• γ secretase
  • Notch

γ Secretase Selective Inhibitors | Modulators

Catalog No. Product Name Information Selective / Pan IC50 / Ki
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. Selective
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. Selective
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. Selective γ-secretase, IC50: 6.2 nM
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. Selective Gamma-secretase, Ki: 17 nM
S7394 MDL-28170 MDL-28170 (Calpain Inhibitor III) is a potent and selective calpain inhibitor of calpain that penetrates the blood-brain barrier and inhibits brain cysteine protease activity after systemic administration. MDL-28170 is also an inhibitor of γ-secretase. Selective
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. Pan γ secretase (cell-based), IC50: 0.082 nM; γ secretase (membrane-based), IC50: 0.078 nM
S2711 Dibenzazepine (YO-01027) Dibenzazepine (YO-01027, DBZ) 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. Pan γ secretase(APPL), IC50: 2.6 nM
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. Pan γ secretase, IC50: 4 nM