Beta Amyloid
Signaling Pathway Map
Research Area
Inhibitory Selectivity
Beta Amyloid Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S2215 |
DAPT (GSI-IX)DAPT (GSI-IX, LY-374973) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells. DAPT enhances the apoptosis of human tongue carcinoma cells and regulates autophagy. |
Western blotting showing increased unconjugated SUMO1 levels in Notch1 ΔE cells treated with 10 uM DAPT for 3 days. Tubulin was used as a loading control.
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| S1575 |
RO4929097RO4929097 is a γ secretase inhibitor with IC50 of 4 nM in a cell-free assay, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. Phase 2. |
|
|
| S1594 |
Semagacestat (LY450139)Semagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, also inhibits Notch signaling with IC50 of 14.1 nM in H4 human glioma cell. Phase 3. |
HEK/APPswe cells were either left non-treated (-) or exposed to the γ-secretase inhibitor (GSI) semagacestat (+) for 19 h prior to cell harvesting and membrane preparation (Substrate accumulation). Exposure of cells with GSI prior to membrane preparation results in higher Aβ1-42 and Aβx-42 signals as compared to membranes derived from non-GSI treated cells. Direct addition of semagacestat to the membranes in the novo Aβ production assay inhibited Aβ production (Semagacestat (1 µM)). The amount of Aβx-42 is higher than Aβ1-42 suggesting that C83 is the major substrate for the Aβ42 signal detected. |
|
| S2660 |
MK-0752MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2. |
HES1 expression after treatment with clinically available GSIs R04929097, BMS-708163, LY450139, and MK-0752 as determined by qRT-PCR.
|
|
| S1262 |
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. |
A panel of GICs lines was treated with various concentrations of γ secretase inhibitors BMS-708163. Cells were treated with increasing concentrations of γ secretase inhibitors in triplicate wells for 72 hours, and cell viability was assessed by CellTiter-Blue assay as described in Materials and Methods. The results shown are of a single experiment with three independent replicates cell viability was measured by CellTiter-Blue assay. The graph depicts cell viability at 72 hours. Cell viability in the vehicle control was considered as to be 100%. |
|
| S0486New |
Hoechst 34580Hoechst 34580 (HOE 34580) is a cell-permeable blue fluorescent dye to stain DNA and nuclei. Hoechst 34580 is also a good candidate for treating the Alzheimer's disease by inhibiting amyloid beta (Aβ) formation with IC50 of 0.86 μM. |
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| S2418New |
FrentizoleFrentizole is a novel inhibitor of amyloid beta peptide (Abeta) binding alcohol dehydrogenase (ABAD) interaction with IC50 of 200 μM. Frentizole is a nontoxic antiviral and immunosuppressive agent used clinically in rheumatoid arthritis and systemic lupus erythematosus. |
||
| S1528 |
LY2811376LY2811376 is the first orally available non-peptidic β-secretase(BACE1) inhibitor with IC50 of 239 nM-249 nM, that act to decrease Aβ secretion with EC50 of 300 nM, demonstrated to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin. Phase 1. |
|
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| S4261 |
EUK 134EUK 134, a synthetic superoxide dismutase (SOD)/catalase mimetic, exhibits potent antioxidant activities, and inhibits the formation of β-amyloid and related amyloid fibril. |
||
| S4760 |
(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD)(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD, HP-β-cyclodextrin), a well-known sugar used in drug delivery, genetic vector, environmental protection and treatment of Niemann-Pick disease type C1 (NPC1), is an inhibitor of amyloid-β aggregation. |
||
| S8185 |
FPS-ZM1FPS-ZM1 is a blood-brain-barrier permeant, non-toxic, tertiary amide compound which is a high affinity RAGE-specific inhibitor, blocking Aβ binding to the V domain of RAGE. |
FPS-ZM1 suppresses S100B promoted migration and invasion abilities. *P < 0.05, **P < 0.01 vs “CM” groups; &P < 0.05, &&P < 0.01 vs “S100B+FPS” groups. |
|
| S5101 |
Tabersonine hydrochlorideTabersonine, an ingredient extracted from the bean of Voacanga africana, is a potent inhibitor against Aβ(1−42) aggregation and toxicity. |
||
| S9087 |
TenuifolinTenuifolin, a secondary saponin isolated from hydrolysates of polygalasaponins, inhibits beta-amyloid synthesis in vitro and has nootropic activity in vivo via acetylcholine esterase inhibition and increases norepinephrine and dopamine production. |
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| S6733 |
Edonerpic maleateEdonerpic maleate is a novel neurotrophic agent which can inhibit amyloid-β peptides (Aβ). |
||
| S3811 |
Ginsenoside ReGinsenoside Re (Ginsenoside B2), an extract from Panax notoginseng, is a major ginsenoside in ginseng and belongs to 20(S)-protopanaxatriol group. It has diverse in vitro and in vivo effects, including vasorelaxant, antioxidant, antihyperlipidemic, and angiogenic actions. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB. |
||
| S5742 |
Deferoxamine mesylateDeferoxamine mesylate is the mesylate salt of Deferoxamine, which forms iron complexes and is used as a chelating agent. Deferoxamine is a ferroptosis inhibitor that stabilizes HIF-1α expression and improves HIF-1α transactivity in hypoxic and hyperglycemic states in vitro. Deferoxamine decreases beta-amyloid (Aβ) deposition and induces autophagy. |
||
| S3923 |
Ginsenoside Rg1Ginsenoside Rg1, one of the major active components of ginseng, is identified as a protopanaxatriol-type and has pharmacological actions such as neuroprotective and anti-tumor effects on various cancer types. Ginsenoside Rg1 reduces cerebral Aβ levels and NF-κB nuclear translocation. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S2215 |
DAPT (GSI-IX)DAPT (GSI-IX, LY-374973) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells. DAPT enhances the apoptosis of human tongue carcinoma cells and regulates autophagy. |
Western blotting showing increased unconjugated SUMO1 levels in Notch1 ΔE cells treated with 10 uM DAPT for 3 days. Tubulin was used as a loading control.
