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
T2262	CHF5074	CHF5074, a γ-secretase modulator, reduces Aβ42/40 secretion (IC50: 3.6/18.4 μM).
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.
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).
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 ...
TQ0026	MDR-1339	MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable inhibitor of amyloid-β (Aβ) aggregation.
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...
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...
T12246	CB-103	CB-103 is a orally active inhibitor of notch signaling pathway, with anti-tumor activity.
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...
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...

Cat No.

product name

T2262

CHF5074

CHF5074, a γ-secretase modulator, reduces Aβ42/40 secretion (IC50: 3.6/18.4 μM).

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.

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).

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 ...

TQ0026

MDR-1339

MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable inhibitor of amyloid-β (Aβ) aggregation.

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...

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...

T12246

CB-103

CB-103 is a orally active inhibitor of notch signaling pathway, with anti-tumor activity.

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...

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...