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Neuroscience Gamma-secretase

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
T12246 CB-103 CB-103 is a orally active inhibitor of notch signaling pathway, with anti-tumor activity.
T14683 BMS-983970 BMS-983970 is an oral inhibitor of pan-Notch, and for the treatment of multiplecancers.
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 ai...
T2262 CHF5074 CHF5074, a γ-secretase modulator, reduces Aβ42/40 secretion (IC50: 3.6/18.4 μM).
T2625 MK0752 MK-0752, a γ-secretase inhibitor, reduces Aβ40 production(IC50=5 nM).
T2639 LY2811376 LY2811376, an orally available non-peptidic β-secretase(BACE1) inhibitor (IC50: 239-249 nM), can decrease Aβ secretion (EC50: 300 nM). It has 10-fold selectiv...
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...
T3075 FLI06 FLI-06 is a Notch signaling inhibitor (EC50: 2.3 μM).
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.
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 re...
T4077 PE859 PE859 is a potent inhibitor of both tau and Aβ aggregation.
T4364 Aftin4 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 ...
T6063 LY411575 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....
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).
T6135 Dibenzazepine YO-01027 is a potent γ-secretase inhibitor.
T6202 DAPTHOT 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).
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 ...
T6274 RO4929097HOT RO4929097, a γ secretase inhibitor (IC50: 4 nM), inhibits cellular processing of Aβ40 and Notch (EC50: 14/5 nM).
T6861 IMR1 IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μMol/L.
T6870 L-685,458 L-685, 458 is a specific and potent inhibitor of A beta PP gamma-secretase activity with Ki of 17 nM.
T6935 PF03084014 PF-03084014 (PF-3084014) is a specific γ-secretase inhibitor (IC50: 6.2 nM, in a cell-free assay).
T9015 LY900009 LY900009 is a small molecule inhibitor of Notch signalling via selective inhibition of the γ-secretase protein.
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 epiderm...
TQ0026 MDR-1339 MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable inhibitor of amyloid-β (Aβ) aggregation.
CB-103
T12246CAS 218457-67-1
CB-103 is a orally active inhibitor of notch signaling pathway, with anti-tumor activity.
BMS-983970
T14683CAS 1584713-87-0
BMS-983970 is an oral inhibitor of pan-Notch, and for the treatment of multiplecancers.
E 2012
T15184CAS 870843-42-8
E2012 is a γ-secretase modulator (GSM). E2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 ai...
CHF5074
T2262CAS 749269-83-8
CHF5074, a γ-secretase modulator, reduces Aβ42/40 secretion (IC50: 3.6/18.4 μM).
MK0752
T2625CAS 471905-41-6
MK-0752, a γ-secretase inhibitor, reduces Aβ40 production(IC50=5 nM).
LY2811376
T2639CAS 1194044-20-6
LY2811376, an orally available non-peptidic β-secretase(BACE1) inhibitor (IC50: 239-249 nM), can decrease Aβ secretion (EC50: 300 nM). It has 10-fold selectiv...
Tangeretin
T2842CAS 481-53-8
Tangeretin, a flavonoid from citrus fruit peels, has been proven to play an important role in anti-inflammatory responses and neuroprotective effects in several...
FLI06
T3075CAS 313967-18-9
FLI-06 is a Notch signaling inhibitor (EC50: 2.3 μM).
IMR-1A
T3540CAS 331862-41-0
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.
Crenigacestat
T3633CAS 1421438-81-4
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 re...
PE859
T4077CAS 1402727-29-0
PE859 is a potent inhibitor of both tau and Aβ aggregation.
Aftin4
T4364CAS 866893-90-5
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 ...
LY411575
T6063CAS 209984-57-6
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....
Semagacestat
T6125CAS 425386-60-3
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).
Dibenzazepine
T6135CAS 209984-56-5
YO-01027 is a potent γ-secretase inhibitor.
DAPT HOT
T6202CAS 208255-80-5
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).
Avagacestat
T6249CAS 1146699-66-2
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 ...
RO4929097 HOT
T6274CAS 847925-91-1
RO4929097, a γ secretase inhibitor (IC50: 4 nM), inhibits cellular processing of Aβ40 and Notch (EC50: 14/5 nM).
IMR1
T6861CAS 310456-65-6
IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μMol/L.
L-685,458
T6870CAS 292632-98-5
L-685, 458 is a specific and potent inhibitor of A beta PP gamma-secretase activity with Ki of 17 nM.
PF03084014
T6935CAS 1290543-63-3
PF-03084014 (PF-3084014) is a specific γ-secretase inhibitor (IC50: 6.2 nM, in a cell-free assay).
LY900009
T9015CAS 209984-68-9
LY900009 is a small molecule inhibitor of Notch signalling via selective inhibition of the γ-secretase protein.
Jagged-1 188-204
TP1540CAS 219127-21-6
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 epiderm...
MDR-1339
TQ0026CAS 1018946-38-7
MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable inhibitor of amyloid-β (Aβ) aggregation.