- Cat. No.
- A11176
LY-411575
LY-411575 is a selective, cell permeable, small molecule gamma secretase inhibitor.
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γ-Secretase inhibitors and modulators act on the intramembrane protease that cleaves amyloid precursor protein (APP). The enzyme is a multiprotein complex with presenilin as its catalytic subunit, and Notch receptors are among its substrates. In 1998, loss of presenilin-1 in neurons was shown to block the γ-secretase cleavage of APP that releases amyloid-β (Aβ). A year later, a presenilin-1-dependent protease was found to release the Notch intracellular domain. DAPT, LY-411575 and semagacestat inhibit both APP and Notch processing and are used in Aβ and Notch signaling studies. Avagacestat and RO4929097 are further inhibitors, and DAPT is also common in organoid and stem cell work. E 2012 is a γ-secretase modulator that shifts Aβ production.
LY-411575 is a selective, cell permeable, small molecule gamma secretase inhibitor.
Synonyms: GSIIX
DAPT (GSI-IX) is an inhibitor of γ-secretase that causes a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures with IC50 values of 115 and 200 nM for total Aβ and Aβ42 respectively.
RO4929097 is an orally bioavailable, small-molecule gamma secretase (GS) inhibitor with an IC50 of 4 nM.
Synonyms: LY-450139
Semagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, respectively. Semagacestat also inhibits Notch signaling with IC50 of 14.1 nM.
Synonyms: Dibenzazepine; Deshydroxy LY 411575
YO-01027 is a dipeptidic γ-secretase inhibitor, an antiAlzheimer agent.
E 2012 is γ-secretase inhibitor.
BMS 299897 is an orally active, potent γ-secretase inhibitor (IC50 = 12 nM). Inhibits Aβ40 and Aβ42 formation in vitro (IC50 values are 7.4 and 7.9 nM respectively) and reduces Aβ in the brain, plasma and cerebrospinal fluid in vivo.
FLI-06 is a Notch inhibitor and the early secretory pathway inhibitor. FLI-06 disrupts the Golgi apparatus in a manner distinct from that of brefeldin A and golgicide A.
Synonyms: BMS-708163
BMS-708163 is an oral gamma secretase inhibitor designed for selective inhibition of amyloid beta synthesis.
MK-0752 inhibits the Notch signaling pathway, which may result in induction of growth arrest and apoptosis in tumor cells in which the Notch signaling pathway is overactivated.
Synonyms: GSI953
Begacestat is a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.
Synonyms: PF 03084014
PF-03084014 is a reversible and selective inhibitor of γ-secretase with IC50 value of 6.2 nM .
BMS 433796 is a γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease.
gamma-secretase modulator 1 is a gamma-secretase modulator, gamma-secretase modulator 1 is useful for Alzheimer's disease.
gamma-secretase modulator 2 is a potent and selective gamma-secretase modulator for treatment of Alzheimer's disease.
Synonyms: (R)-Flurbiprofen; MPC 7869; Tarenflurbil
Flurizan is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits γ-secretase activity.
TC-E 5006 is a gamma-secretase modulator. Reduces Aβ42 levels in vitro (EC50 = 390 nM) and in vivo.
Flurbiprofen Axetil is potentnon-steroidal anti-inflammatory drug(NSAID).
SPL-707 is a potent, selective and orally available signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 80 nM.
gamma-secretase modulator 3 is a gamma-secretase modulator.
Synonyms: CW3,5-Bis(4-nitrophenoxy)benzoic acid
Compound W is a γ-secretase inhibitor that has been shown to lower the levels of secreted Aβ42 and Nβ25.
JLK 6 is an inhibitor of γ-secretase that selectively inhibits APP cleavage without affecting other γ-secretase-mediated pathways.
MRK 560 is an orally bioavailable gamma-secretase inhibitor with the ability to markedly reduce Abeta peptide in the brain and CSF of the rat and confirm the utility of the rat for assessing the effects of gamma-secretase inhibitors on central nervous system Abeta(40) levels in vivo.
Synonyms: L685,458
L-685458 is a specific and potent inhibitor of A beta PP gamma-secretase activity with Ki of 17 nM.
Synonyms: MK-8931
Verubecesta is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor.