γ-Secretase
Catalog No. | Inhibitor Name | γ secretase | Aβ | Notch | Other |
---|---|---|---|---|---|
A10288 | DAPT (GSI-IX) | * | |||
A10802 | RO4929097 | *** | *** | Aβ40 | |
A10836 | Semagacestat | ** | ** | ||
A10157 | Avagacestat | **** | |||
A11174 | Dibenzazepine | *** | *** | ||
A11176 | LY411575 | **** | **** | ||
A15899 | L-685458 | * | |||
A13815 | FLI-06 | * | |||
A13319 | PF-03084014 | ** | |||
A11194 | MK-0752 | *** | Aβ40 | ||
A13544 | LY3039478 | **** | |||
A16152 | IMR-1 | * | |||
A16223 | IMR-1A | * | |||
A11258 | Begacestat (GSI-953) | ** | |||
A12444 | BMS 299897 | ||||
A13217 | TC-E 5006 | * | |||
A15304 | MRK 560 | **** | |||
A15301 | JLK 6 | ||||
A16214 | CHF5074 | * | |||
A16215 | Z-Ile-Leu-aldehyde |
Notes:
1.Hover mouse over " " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
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Z-Ile-Leu-aldehyde
Catalog No. A16215 γ-Secretase inhibitorZ-Ile-Leu-aldehyde is a potent gamma-Secretase inhibitor; Notch signaling inhibitor. Learn More -
MRK 560
Catalog No. A15304 γ-secretase inhibitorMRK 560 is an orally bioavailable gamma-secretase inhibitor with the ability to markedly reduce Abeta peptide in the brain and CSF of the rat and confirm the utility of the rat for assessing the effects of gamma-secretase inhibitors on central nervous system Abeta(40) levels in vivo. Learn More -
PF-03084014
Catalog No. A11259 γ-secretase inhibitorPF-03084014 is a reversible and selective inhibitor of γ-secretase with IC50 value of 6.2 nM . Learn More -
L-685458
Catalog No. A15899 γ-secretase inhibitorL-685458 is a specific and potent inhibitor of A beta PP gamma-secretase activity with Ki of 17 nM. Learn More -
Begacestat (GSI-953)
Catalog No. A11258 γ-secretase inhibitorBegacestat is a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease. Learn More -
gamma-secretase modulator 1
Catalog No. A11425 Gamma-secretase modulatorgamma-secretase modulator 1 is a gamma-secretase modulator, gamma-secretase modulator 1 is useful for Alzheimer's disease. Learn More -
gamma-secretase modulator 2
Catalog No. A11427 Gamma-secretase modulatorgamma-secretase modulator 2 is a potent and selective gamma-secretase modulator for treatment of Alzheimer's disease. Learn More -
TC-E 5006
Catalog No. A13217 Gamma-secretase modulatorTC-E 5006 is a gamma-secretase modulator. Reduces Aβ42 levels in vitro (EC50 = 390 nM) and in vivo. Learn More -
Verubecestat (MK-8931)
Catalog No. A16113 β-secretase/BACE1 inhibitorVerubecesta is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. Learn More -
CHF5074
Catalog No. A16214 γ-Secretase modulatorCHF5074 is a novel γ-secretase modulator, reduces Aβ42 and Aβ40 secretion, with an IC50 of 3.6 and 18.4 uM, respectively. Learn More -
Flurbiprofen Axetil
Catalog No. A13662 gamma-secretase inhibitorFlurbiprofen Axetil is potentnon-steroidal anti-inflammatory drug(NSAID). Learn More -
BACE1-IN-4
Catalog No. A18462 BACE1 inhibitorBACE1-IN-4 is a potent and highly selective BACE1 inhibitor, with an IC50 of 3.8 nM and a Ki of 1.9 nM, more selective at BACE1 over BACE2. Anti-Alzheimer's disease. Learn More -
PF-06751979
Catalog No. A20066 BACE1 inhibitorPF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 7.3 nM in BACE1 binding assay. Learn More -
Umibecestat (CNP520)
Catalog No. A18987 BACE-1 inhibitorUmibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively. Learn More -
Lanabecestat
Catalog No. A12282 BACE1 inhibitorLanabecestat (AZD3293) is a potent, highly permeable, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM. Learn More -
BACE1-IN-1
Catalog No. A12183 BACE1 inhibitorBACE1-IN-1 is a potent and highly brain penetrant BACE1 inhibitor with IC50s of 32 and 47 nM for human BACE1 and BACE2, respectively. Learn More -
BMS-906024
Catalog No. A21172 gamma secretase inhibitorBMS-906024 is an oral and selective gamma secretase inhibitor (GSI) that is a small molecule Notch inhibitor. Learn More -
Compound E
Catalog No. A21292 -
β-Secretase Inhibitor IV
Catalog No. A21346 BACE-1 inhibitorβ-Secretase Inhibitor IV is a potent, cell-active BACE-1 inhibitor with IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively. Learn More -
AZD3839 free base
Catalog No. A21606 BACE1 inhibitorAZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor. Learn More -
Compound W
Catalog No. A15296 Gamma-secretase modulatorCompound W is a γ-secretase inhibitor that has been shown to lower the levels of secreted Aβ42 and Nβ25. Learn More -
