Secretase

Isoform-selective Products

Secretase Products

  • All (14)
  • Secretase Inhibitors (12)
  • Secretase Modulators (2)
  • New Secretase Products
Catalog 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.
Nat Biotechnol, 2024, 10.1038/s41587-024-02386-x
Nat Commun, 2024, 15(1):9529
J Clin Invest, 2024, 134(18)e179860
S1575 RO4929097 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.
J Cell Physiol, 2024, 10.1002/jcp.31291
Cell Transplant, 2024, 33:9636897241288932
Res Sq, 2024, rs.3.rs-3843028
S2711 DBZ (Dibenzazepine) 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.
Nat Commun, 2024, 15(1):9771
J Exp Clin Cancer Res, 2024, 43(1):295
Oncogene, 2024,
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, 2024, 15(1):8159
Cell Death Dis, 2024, 15(1):53
Cell Rep, 2024, 43(3):113837
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.
Nat Commun, 2022, 13(1):6345
Sci Rep, 2022, 12(1):7
Cell, 2021, 184(2):521-533.e14
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
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, also inhibits Notch signaling with IC50 of 14.1 nM in H4 human glioma cell. Phase 3.
Cancers (Basel), 2023, 15(6)1883
Sci Rep, 2022, 12(1):7
Calcif Tissue Int, 2022, 111(2):211-223
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. Nirogacestat (PF-03084014, PF-3084014) induces apoptosis. Phase 2.
Int J Mol Sci, 2023, 24(17)13660
Int J Mol Sci, 2023, 24(17)13660
Cancers (Basel), 2023, 15(6)1883
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
S7323 Itanapraced (CHF 5074) Itanapraced (CHF 5074, CSP-1103) is a gamma-secretase modulator that reduces Aβ42 and Aβ40 secretion. The IC50s of CHF5074 for inhibition of COX-1 and COX-2 is above 100 μmol/L.
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.
S0058New 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.
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.
S8603 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.
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.
Nat Biotechnol, 2024, 10.1038/s41587-024-02386-x
Nat Commun, 2024, 15(1):9529
J Clin Invest, 2024, 134(18)e179860
S1575 RO4929097 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.
J Cell Physiol, 2024, 10.1002/jcp.31291
Cell Transplant, 2024, 33:9636897241288932
Res Sq, 2024, rs.3.rs-3843028
S2711 DBZ (Dibenzazepine) 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.
Nat Commun, 2024, 15(1):9771
J Exp Clin Cancer Res, 2024, 43(1):295
Oncogene, 2024,
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, 2024, 15(1):8159
Cell Death Dis, 2024, 15(1):53
Cell Rep, 2024, 43(3):113837
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.
Nat Commun, 2022, 13(1):6345
Sci Rep, 2022, 12(1):7
Cell, 2021, 184(2):521-533.e14
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
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, also inhibits Notch signaling with IC50 of 14.1 nM in H4 human glioma cell. Phase 3.
Cancers (Basel), 2023, 15(6)1883
Sci Rep, 2022, 12(1):7
Calcif Tissue Int, 2022, 111(2):211-223
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. Nirogacestat (PF-03084014, PF-3084014) induces apoptosis. Phase 2.
Int J Mol Sci, 2023, 24(17)13660
Int J Mol Sci, 2023, 24(17)13660
Cancers (Basel), 2023, 15(6)1883
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
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.
S0058New 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.
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.
S7323 Itanapraced (CHF 5074) Itanapraced (CHF 5074, CSP-1103) is a gamma-secretase modulator that reduces Aβ42 and Aβ40 secretion. The IC50s of CHF5074 for inhibition of COX-1 and COX-2 is above 100 μmol/L.
S8603 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.
S0058New 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.

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Tags: Secretase antagonist |Secretase inhibitor |Secretase agonist |Secretase activator