Aβ Selective Inhibitors
| Catalog No. | Product Name | Information | Selective / Pan | IC50 / Ki |
|---|---|---|---|---|
| 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. |
Selective | γ secretase(Aβ42), IC50: 0.27 nM; γ secretase(Aβ40), IC50: 0.3 nM |
| S2215 | DAPT (GSI-IX) | DAPT (GSI-IX) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells. |
Selective | γ secretase(Aβ), IC50: 20 nM |
| S2660 | MK-0752 | MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2. |
Selective | |
| 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. Phase 3. |
Pan | γ secretase(Aβ38), IC50: 12.0 nM; γ secretase(Aβ42), IC50: 10.9 nM; γ secretase(Aβ40), IC50: 12.1 nM |
