γ secretase(aβ)

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.

BMS 433796 is a γ-secretase inhibitor that demonstrates Aβ-lowering activity in a transgenic mouse model of Alzheimer's disease.

Aβ-IN-1 is a novel, potent and orally active γ-secretase modulator (GSM). Aβ-IN-1 potently reduced Aβ42 levels with an IC 50 value of 0.091 μM in cultured cells without inhibiting CYP3A4. Aβ-IN-1 shows a sustained pharmacokinetic profile.

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).

Aftin-4, an amyloid forty-two inducer, activates γ-secretase, promoting the generation of amyloid-β-1-42 (Aβ1-42) from amyloid-β protein precursor. Aftin-4(Aftin4) increased Aβ-1-42, but not Aβ-1-40 in mouse hipppocampus, accompanied by learning deficits and mitochondrial ultrastructural changes similar to those found in the brains of patients with AD. Aftin-4(Aftin4) can thus be used to induce a rapid, acute Alzheimer's disease-like toxicity in the rodent brain.

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 modulator 3 (γ-secretase modulator 3) is a γ-secretase modulator that reduces Aβ production.

BMS 299897 is a sulfonamide γ-secretase inhibitor with an IC50 of 7 nM for inhibiting Aβ production in HEK293 cells stably overexpressing amyloid precursor protein (APP).

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

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

L458-BPyne is a γ-secretase modulator photoaffinity probe that acts by identifying distinct allosteric binding sites on presenilin. It also can be exploited to reduce levels of pathogenic Aβ species.

RO-57-Bpyne is a γ-secretase modulator photoaffinity probe. It also can be exploited to reduce levels of pathogenic Aβ species. It acts by identifying distinct allosteric binding sites on presenilin.

Leucyl-phenylalanine amide is an intermediate in the synthesis of γ-Secretase Inhibitor, the enzyme complex that catalyzes the cleavage of the amyloid precursor protein (APP) to produce amyloid β-peptide (Aβ) which is the major causative agent in Alzheime

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

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

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 alpha- and gamma-secretase cleavage of amyloid precursor protein (APP) and can trigger neuronal apoptosis via the Fas-like caspase-8 activation pathway [1].

Sulindac EP Impurity C-d3 is a deuterated compound of Sulindac EP Impurity C. Sulindac EP Impurity C has a CAS number of 32004-67-4. (E Z)-Sulindac sulfide is a potent γ-secretase modulator (GSM) that selectively reduces Aβ42 production in favor of shorter Aβ species. (E Z)-Sulindac sulfide can be used for researching Alzheimer's disease [1].