All AbMole products are for research use only, cannot be used for human consumption.
MK-0752 is a potent gamma secretase inhibitor, an enzyme required for Notch pathway activation. MK-0752 reduces Aβ40 production with IC50 of 5 nM in human SH-SY5Y cells. MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation in vitro. MK-0752 treatment increases levels of Aβ 1-14, Aβ 1-15 and Aβ 1-16, while decreases levels of Aβ 1-17. Phase I clinical trials has been completed in 2006, and the results reported showed that MK-0752 was well-tolerated in a limited number of patients below 300 mg/m2, and further enrollment was underway to establish the MTD.
 |
Source | Oncol Lett (2016). Figure 2. MK-0752 |
| Method | Flow cytometric analysis | |
| Cell Lines | T‑cell | |
| Concentrations | 50 μM | |
| Incubation Time | 48 h | |
| Results | Furthermore, the second GSI MK.0752, which is currently under clinical evaluation for various cancer types, also significantly enhanced TRAIL.induced apoptosis in T.ALL cells |
| Molecular Weight | 442.9 |
| Formula | C21H21ClF2O4S |
| CAS Number | 471905-41-6 |
| Solubility (25°C) | DMSO 79 mg/mL Ethanol 35 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. |
| 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. |
| LY2811376
LY2811376 is an orally available, non-peptidic β-secretase inhibitor with IC50 of 239 nM-249 nM. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
