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Data Sheet
Product Name:Cat. No.:CAS No.:
Molecular Formula:Molecular Weight:Target:Pathway:Solubility:
MK–0752HY-10974471905-41-6C21H21ClF2O4S442.90
γ–secretase; γ–secretase
Stem Cell/Wnt; Neuronal Signaling10 mM in DMSO
BIOLOGICAL ACTIVITY:
MK–0752 is a moderately potent γ–secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM.IC50 value: 5 nM (reduces Aβ40 production) [1]Target: γ–secretase
in vitro: MK–0752 is identified as a moderately potent γ–secretase inhibitor, which reduces Aβ40 in a dose–dependent manner with anIC50 of 5 nM in human SH–SY5Y cells [1]. In vitro, MK–0752 blocks Notch–intracellular domain (ICD) cleavage and its subsequentnuclear translocation [2].
in vivo: MK–0752 (240 mg/kg) reduces the generation of newly produced Aβ with 90% decrease of AUV in the brain of rhesusmonkeys. In addition, MK–0752 treatment increases levels of Aβ 1–14, Aβ 1–15, and Aβ 1–16 , while decreases levels of Aβ 1–17 [1]. Inguinea–pigs, oral administration of MK–0752 (10 mg/kg –30 mg/kg) results in the dose–dependent reduction of Aβ40 in plasma, brainand cerebrospinal fluid (CSF) with IC50 of 440 nM in brain [2].
References:
[1]. Cook JJ, et al. Acute gamma–secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid–betaproduction to alternative APP fragments without amyloid–beta rebound. J Neurosci, 2010, 30(19), 6743–6750.
[2]. Harrison H, et al. Regulation of breast cancer stem cell activity by signaling through the Notch4 receptor. Cancer Res, 2010, 70(2), 709–718.
Caution: Product has not been fully validated for medical applications. For research use only.
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