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Gamma-secretase

Gamma secretase is a multi-subunit protease complex, itself an integral membrane protein, that cleaves single-pass transmembrane proteins at residues within the transmembrane domain. Proteases of this type are known as intramembrane proteases. The most well-known substrate of gamma secretase is amyloid precursor protein, a large integral membrane protein that, when cleaved by both gamma and beta secretase, produces a short 37-43[verification needed] amino acid peptide called amyloid beta whose abnormally folded fibrillar form is the primary component of amyloid plaques found in the brains of Alzheimer's disease patients. Gamma secretase is also critical in the related processing of several other type I integral membrane proteins, such as Notch, ErbB4, E-cadherin, N-cadherin, ephrin-B2, or CD44.
Cat No. product name
T21890 JLK6 JLK6 was a gamma-secretase inhibitor that does not interfere with Notch signalling
T6063 LY-411575 LY411575, 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...
T6935 Nirogacestat PF-03084014 (PF-3084014) is a specific γ-secretase inhibitor (IC50: 6.2 nM, in a cell-free assay).
T6125 Semagacestat Semagacestat (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).
T6870 L-685458 L-685, 458 is a specific and potent inhibitor of A beta PP gamma-secretase activity with Ki of 17 nM.
T4652 (+)-Taxifolin Flavonoid, antioxidant. Inhibits lipogenesis in cancer cells, most likely by targeting fatty acid synthase activity.
T7064 Valproic Acid Valproic Acid is a branched chain fatty acid which potentially enhances central GABAergic neurotransmission and inhibits Na+ channels. Currently, the various mol...
T4S1990 Carvacrol 1. 5-Isopropyl-2-methylphenol presents anxiolytic effects. 2. 5-Isopropyl-2-methylphenol presents antinociceptive activity. 3. 5-Isopropyl-2-methylphenol present...
T1602 Valproic acid sodium salt Valproate Sodium is the sodium salt form of valproic acid with anti-epileptic activity. Valproate sodium is converted into its active form, valproate ion, in blo...
T4364 Aftin-4 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 incre...
T9422 Fosciclopirox Fosciclopirox, the phosphoryloxymethyl ester of CPX (Ciclopirox Prodrug, CPX-POM), selectively delivers the active metabolite, CPX, to the entire urinary tract f...
T2842 Tangeretin Tangeretin, a flavonoid from citrus fruit peels, has been proven to play an important role in anti-inflammatory responses and neuroprotective effects in several ...
T3540 IMR-1A IMR-1A is the metabolite of IMR-1 which is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μMol/L.
T3399 Psoralidin Psoralidin inhibits Akt phosphorylation and phosphatidylinositol 3-kinase activation and transcriptionally. Psoralidin possesses anticancer and chemopreventive p...
T6202 DAPT DAPT is a novel γ-secretase inhibitor which reduces the Aβ production (IC50: 20 nM in HEK 293 cells) and Aβ42 levels (IC50: 200 nM).
TWS2045 Bruceine D 1. Bruceine D from Brucea javanica, may have the potential to be used as a natural viricide, or a lead compound for new viricides. 2. Bruceine D inhibits the gro...
T13410 ZLDI-8 ZLDI-8 is an inhibitor of Notch activating/cleaving enzyme ADAM-17 and inhibits the cleavage of Notch protein.
T22678 3,5-Bis(4-nitrophenoxy)benzoic acid The compound 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).
T2262 Itanapraced CHF5074, a γ-secretase modulator, reduces Aβ42/40 secretion (IC50: 3.6/18.4 μM).
T2625 MK-0752 MK-0752, a γ-secretase inhibitor, reduces Aβ40 production(IC50=5 nM).
T9015 LY900009 LY900009 is a small molecule inhibitor of Notch signalling via selective inhibition of the γ-secretase protein.
T12246 CB-103 CB-103 is a orally active inhibitor of notch signaling pathway, with anti-tumor activity.
TQ0026 MDR-1339 MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable inhibitor of amyloid-β (Aβ) aggregation.
TP1540 Jagged-1 (188-204) This peptide is a fragment of the JAG-1 protein. JAG-1 is Notch ligand, a peptide that is the most conspicuously expressed ligand in skin. JAG-1 induces epiderma...
TP1293 Jagged-1 (188-204) TFA(219127-21-6 free base) Jagged-1 (188-204) TFA is a fragment of the JAG-1 protein. JAG-1 is Notch ligand, a peptide that is the most conspicuously expressed ligand in skin. JAG-1 induce...
T6861 IMR-1 IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μMol/L.
T6249 Avagacestat Avagacestat (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-...
T6274 RO4929097 RO4929097, a γ secretase inhibitor (IC50: 4 nM), inhibits cellular processing of Aβ40 and Notch (EC50: 14/5 nM).
T6135 YO-01027 YO-01027 is a potent γ-secretase inhibitor.
T4077 PE859 PE859 is a potent inhibitor of both tau and Aβ aggregation.
T3075 FLI-06 FLI-06 is a Notch signaling inhibitor (EC50: 2.3 μM).
