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MK-0752

Catalog No.
A4006
γ-secretase inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$193.00
In stock
Evaluation Sample
$30.00
In stock
5mg
$187.00
In stock
10mg
$253.00
In stock
50mg
$649.00
In stock
100mg
$1,188.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

MK-0752 (CAS 471905-41-6) is a small molecule inhibitor of γ-secretase, an enzymatic complex responsible for proteolytic cleavage of the Notch receptor. γ-secretase-mediated cleavage releases the Notch intracellular domain (NICD), thereby activating gene transcription essential for cellular differentiation, proliferation, and survival. MK-0752 potently inhibits γ-secretase enzymatic activity, with an IC50 of approximately 50 nM. In vitro, inhibition of γ-secretase by MK-0752 suppresses proliferation of breast cancer cells. This compound has been investigated in clinical studies for advanced breast cancer and other solid tumors as well as pediatric refractory CNS malignancies, underscoring its relevance for oncology research targeting Notch signaling.

Product Citation

Chemical Properties

StorageStore at -20°C
M.Wt442.9
Cas No.471905-41-6
FormulaC21H21ClF2O4S
SynonymsMK 0752, MK0752
Solubility≥22.15 mg/mL in DMSO; insoluble in H2O; ≥48.8 mg/mL in EtOH with ultrasonic
Chemical Name3-[4-(4-chlorophenyl)sulfonyl-4-(2,5-difluorophenyl)cyclohexyl]propanoic acid
SDFDownload SDF
Canonical SMILESC1CC(CCC1CCC(=O)O)(C2=C(C=CC(=C2)F)F)S(=O)(=O)C3=CC=C(C=C3)Cl
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment: [1]

Cell lines

SH-SY5Y cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

IC50: 5 nM.

Applications

As a moderately potent γ-secretase inhibitor, MK-0752 inhibited the production of Aβ40 in a dose-dependent manner with an IC50 of 5 nM in human SH-SY5Y cells.

Animal experiment : [1]

Animal models

Male CMP rhesus monkeys

Dosage form

Oral administration, 60 mg/kg and 240mg/kg

Applications

Oral administration of MK-0752 demonstrated a dose-related reduction of Aβ levels. After 48 h, the Aβ levels with 240mg/kg treatment only recovered to 50%of baseline, while the 60mg/kg treatment group reached baseline at 30 h without overshoot. Plasma Aβ levels rebounded above baseline after MK-0752 inhibition (60 mg/kg, h 33–48).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Cook J J, Wildsmith K R, Gilberto D B, et al. Acute γ-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-β production to alternative APP fragments without amyloid-β rebound[J]. The Journal of Neuroscience, 2010, 30(19): 6743-6750.

Biological Activity

Targets γ-secretase          
IC50 5 nM          

Quality Control