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YO-01027 is a dipeptidic gamma-secretase inhibitor with IC50 of 2.6 and 2.9 nM for the proteolysis of APPL and Notch, respectively. YO-01027 is used as an anti-Alzheimer agent. YO-01027 directly interact with the gamma-secretase complex. Unlike other gamma-secretase inhibitors,YO-01027 targets different functional domain of the complex. YO-01027 targets the N-terminal Presenilin fragment as well as another gamma-secretase inhibitor Compound E (Cpn E), whereas DFK167 and DAPT, another two gamma-secretase inhibitors, bind to the catalytic site of the Presenilin aspartyl protease subunit and the C-terminal Presenilin fragment, respectively. In a study, YO-01027 and CpnE indicated no apparent discrimination in blocking APPL and Notch cleavages, displaying statistically equivalent IC50 values for both substrates.
| Cell Experiment | |
|---|---|
| Cell lines | BCSC |
| Preparation method | Resuspending cells at ≤1 × 106 in 100 μL sorting buffer (PBS containing 0.5% bovine serum albumin, 2 mM EDTA) and incubating with preconjugated primary antibodies BEREP4-FITC (1:10), CD44-APC (1:20), and CD24-PE (1:10) for 10 minutes at 4 °C. Washing the cells in PBS and centrifuged at 800 × g for 2 minutes. For analysis, cells are resuspending in 500 μL of sorting buffer and using FACSCalibur to measure fluorescence and using WinMIDI 2.8 to analyze . For sorting, cells are resuspended in 1× HBSS after incubation with the primary antibodies. Cells are sorted, with HBSS as sheath fluid, at 16 p.s.i. using FACSAria. The CD24low cell population gated by FACS is the lowest quintile of CD24-positive cells plus all the CD24-negative cells. |
| Concentrations | 10 μM |
| Incubation time | 3 days |
| Animal Experiment | |
|---|---|
| Animal models | C57BL/6 mice |
| Formulation | 0, 3Injected daily intraperitoneally, 10, 30 μmol/kg |
| Dosages | YO-01027 is suspended finely in 0.5% (w/v) hydroxypropylmethylcellulose (Methocel E4M) and 0.1% (w/v) Tween 80 in water. |
| Administration | Injected daily intraperitoneally |
| Molecular Weight | 463.48 |
| Formula | C26H23F2N3O3 |
| CAS Number | 209984-56-5 |
| Solubility (25°C) | DMSO 83 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Gamma-secretase/Beta-secretase Products |
|---|
| DAPT
DAPT (GSI-IX) is a γ-secretase inhibitor with IC50 values of 115 and 200 nM for total Aβ and Aβ42 respectively. DAPT inhibits the activation of Notch 1 signaling. |
| BMS-708163
BMS-708163 (Avagacestat) is a selective γ-secretase inhibitor (IC50 = 0.3 nM). |
| RO4929097
RO4929097 is a potent and selective inhibitor of γ-secretase and as a result is able to inhibit Notch pathway signaling. |
| MK-0752
MK-0752 is a potent, oral inhibitor of γ-secretase with IC50 of 5 nM in human SH-SY5Y cells. |
| LY-411575
LY-411575 is potent and selective small molecule γ-secretase inhibitor with IC50 of 0.1 nM for APP23 and APP51/16 primary neurons. |
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