Gamma secretase (γ-secretase), a member of the intramembrane cleaving protease (i-CLiP) family, is a promiscuous di-aspartyl protease that catalyzes the regulated intramembrane proteolysis (RIP), in which substrate proteins are cleaved within their membrane-spanning domain. A functional γ-secretase is a multi-protein complex consisting of the catalytic component, presenilin (PSEN), and three protein cofactors, including nicastrin (NCT), anterior-pharynx defective-1 (APH1) and PSEN enhancer-2 (PEN2). So far, 90 substrates of γ-secretase have been identified, which are type-I transmembrane proteins, except for glutamate receptor GluR3, polycystin-1 and glucosaminyltransferase (GnT-V), and appear to function as signaling proteins regulating a wide variety of cellular events, such as Notch signaling pathway.
- TC-E 5006Catalog No. :B7719γ-secretase modulatorNew Product
- BegacestatCatalog No. :A4406γ-secretase inhibitorγ-secretase inhibitor; selectively inhibits cleavage of amyloid precursor protein (APP) over Notch.
- FlurizanCatalog No. :A4402NSAID,inhibits γ-secretase activityNonsteroidal anti-inflammatory drug (NSAID) that inhibits γ-secretase activity.
- MRK 560Catalog No. :A4405γ-secretase inhibitorγ-secretase inhibitor; inhibits proteolytic cleavage of amyloid precursor protein (APP) over the Notch pathway. Reduces levels of Aβ in the brain (inhibits Aβ40 and Aβ42 in SH-SY5Y neuroblastoma cells with an IC50 of 0.65 nM); attenuates plaque deposition. Orally bioavailable.
- L-685,458Catalog No. :A4404γ-secretase inhibitor
L-685,458 is a selective and Potent inhibitor of γ-secretase with IC50 value of 17 nM.
- JLK 6Catalog No. :A4403γ-secretase inhibitorInhibitor of γ-secretase that selectively inhibits βAPP cleavage without affecting other γ-secretase-mediated pathways. Prevents recovery of Aβ40 and Aβ42 from HEK293 cell overexpressing wild-type or Swedish-mutated βAPP (IC50 ~ 30 μM) but displays no effect on Notch cleavage and Notch-mediated intracellular signaling. Displays no activity on BACE1, BACE2, α-secretase, the proteosome or GSK3β.
- Compound WCatalog No. :A4401γ-secretase inhibitorInhibitor of γ-secretase; causes a decrease in the released levels of Aβ42 and notch-1 Aβ-like peptide 25 (Nβ25).
- BMS 299897Catalog No. :A4400γ--secretase inhibitor, potent and orally activeBMS-299897 is a selective inhibitor of γ-secretase with IC50 value of 12 nM .
- PF-03084014Catalog No. :A3711γ-secretase inhibitorPF-03084014 is a reversible and selective inhibitor of γ-secretase with IC50 value of 6.2 nM .
- LY3039478Catalog No. :A4023Notch inhibitor, novel and potent
LY3039478 is a novel and potent Notch inhibitor with IC50 of 0.41 nM.