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Gamma-secretase
T2262 GHF-5074 CHF5074, a γ-secretase modulator, reduces Aβ42/40 secretion (IC50: 3.6/18.4 μM).
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.
T3633 LY3039478 LY3039478 is an orally bioavailable Notch inhibitor with an IC50 of ~1nM in most of the tumor cell lines tested. LY3039478 effectively inhibits mutant Notch receptor activity. In a xenograft tumor model, LY3039478 inhibited expression of Notch-regulated genes and N1ICD cleavage in the tumor microenv
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 0.39 nM.
T6125 Semagacestat (LY450139) 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 YO-01027 (Dibenzazepine) YO-01027 is a potent γ-secretase inhibitor.
T6202 DAPT (GSI-IX) DAPT (GSI-IX) is a novel γ-secretase inhibitor, which reduces the Aβ production with IC50 of 20 nM in HEK 293 cells.
T6249 Avagacestat (BMS-708163) 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-fold selectivity against Notch. Phase 2.
T6274 RO4929097 RO4929097, a γ secretase inhibitor (IC50: 4 nM), inhibits cellular processing of Aβ40 and Notch (EC50: 14/5 nM).
T6861 IMR-1 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 PF-03084014 (PF-3084014) PF-03084014 (PF-3084014) is a specific γ-secretase inhibitor (IC50: 6.2 nM, in a cell-free assay).
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 increased Aβ-1-42, but not Aβ-1-40 in mouse hipppocampus, accompanied by learning deficits and mitochondrial ultrastructural changes simil
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