| 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 |
|
| 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. |
Selective |
γ secretase, IC50: 0.078 nM; γ secretase, IC50: 0.082 nM |
| 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. |
Selective |
γ secretase, 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. |
Selective |
γ secretase, IC50: 4 nM |
| 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 |
gamma-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 |
