Gamma-secretase

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Gamma-secretase Inhibitors (10)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
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.
  • Nat Med, 2014, 20(4):350-9
  • Oncogene, 2014, 10.1038/onc.2014.319
  • Stem Cells, 2014, 32(1):301-12
S1575 RO4929097 RO4929097 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.
  • Hepatology, 2015, 10.1002/hep.28367
  • Dev Cell, 2014, 30(4):410-22
  • Stem Cells, 2013, 32(1):301-12
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.
  • J Biol Chem, 2014, 289(3):1540-50
  • J Biol Chem, 2012, 287(15):11810-9
  • PLoS One, 2015, 10(4):e0122451
S2660 MK-0752 MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2.
  • Oncogene, 2015, 10.1038/onc.2015.306
  • Oncotarget, 2014, 5(2):363-74
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.
  • Stem Cells, 2014, 32(1):301-12
  • Oncotarget, 2014, 5(2):363-74
  • Sci Rep, 2015, 5:8782
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.
S2711 YO-01027 (Dibenzazepine) YO-01027 (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.
  • Cell Death Dis, 2015, 6:e1631
  • J Pharma Invest, 2014, 10.1007/s40005-014-0151-2
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.
  • Cell Rep, 2014, 6(3):467-81
S7399 FLI-06 FLI-06 is a novel inhibitor of Notch signaling with EC50 of 2.3 μM.
S8018 PF-03084014 (PF-3084014) PF-03084014 (PF-3084014) is a selective gamma-secretase inhibitor with IC50 of 6.2 nM in a cell-free assay. Phase 2.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S2215 DAPT (GSI-IX) <1 mg/mL 86 mg/mL 50 mg/mL
S1575 RO4929097 <1 mg/mL 94 mg/mL 16 mg/mL
S1594 Semagacestat (LY450139) <1 mg/mL 72 mg/mL 41 mg/mL
S2660 MK-0752 <1 mg/mL 89 mg/mL 45 mg/mL
S1262 Avagacestat (BMS-708163) <1 mg/mL 104 mg/mL <1 mg/mL
S7673 L-685,458 <1 mg/mL 100 mg/mL 6 mg/mL
S2711 YO-01027 (Dibenzazepine) <1 mg/mL 92 mg/mL <1 mg/mL
S2714 LY411575 <1 mg/mL 95 mg/mL 13 mg/mL
S7399 FLI-06 <1 mg/mL 88 mg/mL 8 mg/mL
S8018 PF-03084014 (PF-3084014) <1 mg/mL 97 mg/mL 97 mg/mL
Tags: Gamma-secretase inhibition | Gamma-secretase inhibitor Notch | Gamma-secretase activity | Gamma-secretase assay | Gamma-secretase cleavage | Gamma-secretase inhibitor in clinical trial | Gamma-secretase inhibitor review
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