LY2886721
Catalog No. A10543 BACE1 inhibitorLY2886721 is a novel potent agent that is used to treat Alzheimer's Disease in preclinical experiments. Learn More -
AZD3839
Catalog No. A12825 BACE1 inhibitorAZD3839 is a potent and selective inhibitor of human BACE1 with Ki of 26.1 nM. Learn More -
AMG-8718
Catalog No. A14407 BACE1 inhibitorAMG-8718 is a potent and orally efficacious BACE1 inhibitor. Learn More -
JLK 6
Catalog No. A15301 γ-secretase inhibitorJLK 6 is an inhibitor of γ-secretase that selectively inhibits APP cleavage without affecting other γ-secretase-mediated pathways. Learn More -
gamma-secretase modulator 3
Catalog No. A15090 gamma-secretase modulatorgamma-secretase modulator 3 is a gamma-secretase modulator. Learn More -
Timosaponin b-II
Catalog No. A14591 BACE1 InhibitorTimosaponin B-II is a major active component of Anemarrhena asphodeloides Bunge (Liliaceae, rhizome) that has protective effects against cerebral ischaemic damage. Learn More -
NGP-555
Catalog No. A17051 γ-Secretase ModulatorNGP-555 is a gamma-secretase modulator with a selective mechanism to reduce Abeta 42 while raising shorter Abeta forms such as Abeta 37 and 38. Learn More -
BMS-708163 (Avagacestat)
Catalog No. A10157 Gamma-secretase inhibitorBMS-708163 is an oral gamma secretase inhibitor designed for selective inhibition of amyloid beta synthesis. Learn More -
MK-0752
Catalog No. A11194 Gamma-secretase inhibitorMK-0752 inhibits the Notch signaling pathway, which may result in induction of growth arrest and apoptosis in tumor cells in which the Notch signaling pathway is overactivated. Learn More -
DAPT (GSI-IX)
Catalog No. A10288 Gamma secretase inhibitorDAPT (GSI-IX) is an inhibitor of γ-secretase that causes a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures with IC50 values of 115 and 200 nM for total Aβ and Aβ42 respectively. Learn More -
YO-01027
Catalog No. A11174 γ-secretase inhibitorYO-01027 is a dipeptidic γ-secretase inhibitor, an antiAlzheimer agent. Learn More -
LY-411575
Catalog No. A11176 Gamma secretase inhibitorLY-411575 is a selective, cell permeable, small molecule gamma secretase inhibitor.
Learn More -
Semagacestat (LY450139)
Catalog No. A10836 Gamma-secretase inhibitorSemagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, respectively. Semagacestat also inhibits Notch signaling with IC50 of 14.1 nM. Learn More -
LY2811376
Catalog No. A11776 BACE1 inhibitorLY2811376 is the first orally available non-peptidic BACE1 inhibitor that produces profound Aβ-lowering effects in animals. Learn More -
BMS 433796
Catalog No. A11337 γ-Secretase InhibitorBMS 433796 is a γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease. Learn More -
BPN-15606
Catalog No. A18681 γ-secretase modulatorBPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. Learn More -
IMR-1A
Catalog No. A16223 Notch inhibitorIMR-1A is the metabolite of IMR-1. IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 umol/L. Learn More -
E 2012
Catalog No. A11393 gamma-secretase modulatorE 2012 is γ-secretase inhibitor. Learn More -
BMS 299897
Catalog No. A12444 γ-secretase inhibitorBMS 299897 is an orally active, potent γ-secretase inhibitor (IC50 = 12 nM). Inhibits Aβ40 and Aβ42 formation in vitro (IC50 values are 7.4 and 7.9 nM respectively) and reduces Aβ in the brain, plasma and cerebrospinal fluid in vivo. Learn More -
IMR-1
Catalog No. A16152 Notch inhibitorIMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with IC50 of 6 umol/L. Learn More -
LY-900009
Catalog No. A14088 Notch inhibitorLY-900009 is a potent inhibitor of Notch with IC50 value of 0.27 nM. Learn More -
Flurizan
Catalog No. A12433 gamma-secretase modulatorFlurizan is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits γ-secretase activity. Learn More -
FLI-06
Catalog No. A13815 Gamma-secretase inhibitorFLI-06 is a Notch inhibitor and the early secretory pathway inhibitor. FLI-06 disrupts the Golgi apparatus in a manner distinct from that of brefeldin A and golgicide A. Learn More -
RO4929097
Catalog No. A10802 Gamma-secretase inhibitorRO4929097 is an orally bioavailable, small-molecule gamma secretase (GS) inhibitor with an IC50 of 4 nM. Learn More -
LY3039478
Catalog No. A13544 Notch inhibitorLY3039478 is a orally bioavailable, novel small molecule Notch inhibitor with an IC50 of ~1nM in most of the tumor cell lines tested. Learn More