T3633 Crenigacestat LY3039478 is an orally bioavailable Notch inhibitor with an IC50 of ~1 nM in most of the tumor cell lines tested. LY3039478 effectively inhibits mutant Notch rec...
T16294 NGP555 NGP555 is a modulator of γ-secretase.
T15184 E 2012 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 ...
T14683 BMS-983970 BMS-983970 is an oral inhibitor of pan-Notch, and for the treatment of multiplecancers.
JLK6
T21890
JLK6 was a gamma-secretase inhibitor that does not interfere with Notch signalling
LY-411575
T6063
LY411575, 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 0.3...
Nirogacestat
T6935
PF-03084014 (PF-3084014) is a specific γ-secretase inhibitor (IC50: 6.2 nM, in a cell-free assay).
Semagacestat
T6125
Semagacestat (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).
L-685458
T6870
L-685, 458 is a specific and potent inhibitor of A beta PP gamma-secretase activity with Ki of 17 nM.
(+)-Taxifolin
T4652
Flavonoid, antioxidant. Inhibits lipogenesis in cancer cells, most likely by targeting fatty acid synthase activity.
Valproic Acid
T7064
Valproic Acid is a branched chain fatty acid which potentially enhances central GABAergic neurotransmission and inhibits Na+ channels. Currently, the various mol...
Carvacrol
T4S1990
1. 5-Isopropyl-2-methylphenol presents anxiolytic effects. 2. 5-Isopropyl-2-methylphenol presents antinociceptive activity. 3. 5-Isopropyl-2-methylphenol present...
Valproic acid sodium salt
T1602
Valproate Sodium is the sodium salt form of valproic acid with anti-epileptic activity. Valproate sodium is converted into its active form, valproate ion, in blo...
Aftin-4
T4364
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 i...
Fosciclopirox
T9422
Fosciclopirox, the phosphoryloxymethyl ester of CPX (Ciclopirox Prodrug, CPX-POM), selectively delivers the active metabolite, CPX, to the entire urinary tract f...
Tangeretin
T2842
Tangeretin, a flavonoid from citrus fruit peels, has been proven to play an important role in anti-inflammatory responses and neuroprotective effects in several ...
IMR-1A
T3540
IMR-1A is the metabolite of IMR-1 which is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μMol/L.
Psoralidin
T3399
Psoralidin inhibits Akt phosphorylation and phosphatidylinositol 3-kinase activation and transcriptionally. Psoralidin possesses anticancer and chemopreventive p...
DAPT
T6202
DAPT is a novel γ-secretase inhibitor which reduces the Aβ production (IC50: 20 nM in HEK 293 cells) and Aβ42 levels (IC50: 200 nM).
Bruceine D
TWS2045
1. Bruceine D from Brucea javanica, may have the potential to be used as a natural viricide, or a lead compound for new viricides. 2. Bruceine D inhibits the gro...
ZLDI-8
T13410
ZLDI-8 is an inhibitor of Notch activating/cleaving enzyme ADAM-17 and inhibits the cleavage of Notch protein.
3,5-Bis(4-nitrophenoxy)benzoic acid
T22678
The compound 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).
Itanapraced
T2262
CHF5074, a γ-secretase modulator, reduces Aβ42/40 secretion (IC50: 3.6/18.4 μM).
MK-0752
T2625
MK-0752, a γ-secretase inhibitor, reduces Aβ40 production(IC50=5 nM).
LY900009
T9015
LY900009 is a small molecule inhibitor of Notch signalling via selective inhibition of the γ-secretase protein.
CB-103
T12246
CB-103 is a orally active inhibitor of notch signaling pathway, with anti-tumor activity.
MDR-1339
TQ0026
MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable inhibitor of amyloid-β (Aβ) aggregation.
Jagged-1 (188-204)
TP1540
This peptide is a fragment of the JAG-1 protein. JAG-1 is Notch ligand, a peptide that is the most conspicuously expressed ligand in skin. JAG-1 induces epiderma...
Jagged-1 (188-204) TFA(219127-21-6 free base)
TP1293
Jagged-1 (188-204) TFA is a fragment of the JAG-1 protein. JAG-1 is Notch ligand, a peptide that is the most conspicuously expressed ligand in skin. JAG-1 induce...
IMR-1
T6861
IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μMol/L.
Avagacestat
T6249
Avagacestat (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 1...
RO4929097
T6274
RO4929097, a γ secretase inhibitor (IC50: 4 nM), inhibits cellular processing of Aβ40 and Notch (EC50: 14/5 nM).
YO-01027
T6135
YO-01027 is a potent γ-secretase inhibitor.
PE859
T4077
PE859 is a potent inhibitor of both tau and Aβ aggregation.
FLI-06
T3075
FLI-06 is a Notch signaling inhibitor (EC50: 2.3 μM).
Crenigacestat
T3633
LY3039478 is an orally bioavailable Notch inhibitor with an IC50 of ~1 nM in most of the tumor cell lines tested. LY3039478 effectively inhibits mutant Notch rec...
NGP555
T16294
NGP555 is a modulator of γ-secretase.
E 2012
T15184
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 ...
BMS-983970
T14683
BMS-983970 is an oral inhibitor of pan-Notch, and for the treatment of multiplecancers.