Notch Selective Inhibitors

Catalog No.	Product Name	Information	Selective / Pan	IC50 / Ki
S7169	Crenigacestat (LY3039478)	Crenigacestat (LY3039478) is an oral Notch and gamma-secretase inhibitor with IC50 of 0.41 nM for Notch.	Selective	Notch, IC50: ~1 nM
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	Notch S3 cleavage, IC50: 0.39 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	Notch, IC50: 2.9 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	Notch, IC50: 5 nM
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.	Pan	Notch, IC50: 14.1 nM