A potent inhibitor of γ-secretase
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MK-0752

Item No. 16706

Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)-cyclohexanepropanoic acid
CAS Number
471905-41-6
Molecular Formula
C21H21ClF2O4S
Formula Weight
442.9
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mlDMSO: 10 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/mlEthanol: 5 mg/ml
λmax
230, 275 nm
SMILES
O=C(O)CC[C@H]1CC[C@](S(C2=CC=C(Cl)C=C2)(=O)=O)(C3=C(F)C=CC(F)=C3)CC1
InChi Code
InChI=1S/C21H21ClF2O4S/c22-15-2-5-17(6-3-15)29(27,28)21(18-13-16(23)4-7-19(18)24)11-9-14(10-12-21)1-8-20(25)26/h2-7,13-14H,1,8-12H2,(H,25,26)/t14-,21+
InChi Key
XCGJIFAKUZNNOR-QCKZDCLWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $75

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    5 mg

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    10 mg

    $479

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    Cayman Chemical
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    Product Description

    MK-0752 is a potent, reversible inhibitor of γ-secretase, reducing the cleavage of APP to Aβ40 in human neuroblastoma SH-SY5Y cells with an IC50 value of 5 nM.1,2 It is orally bioavailable and crosses the blood-brain barrier, as orally administered MK-0752 dose-dependently reduces the generation of new amyloid β protein in the brain of rhesus monkeys.2 Through its effects on the Notch pathway, MK-0752 reduces the number of breast cancer stem cells in tumorgrafts, enhancing the efficacy of the chemotherapy drug docetaxel (Item No. 11637) in mice with breast cancer tumors.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Matthews, C.Z., and Woolf, E.J. Determination of a novel gamma-secretase inhibitor in human plasma and cerebrospinal fluid using automated 96 well solid phase extraction and liquid chromatography/tandem mass spectrometry. J. Chromatogr. B Analyt. Technol. Biomed. Life Sci. 863(1), 36-45 (2008).

    2. 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. Neurosci. 30(19), 6743-6750 (2010).

    3. Schott, A.F., Landis, M.D., Dontu, G., et al. Preclinical and clinical studies of gamma secretase inhibitors with docetaxel on human breast tumors. Clin. Cancer Res. 19(6), 1512-1524 (2013).