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.

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...