Home Neuronal Signaling Secretase

Secretase Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S2215 DAPT DAPT 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.
Signal Transduct Target Ther, 2025, 10(1):334
Cell Host Microbe, 2025, 33(3):408-419.e8
Nat Commun, 2025, 16(1):8693
Verified customer review of DAPT
S1575 RO4929097 (RG-4733) RO4929097 (RG-4733) 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.
Nat Commun, 2025, 16(1):10435
Cell Rep Med, 2025, S2666-3791(25)00102-8
Cell Death Dis, 2025, 16(1):150
Verified customer review of RO4929097 (RG-4733)
S2714 LY411575 LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch cleavage with IC50 of 0.39 nM in APP or NΔE expressing HEK293 cells. LY411575 induces apoptosis.
Nat Commun, 2025, 16(1):5913
Dev Cell, 2025, S1534-5807(25)00468-X
Cell Rep, 2025, 44(4):115508
Verified customer review of LY411575
S2711 Dibenzazepine (YO-01027) DBZ (Dibenzazepine) is a dipeptidic γ-secretase inhibitor with IC50 of 2.6 nM and 2.9 nM in cell-free assays for APPL and Notch cleavage, respectively.
Acta Neuropathol Commun, 2025, 13(1):87
Sci Rep, 2025, 15(1):12154
Nat Commun, 2024, 15(1):9771
Verified customer review of Dibenzazepine (YO-01027)
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, respectively. It also inhibits Notch signaling with IC50 of 14.1 nM in H4 human glioma cell. This compound has reached Phase 3 clinical trials.
Cell Rep Med, 2025, S2666-3791(25)00102-8
Biochim Biophys Acta Mol Basis Dis, 2025, 1871(8):167992
Cancers (Basel), 2023, 15(6)1883
Verified customer review of Semagacestat (LY450139)
S2660 MK-0752 MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2.
Nat Cell Biol, 2024, 26(3):353-365
Cancers (Basel), 2023, 15(6)1883
J Cancer Res Clin Oncol, 2023, 149(16):14691-14699
Verified customer review of MK-0752
S1262 Avagacestat (BMS-708163) Avagacestat (BMS-708163) is a potent, selective, and orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 values of 0.3 nM and 0.27 nM, respectively. This compound demonstrates a 193-fold selectivity against Notch and has reached Phase 2 clinical trials.
Nat Commun, 2022, 13(1):6345
Sci Rep, 2022, 12(1):7
Cell, 2021, 184(2):521-533.e14
Verified customer review of Avagacestat (BMS-708163)
S8018 Nirogacestat (PF-03084014) Nirogacestat (PF-03084014, PF-3084014) is a selective gamma-secretase inhibitor with IC50 of 6.2 nM in a cell-free assay, and it induces apoptosis. Phase 2.
J Cell Biol, 2024, 223(10)e202305093
Biochem Pharmacol, 2024, 230(Pt 2):116577
Neurooncol Adv, 2024, 6(1):vdae188
Verified customer review of Nirogacestat (PF-03084014)
S7673 L-685,458 L-685,458 is a specific and potent inhibitor of A beta PP gamma-secretase activity with Ki of 17 nM.
iScience, 2022, 25(10):105182
Biochem Biophys Res Commun, 2021, 570:137-142
Aging (Albany NY), 2020, 12(1):481-501
Verified customer review of L-685,458
E0465 Fosciclopirox Fosciclopirox(CPX-POM) selectively delivers the active metabolite, Ciclopirox (CPX) that targets γ-secretase complex (Presenilin 1 and Nicastrin)2. It is used in the treatment of urothelial cancer and a number of solid and hematologic malignancies.
S0058 Compound E Compound E (γ-Secretase-IN-1) is a potent inhibitor of γ-secretase, which blocks γ-secretase-mediated cleavage of Notch with an IC50 of 0.32 nM. It also suppresses the production of β-amyloid(40) and β-amyloid(42) with IC50 values of 0.24 nM and 0.37 nM, respectively. It also inhibits Notch signalling, significantly disrupting gonadotropin-dependent follicle growth and halting progression to the preovulatory stage of development.
E6426New Sulindac sulfide Sulindac sulfide is a potent, reversible and noncompetitive inhibitor of γ42-secretase with an IC50 of 20.2 μM. It preferentially reduces Aβ42 generation, inhibits Aβ40 and Notch intracellular domain production, and can be used in Alzheimer's disease research.
E0079 Compound W Compound W (3,5-Bis(4-nitrophenoxy)benzoic acid) is a 3,3'-diiodothyronine sulfate (3,3'-T2S) cross-reactive material in maternal serum, which can inhibit γ-secretase.