|
|
| S1575 |
RO4929097RO4929097 is a γ secretase inhibitor with IC50 of 4 nM in a cell-free assay, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. Phase 2. |
|
|
| S1594 |
Semagacestat (LY450139)Semagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, also inhibits Notch signaling with IC50 of 14.1 nM in H4 human glioma cell. Phase 3. |
HEK/APPswe cells were either left non-treated (-) or exposed to the γ-secretase inhibitor (GSI) semagacestat (+) for 19 h prior to cell harvesting and membrane preparation (Substrate accumulation). Exposure of cells with GSI prior to membrane preparation results in higher Aβ1-42 and Aβx-42 signals as compared to membranes derived from non-GSI treated cells. Direct addition of semagacestat to the membranes in the novo Aβ production assay inhibited Aβ production (Semagacestat (1 µM)). The amount of Aβx-42 is higher than Aβ1-42 suggesting that C83 is the major substrate for the Aβ42 signal detected. |
|
| S2660 |
MK-0752MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2. |
HES1 expression after treatment with clinically available GSIs R04929097, BMS-708163, LY450139, and MK-0752 as determined by qRT-PCR.
|
|
| S1262 |
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. |
A panel of GICs lines was treated with various concentrations of γ secretase inhibitors BMS-708163. Cells were treated with increasing concentrations of γ secretase inhibitors in triplicate wells for 72 hours, and cell viability was assessed by CellTiter-Blue assay as described in Materials and Methods. The results shown are of a single experiment with three independent replicates cell viability was measured by CellTiter-Blue assay. The graph depicts cell viability at 72 hours. Cell viability in the vehicle control was considered as to be 100%. |
|
| S0486New |
Hoechst 34580Hoechst 34580 (HOE 34580) is a cell-permeable blue fluorescent dye to stain DNA and nuclei. Hoechst 34580 is also a good candidate for treating the Alzheimer's disease by inhibiting amyloid beta (Aβ) formation with IC50 of 0.86 μM. |
||
| S2418New |
FrentizoleFrentizole is a novel inhibitor of amyloid beta peptide (Abeta) binding alcohol dehydrogenase (ABAD) interaction with IC50 of 200 μM. Frentizole is a nontoxic antiviral and immunosuppressive agent used clinically in rheumatoid arthritis and systemic lupus erythematosus. |
||
| S1528 |
LY2811376LY2811376 is the first orally available non-peptidic β-secretase(BACE1) inhibitor with IC50 of 239 nM-249 nM, that act to decrease Aβ secretion with EC50 of 300 nM, demonstrated to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin. Phase 1. |
|
|
| S4261 |
EUK 134EUK 134, a synthetic superoxide dismutase (SOD)/catalase mimetic, exhibits potent antioxidant activities, and inhibits the formation of β-amyloid and related amyloid fibril. |
||
| S4760 |
(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD)(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD, HP-β-cyclodextrin), a well-known sugar used in drug delivery, genetic vector, environmental protection and treatment of Niemann-Pick disease type C1 (NPC1), is an inhibitor of amyloid-β aggregation. |
||
| S8185 |
FPS-ZM1FPS-ZM1 is a blood-brain-barrier permeant, non-toxic, tertiary amide compound which is a high affinity RAGE-specific inhibitor, blocking Aβ binding to the V domain of RAGE. |
FPS-ZM1 suppresses S100B promoted migration and invasion abilities. *P < 0.05, **P < 0.01 vs “CM” groups; &P < 0.05, &&P < 0.01 vs “S100B+FPS” groups. |
|
| S5101 |
Tabersonine hydrochlorideTabersonine, an ingredient extracted from the bean of Voacanga africana, is a potent inhibitor against Aβ(1−42) aggregation and toxicity. |
||
| S9087 |
TenuifolinTenuifolin, a secondary saponin isolated from hydrolysates of polygalasaponins, inhibits beta-amyloid synthesis in vitro and has nootropic activity in vivo via acetylcholine esterase inhibition and increases norepinephrine and dopamine production. |
||
| S6733 |
Edonerpic maleateEdonerpic maleate is a novel neurotrophic agent which can inhibit amyloid-β peptides (Aβ). |
||
| S3811 |
Ginsenoside ReGinsenoside Re (Ginsenoside B2), an extract from Panax notoginseng, is a major ginsenoside in ginseng and belongs to 20(S)-protopanaxatriol group. It has diverse in vitro and in vivo effects, including vasorelaxant, antioxidant, antihyperlipidemic, and angiogenic actions. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB. |
||
| S5742 |
Deferoxamine mesylateDeferoxamine mesylate is the mesylate salt of Deferoxamine, which forms iron complexes and is used as a chelating agent. Deferoxamine is a ferroptosis inhibitor that stabilizes HIF-1α expression and improves HIF-1α transactivity in hypoxic and hyperglycemic states in vitro. Deferoxamine decreases beta-amyloid (Aβ) deposition and induces autophagy. |
||
| S3923 |
Ginsenoside Rg1Ginsenoside Rg1, one of the major active components of ginseng, is identified as a protopanaxatriol-type and has pharmacological actions such as neuroprotective and anti-tumor effects on various cancer types. Ginsenoside Rg1 reduces cerebral Aβ levels and NF-κB nuclear translocation. |
