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.
Inhibitors Catalog Download
产品编号 产品名称
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).
T6274 RO4929097HOT RO4929097, a γ secretase inhibitor (IC50: 4 nM), inhibits cellular processing of Aβ40 and Notch (EC50: 14/5 nM).
T9422 Fosciclopirox Fosciclopirox, the phosphoryloxymethyl ester of CPX (Ciclopirox Prodrug, CPX-POM), selectively delivers the active metabolite, CPX, to the entire urinary tract f...
T2625 MK-0752 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 selectivi...
T6935 Nirogacestat PF-03084014 (PF-3084014) is a specific γ-secretase inhibitor (IC50: 6.2 nM, in a cell-free assay).
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...
T6135 YO-01027 YO-01027 is a potent γ-secretase inhibitor.
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 0.3...
T6870 L-685458 L-685, 458 is a specific and potent inhibitor of A beta PP gamma-secretase activity with Ki of 17 nM.
T6861 IMR-1 IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μMol/L.
T3075 FLI-06 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.
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).
T2262 Itanapraced CHF5074, a γ-secretase modulator, reduces Aβ42/40 secretion (IC50: 3.6/18.4 μM).
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 ...
T9015 LY900009 LY900009 is a small molecule inhibitor of Notch signalling via selective inhibition of the γ-secretase protein.
T4077 PE859 PE859 is a potent inhibitor of both tau and Aβ aggregation.
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 i...
TQ0026 MDR-1339 MDR-1339 is a blood-brain-barrier-permeable inhibitor of amyloid-β (Aβ) aggregation.
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...
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...
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 aim...
T16133 MRK-560 MRK-560 is an effective and brain-penetrant inhibitor of γ-secretase.
T16294 NGP555 NGP555 is a modulator of γ-secretase.
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).
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 1...
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).
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).
Fosciclopirox
T9422CAS 1380539-06-9
Fosciclopirox, the phosphoryloxymethyl ester of CPX (Ciclopirox Prodrug, CPX-POM), selectively delivers the active metabolite, CPX, to the entire urinary tract f...
MK-0752
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 selectivi...
Nirogacestat
T6935CAS 1290543-63-3
PF-03084014 (PF-3084014) is a specific γ-secretase inhibitor (IC50: 6.2 nM, in a cell-free assay).
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 rec...
YO-01027
T6135CAS 209984-56-5
YO-01027 is a potent γ-secretase inhibitor.
LY-411575
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 0.3...
L-685458
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.
IMR-1
T6861CAS 310456-65-6
IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 μMol/L.
FLI-06
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.
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).
Itanapraced
T2262CAS 749269-83-8
CHF5074, a γ-secretase modulator, reduces Aβ42/40 secretion (IC50: 3.6/18.4 μM).
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 ...
LY900009
T9015CAS 209984-68-9
LY900009 is a small molecule inhibitor of Notch signalling via selective inhibition of the γ-secretase protein.
PE859
T4077CAS 1402727-29-0
PE859 is a potent inhibitor of both tau and Aβ aggregation.
Aftin-4
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 i...
MDR-1339
TQ0026CAS 1018946-38-7
MDR-1339 is a blood-brain-barrier-permeable inhibitor of amyloid-β (Aβ) aggregation.
Jagged-1 (188-204) TFA(219127-21-6 free base)
TP1293CAS 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...
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 epiderma...
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 aim...
MRK-560
T16133CAS 677772-84-8
MRK-560 is an effective and brain-penetrant inhibitor of γ-secretase.
NGP555
T16294CAS 1304630-27-0
NGP555 is a modulator of γ-secretase.
3,5-Bis(4-nitrophenoxy)benzoic acid
T22678CAS 173550-33-9
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).
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 1...
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