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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.
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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 |
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Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. |
| RE(EDANS)EVNLDAEFK(DABCYL)R
RE (EDANS) EVNLDAEFK (DABCYL) R is an EDANS and DABCYL double-labeled peptide，serves as a fluorescent substrate for BACE1(Em=360nm，Ex=528nm). |
| β-Secretase inhibitor
β-Secretase inhibitor ([Asn670, Sta671, Val672]-Amyloid β Peptide (662-675)) is a β-secretase and BACE1 inhibitor (IC50: 25 nM for β-secretase). |
| Mca-SEVNLDAEFK(Dnp)
Mca-SEVNLDAEFK(Dnp) is a Beta-secretase 1 (BACE-1) peptide FRET substrate, containing the 'Swedish' Lys-Met/Asn-Leu mutation of the amyloid precursor protein (APP) β-secretase cleavage site. |
| BACE1-IN-10
BACE1-IN-10 is a potent BACE1 Inhibitor. |
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