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Gamma-secretase/Beta-secretase Gamma-secretase/Beta-secretase

Inhibitor

Cat.No.  Name Information
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.
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.
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.
M52425 BACE1-IN-10 BACE1-IN-10 is a potent BACE1 Inhibitor.
M52424 OM99-2 TFA OM99-2 TFA, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin 2 with a Ki value of 9.58 nM.
M52423 SEVNLDAEFR SEVNLDAEFR is a substrate for BACE1.
M52422 OM99-2 OM99-2, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin 2 with a Ki value of 9.58 nM.
M52421 GL189 GL189 is a β-secretase inhibitor.
M49733 AChE/BACE1/GSK3β-IN-1 AChE/BACE1/GSK3β-IN-1 is an orally active triple inhibitor of AChE/BACE1/GSK3β.
M49494 BMS-932481 BMS-932481 is a small molecule gamma-secretase (γ-secretase) inhibitor that can be used in Alzheimer's disease related studies.
M42725 PSEN1-IN-2 PSEN1-IN-2 is a PSEN1 inhibitor.
M42724 PSEN1-IN-1 PSEN1-IN-1 is a PSEN1 inhibitor.
M42634 BACE1-IN-13 BACE1-IN-13 is an orally active BACE1 inhibitor with an IC50 value of 2.9 nM.
M42633 Verubecestat TFA Verubecestat (MK-8931) TFA is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM.
M42632 LY2886721 hydrochloride LY2886721 hydrochloride is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1.
M31065 BPN-15606 besylate  BPN-15606 besylate 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. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
M30807 GSM-1  GSM-1 is a potent γ-secretase modulator. GSM-1 directly targets the transmembrane domain (TMD) 1 of presenilin 1 (PS1).
M29348 Multitarget AD inhibitor-1  Multitarget AD inhibitor-1 is a selective and reversible butyrylcholinesterase (BuChE) inhibitor with IC50s of 7.22 μM and 1.55 μM for hBuChE and eqBuChE (BuChE from equine serum), respectively. Multitarget AD inhibitor-1 inhibits β-secretase (IC50hBACE-1=41.60 μM), amyloid β aggregation (IC50Aβ=3.09 μM), tau aggregation.
M29338 SPL-707  SPL-707 is an orally active, selective signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 77 nM for hSPPL2a. SPL-707 inhibits γ-secretase (IC50=6.1 μM) and SPP (IC50=3.7 μM). SPL-707 has the potential for autoimmune diseases research by targeting B cells and dendritic cells.
M29016 BPN-15606  BPN-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. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
M28977 AM-6494  AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursor protein cleaving enzyme 1) inhibitor (IC50=0.4 nM) with in vivo selectivity over BACE2 (IC50=18.6 nM).
M28634 PF-06648671  PF-06648671 is a novel, brain-penetrable, and orally active γ-secretase modulator (GSM). PF-06648671 reduces Aβ42 and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro. PF-06648671 is used for the study of Alzheimer’s disease.
M28304 Umibecestat Umibecestat (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. Umibecestat can be used for the research of alzheimer's disease.




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