindac sulfide) is a non-steroidal anti-inflammatory compound that has a high affinity for COX-1 and acts as an inhibitor in Ras activation of Raf-1. Sulindac sulfide is a non-competitive inhibitor of gamma-secretase with an IC50 value of 20.2 μM. It is an active metabolite of sulinic acid.

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

JLK6 was a gamma-secretase inhibitor that does not interfere with Notch signalling

LY-411575, a potent γ-secretase inhibitor, is with IC50 of 0.078 nM in the membrane and 0.082 nM in cell-based. It also suppresses Notch clevage with IC50 of 0.39 nM.

Crenigacestat (LY3039478) is an orally bioavailable Notch inhibitor with an IC50 of ~1 nM in most of the tumor cell lines tested. Crenigacestat effectively inhibits mutant Notch receptor activity. In a xenograft tumor model, Crenigacestat inhibited expression of Notch-regulated genes and N1ICD cleavage in the tumor microenvironment.

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

MK-0752, a γ-secretase inhibitor, reduces Aβ40 production(IC50=5 nM).

ELND006 is a novel gamma secretase inhibitor previously under investigation for the oral treatment of Alzheimer's disease. ELND006 shows poor solubility and has moderate to high permeability. The in vivo performance of the ELND006 nanosuspension was tested in fed and fasted beagle dogs and compared with a gelatin capsule containing reference API. The results show that nanosizing ELND006 profoundly improved the oral bioavailability and virtually eliminated variation resulting from food intake.

γ-Secretase modulator 4 is a potent γ-secretase modulator, reduces the Aβ42 level with IC50s of 0.017 μM and 0.014 μM in mouse and human, respectively.

Avagacestat (BMS-708163) (BMS-708163) is a potent, selective, orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch. Phase 2.

ELND007 is a Gamma secretase inhibitor.

Sodium MK-0752 is a novel and potent gamma-secretase inhibitor that has been evaluated in clinical trials for the treatment of various types of cancer.

NGP555 is a modulator of γ-secretase.

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

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

Semagacestat (LY450139) (LY450139) is a γ-secretase blocker for Aβ42/Aβ40/Aβ38 (IC50: 10.9/12.1/12.0 nM) and also inhibits Notch signaling (IC50: 14.1 nM).

EVP-0015962, which is bioavailable orally, is a potent and selective gamma-secretase regulator in vitro and in vivo, detectable in the brain.

GSI-136 is a gamma secretase inhibitor.

Z-Ile-Leu-aldehyde is an effective and competitive peptide aldehyde inhibitor of γ-secretase and notch.

Potent γ-secretase inhibitor (IC50 values are 1.2 and 6.2 nM in whole cell and cell-free assays, respectively). Reduces Aβ in brain, CSF and plasma in mice and guinea pigs. Lanz et al (2010) Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014. J.Pharmacol.Exp.Ther. 334 269 PMID:20363853

γ-Secretase modulator 10 is a novel γ-secretase modulator.

Amyloid 17-42 (Aβ(17-42)), a significant component of diffuse plaques in Alzheimer's disease and cerebellar pre-amyloid in Down's syndrome, results from the alpha- and gamma-secretase cleavage of amyloid precursor protein (APP). It has the capability to trigger neuronal apoptosis through the Fas-like/caspase-8 activation pathway [1].

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.

AZD4800 is a gamma secretase modulators.

Begacestat is a selective thiophene sulfonamide amyloid precursor protein gamma-secretase inhibitor (Aβ40,IC50=15 nM),and for the treatment of Alzheimer's disease.

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.

FRM-024 is a powerful gamma secretase modulator with the ability to penetrate the central nervous system (CNS), designed specifically for the treatment of familial Alzheimer's disease.

Z-LLNle-CHO is a cell permeable inhibitor of gamma-secretase. Z-LLNle-CHO induces apoptosis of human glioblastoma tumor-initiating cells by proteasome inhibition and mitotic arrest response.

MRK-560 is an effective and brain-penetrant inhibitor of γ-secretase.

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

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