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) 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. |
|
|
| 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%. |
|
| 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. |
|
|
| 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. |
||
| S6733New |
Edonerpic maleateEdonerpic maleate is a novel neurotrophic agent which can inhibit amyloid-β peptides (Aβ). |
||
| 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)HP-β-cyclodextrin (HP-β-CD), 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. |
||
| 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. |
||
| 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. |
||
| 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) 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. |
|
|
| 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%. |
|
| 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. |
|
|
| 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. |
||
| S6733New |
Edonerpic maleateEdonerpic maleate is a novel neurotrophic agent which can inhibit amyloid-β peptides (Aβ). |
||
| 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)HP-β-cyclodextrin (HP-β-CD), 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. |
||
| 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. |
||
| 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. |
||
| 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. |
