MK-0752 sodium
Based on 14 publication(s) in Google Scholar
MK-0752 sodium is a potent, orally active and specific γ-secretase inhibitor, showing dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. MK-0752 sodium crosses the blood-brain barrier. MK-0752 sodium reduces newly generated CNS Aβ in vivo.
For research use only. We do not sell to patients.
- CAS No.: 656810-87-6
- Formula: C21H20ClF2NaO4S
- Molecular Weight:464.89
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) MK-0752 sodium
More- Nat Biotechnol. 2024 Nov 25. [Abstract]
- Nat Mater. 2025 Feb 17. [Abstract]
- EMBO Mol Med. 2017 Jul;9(7):950-966. [Abstract]
- Int J Mol Sci. 2022 May 26;23(11):5980. [Abstract]
- Biofactors. 2025 Jan-Feb;51(1):e2091. [Abstract]
- Cancers (Basel). 2024 Jun 10;16(12):2184. [Abstract]
- Front Biosci (Landmark Ed). 2025 Apr 23;30(4):37430. [Abstract]
- J Biol Chem. 2019 Jul 19;294(29):11276-11285. [Abstract]
- J Cell Physiol. 2021 Feb;236(2):1237-1251. [Abstract]
- J Cell Sci. 2021 Oct 8;jcs.258432. [Abstract]
- Mol Biol Rep. 2024 Nov 8;51(1):1134. [Abstract]
- Reprod Fertil Dev. 2019 May;31(6):1091-1103. [Abstract]
- J Recept Signal Transduct Res. 2021 Oct;41(5):457-465. [Abstract]
- Andrologia. 2019 Nov;51(10):e13413. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Biological Activity
Description
Chemical Information
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CAS No. 656810-87-6
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Molecular Weight 464.89
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Formula C21H20ClF2NaO4S
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SMILES
O=C(CC[C@H]1CC[C@@](C2=CC(F)=CC=C2F)(S(=O)(C3=CC=C(Cl)C=C3)=O)CC1)O[Na]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (14)
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Journal Impact Factor
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Most Recent
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Nat Biotechnol
Intravenous administration of blood-brain barrier-crossing conjugates facilitate biomacromolecule transport into central nervous system. [Abstract]2024 Nov 25. PMID: 39587229 -
Nat Mater
Blood-brain-barrier-crossing lipid nanoparticles for mRNA delivery to the central nervous system. [Abstract]2025 Feb 17. PMID: 39962245 -
EMBO Mol Med
γ-Secretase inhibitors in cancer clinical trials are pharmacologically and functionally distinct. [Abstract]2017 Jul;9(7):950-966. PMID: 28539479
MK-0752 sodium purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2017 Jul;9(7):950-966. [Abstract]
IC50 curves of MK-0752 (10-4-104 nM) on cNOTCHsub.
MK-0752 sodium purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2017 Jul;9(7):950-966. [Abstract]
Dose responses of cAPPC100sub and full-length APP cleavage to MK-0752 (10-4-104 nM).
MK-0752 sodium purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2017 Jul;9(7):950-966. [Abstract]
MK-0752 (100 nM-12.5 μM) strongly decreased NICD levels in the breast cancer line MDA-MB-231.
MK-0752 sodium purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2017 Jul;9(7):950-966. [Abstract]
MK-0752 (0.5-12.5 μM) inhibited APP-CTF process in MDA-MB-231 cells in a dose-dependent manner.
MK-0752 sodium purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2017 Jul;9(7):950-966. [Abstract]
Absolute viable cell counts of mammospheres from MDA-MB-231 and MDA-MB-468 cell lines treated with MK-0752 (10 μM; 7 d).
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Int J Mol Sci
Gamma Secretase Inhibitors as Potential Therapeutic Targets for Notch Signaling in Uterine Leiomyosarcoma. [Abstract]2022 May 26;23(11):5980. PMID: 35682660 -
Biofactors
2025 Jan-Feb;51(1):e2091. PMID: 38994725 -
Cancers (Basel)
Combined Treatment of Uterine Leiomyosarcoma with Gamma Secretase Inhibitor MK-0752 and Chemotherapeutic Agents Decreases Cellular Invasion and Increases Apoptosis. [Abstract]2024 Jun 10;16(12):2184. PMID: 38927890 -
Front Biosci (Landmark Ed)
Macrophage Notch1 Participates in LPS-Induced Acute Lung Injury via Regulating CCR5 Expression in Mice. [Abstract]2025 Apr 23;30(4):37430. PMID: 40302346 -
J Biol Chem
Individual and combined presenilin 1 and 2 knockouts reveal that both have highly overlapping functions in HEK293T cells. [Abstract]2019 Jul 19;294(29):11276-11285. PMID: 31167792 -
J Cell Physiol
Vitamin C alleviates the senescence of periodontal ligament stem cells through inhibition of Notch3 during long-term culture. [Abstract]2021 Feb;236(2):1237-1251. PMID: 32662081 -
J Cell Sci
2021 Oct 8;jcs.258432. PMID: 34622921 -
Mol Biol Rep
2024 Nov 8;51(1):1134. PMID: 39514048 -
Reprod Fertil Dev
2019 May;31(6):1091-1103. PMID: 30827331 -
J Recept Signal Transduct Res
Function and mechanism exploration of zinc finger protein 64 in lung adenocarcinoma cell growth and metastasis. [Abstract]2021 Oct;41(5):457-465. PMID: 33054540 -
Andrologia
2019 Nov;51(10):e13413. PMID: 31523838
MK-0752 sodium purchased from MedChemExpress. Usage Cited in: Andrologia. 2019 Nov;51(10):e13413. [Abstract]
MK-0752 regulated the expression of cell proliferation-related genes at the mRNA and protein levels. The relative protein expression of p27 and p21Waf1/Cip1 in TM3 Leydig cells after treatment with 25 μM MK-0752 respectively. The representative Western blots for p27 and p21Waf1/Cip1 after treatment with MK-0752.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Notch Pathway Solutions
The Notch pathway is a contact-dependent signaling pathway that controls cell-fate decisions, differentiation, proliferation, and tissue patterning through interactions between membrane-bound Notch receptors and membrane-bound ligands on neighboring cells. Canonical Notch signaling is activated when ligand engagement triggers proteolytic release of the Notch intracellular domain, which enters the nucleus and regulates transcription together with DNA-binding transcriptional complexes. In the canonical mechanism, ligand-dependent Notch activation leads to release of the intracellular Notch domain, and presenilin-dependent γ-secretase activity is required for production of the active intracellular signaling fragment. The released intracellular domain functions as a nuclear signal that converts Notch receptor activation at the membrane into transcriptional regulation of target programs such as HES/HEY-family genes and other context-dependent downstream targets. The literature links Notch p
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
References
[1]. Cook JJ, et al. Acute gamma-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-beta production to alternative APP fragments without amyloid-beta rebound. J Neurosci. 2010;30(19):6743-6750. [Content Brief]
[2]. Krop I, et al. Phase I pharmacologic and pharmacodynamic study of the gamma secretase (Notch) inhibitor MK-0752 in adult patients with advanced solid tumors. J Clin Oncol. 2012;30(19):2307-2313. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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