Gamma Secretase
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.
Products for Gamma Secretase
- Cat.No. Product Name Information
- GC38011 γ-Secretase modulator 4
- GC67476 (E/Z)-Sulindac sulfide (E/Z)-Sulindac sulfide is a potent γ-secretase modulator (GSM). (E/Z)-Sulindac sulfide selectively reduces Aβ42 production in favor of shorter Aβ species. (E/Z)-Sulindac sulfide can be used for researching Alzheimer's disease.
- GC62859 Aβ42-IN-2 Aβ42-IN-2 is a γ-secretase modulator extracted from patent WO2016070107, compound example 36.
- GC12659 Begacestat An inhibitor of γ-secretase
- GC13099 BMS 299897 A γ-secretase inhibitor
- GC31012 BMS 433796 BMS 433796 is a γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease.
- GC13673 BMS-708163 (Avagacestat) A potent inhibitor of γ-secretase
- GC35535 BMS-906024 BMS-906024 is an orally active and selective γ-secretase (gamma secretase) inhibitor. BMS-906024 is a potent pan-Notch receptors inhibitor with IC50s of 1.6 nM, 0.7 nM, 3.4 nM, and 2.9 nM for Notch1, -2, -3, and -4 receptors, respectively. BMS-906024 demonstrates broad-spectrum antineoplastic activity.
- GC33118 Compound E Compound E is a γ-secretase inhibitor. Compound E bloks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50s of 0.24, 0.37, 0.32 nM, respectively.
- GC15645 Compound W A Notch1 signaling modulator
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GC12942
DAPT (GSI-IX)
Inhibitor of γ-secretase
- GC35921 E 2012 E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing.
- GC30427 ELN 318463 racemate ELN 318463 racemate is the racemate of ELN318463.
- GC10064 Flurizan A COX-inactive enantiomer of flurbiprofen
- GC63366 Fosciclopirox Fosciclopirox suppresses growth of urothelial cancer by targeting the γ-secretase complex.
- GC36107 gamma-secretase modulator 1 γ-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.
- GC38782 gamma-secretase modulator 1 hydrochloride gamma-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.
- GC36108 gamma-secretase modulator 2 gamma-secretase modulator 2 is a potent and selective γ-secretase modulator for treatment of Alzheimer's disease.
- GC36109 gamma-secretase modulator 3 gamma-secretase modulator 3 is a gamma-secretase modulator.
- GC62998 GSM-1 GSM-1 is a potent γ-secretase modulator.
- GC30954 Itanapraced (CHF5074) Itanapraced (CHF5074) (CHF5074) is a novel γ-secretase modulator, reduces Aβ42 and Aβ40 secretion, with an IC50 of 3.6 and 18.4 μM, respectively.
- GC13619 JLK 6 A protease inhibitor
- GC15364 L-685,458 A γ-secretase inhibitor
- GC12191 LY-411575 A γ-secretase inhibitor
- GC36512 LY-411575 isomer 1 LY-411575 isomer 1 is an isomer of LY411575, which is a potent γ-secretase inhibitor.
- GC36513 LY-411575 isomer 2
- GC36514 LY-411575 isomer 3
- GC17791 LY2811376 A BACE1 inhibitor
- GC12653 LY3039478 A Notch inhibitor
- GC15899 MK-0752 A potent inhibitor of γ-secretase
- GC16431 MRK 560 A potent inhibitor of γ-secretase
- GC30887 NGP555 A γ-secretase modulator
- GC50251 PF 3084014 hydrobromide PF 3084014 hydrobromide (PF-3084014 dihydrobromide) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by PF 3084014 hydrobromide while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers.
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GC10998
PF-03084014
γ-secretase inhibitor
- GC63407 PF-06648671 PF-06648671?is a novel, brain‐penetrable, and orally active γ‐secretase modulator (GSM).
- GC19290 PF-3084014 PF-3084014 (PF-3084014) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by PF-3084014 while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers.
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GC16197
RO4929097
An inhibitor of γ-secretase
- GC12096 Semagacestat (LY450139) A pan γ-secretase inhibitor
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GC15059
Sulindac sulfide
COX inhibitor
- GC16434 TC-E 5006 γ-secretase modulator
- GC17671 YO-01027 (Dibenzazepine, DBZ) An inhibitor of γ-secretase
- GC15896 Z-Ile-Leu-aldehyde potent gamma-Secretase inhibitor