Inhibitor
| Cat.No. | Name | Information |
|---|---|---|
| M7934 | MDL 28170 | Mdl-28170 (Calpain Inhibitor III) is a potent, selective, membrane-permeable Inhibitor of cysteine protease (Calpain Inhibitor III) that can quickly cross the blood-brain barrier after systemic administration. Mdl-28170 also blocks gamma-secretase. |
| M2277 | Semagacestat | 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, respectively. |
| M1746 | DAPT | DAPT (GSI-IX) is a γ-secretase inhibitor with IC50 values of 115 and 200 nM for total Aβ and Aβ42 respectively. DAPT inhibits the activation of Notch 1 signaling. |
| M31249 | Fosciclopirox | Fosciclopirox suppresses growth of urothelial cancer by targeting the γ-secretase complex. Fosciclopirox selectively delivers the active metabolite, Ciclopirox (CPX), to the entire urinary tract. Ciclopirox has anticancer activity in a number of solid and hematologic malignancies. |
| M14583 | E 2012 | E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. |
| M9505 | Compound E | Compound E is a cell-permeable, potent, selective inhibitor of γ-secretase and Notch processing. |
| M9041 | PF-03084014 (Nirogacestat) | PF-03084014 (Nirogacestat) is a potent and selective γ-secretase inhibitor with IC50 of 6.2 nM. |
| M7885 | L-685,458 | L-685,458 is a potent, selective, structurally novel γ-secretase inhibitor; equipotent inhibitor of both Aβ1-42 and Aβ1-40 production. |
| M7518 | NGP 555 | NGP 555 is a small-molecule modulator of γ-secretase and has been successful in achieving good oral absorption, brain penetration, CNS activity, and specificity for a lipid-based membrane target preclinically. |
| M3619 | Begacestat | Begacestat selectively inhibits cleavage of amyloid precursor protein (APP) over Notch. Lowers levels of Aβ42 and Aβ40 (EC50 values are 12.4 and 14.8 nM respectively in cells expressing human recombinant APP). |
| M3523 | YO-01027 | YO-01027 (Dibenzazepine, DBZ) is a dipeptidic γ-secretase inhibitor with IC50 of 2.6 nM and 2.9 nM for APPL and Notch cleavage, respectively. |
| M2827 | LY3039478 | LY3039478 (Crenigacestat) is a novel and orally active Notch and γ-secretase inhibitor, with an IC50 of 1 nM in most of the tumor cell lines tested. |
| M2172 | LY2811376 | LY2811376 is an orally available, non-peptidic β-secretase inhibitor with IC50 of 239 nM-249 nM. |
| M2130 | LY-411575 | LY-411575 is potent and selective small molecule γ-secretase inhibitor with IC50 of 0.1 nM for APP23 and APP51/16 primary neurons. |
| M2120 | MK-0752 | MK-0752 is a potent, oral inhibitor of γ-secretase with IC50 of 5 nM in human SH-SY5Y cells. |
| M2015 | RO4929097 | RO4929097 is a potent and selective inhibitor of γ-secretase and as a result is able to inhibit Notch pathway signaling. |
| M1947 | BMS-708163 | BMS-708163 (Avagacestat) is a selective γ-secretase inhibitor (IC50 = 0.3 nM). |
| M56828 | Nirogacestat dihydrobromide | Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. |
| M52428 | RE(EDANS)EVNLDAEFK(DABCYL)R | RE (EDANS) EVNLDAEFK (DABCYL) R is an EDANS and DABCYL double-labeled peptide，serves as a fluorescent substrate for BACE1(Em=360nm，Ex=528nm). |
| M52427 | β-Secretase inhibitor | β-Secretase inhibitor ([Asn670, Sta671, Val672]-Amyloid β Peptide (662-675)) is a β-secretase and BACE1 inhibitor (IC50: 25 nM for β-secretase). |
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