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
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 K_i of 17 nM.	Selective	gamma-secretase, Ki: 17 nM