MK-0752
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.
- 1. Di Huang, Jiamin Qiu, et al. "In Vitro Evaluation of Clinical Candidates of γ-Secretase Inhibitors: Effects on Notch Inhibition and Promoting Beige Adipogenesis and Mitochondrial Biogenesis." Pharm Res 2020 Sep 4;37(10):185. PMID: 32888109
- 2. Chen X, Gong L, et al. "Sequential combination therapy of ovarian cancer with cisplatin and γ-secretase inhibitor MK-0752." Gynecol Oncol. 2016 Mar;140(3):537-44. PMID: 26704638
Storage | Store at -20°C |
M.Wt | 442.9 |
Cas No. | 471905-41-6 |
Formula | C21H21ClF2O4S |
Synonyms | MK 0752, MK0752 |
Solubility | ≥22.15 mg/mL in DMSO; insoluble in H2O; ≥48.8 mg/mL in EtOH with ultrasonic |
Chemical Name | 3-[4-(4-chlorophenyl)sulfonyl-4-(2,5-difluorophenyl)cyclohexyl]propanoic acid |
SDF | Download SDF |
Canonical SMILES | C1CC(CCC1CCC(=O)O)(C2=C(C=CC(=C2)F)F)S(=O)(=O)C3=CC=C(C=C3)Cl |
Shipping Condition | Small 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. |
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. |
Targets | γ-secretase | |||||
IC50 | 5 nM |
Quality Control & MSDS
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Chemical structure

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