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MK-0752

Catalog No. T2625 CAS 471905-41-6

Synonyms: MK0752

MK-0752, a γ-secretase inhibitor, reduces Aβ40 production(IC50=5 nM).

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MK-0752, CAS 471905-41-6

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Purity: 98%

Biological Description

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Storage & Solubility Information

Description	MK-0752, a γ-secretase inhibitor, reduces Aβ40 production(IC50=5 nM).
Targets&IC50	Aβ:5 nM
Kinase Assay	Protein kinase assays : Protein kinase assays are either done in-house by ELISA-based assay methods (Kit, KDR, PDGFRα, and PDGFRβ) or by a radiometric method. In-house ELISA assays used poly(Glu:Tyr) as the substrate bound to the surface of 96-well assay plates; phosphorylation is then detected using an antiphosphotyrosine antibody conjugated to HRP. The bound antibody is then quantitated using ABTS as the peroxidase substrate by measuring the absorbance at 405/490 nm. All assays uses purified recombinant kinase catalytic domains that are either expressed in insect cells or in bacteria. The Kit and EGFR protein used for in-house assays are prepared internally; other enzymes are obtained. Recombinant Kit protein is expressed as an NH2-terminal glutathione S-transferase fusion protein in insect cells and is initially purified as a nonphosphorylated (nonactivated) enzyme with a relatively high Km for ATP (400 μM). In some assays, an activated (tyrosine phosphorylated) form of the enzyme is prepared by incubation with 1 mM ATP for 1 hour at 30 °C. The phosphorylated protein is then passed through a desalting column to remove the majority of the ATP and stored at ?80 °C in buffer containing 50% glycerol. The resultant preparation has a considerably higher specific activity and a lower Km for ATP (25 μM) than the initial nonphosphorylated preparation. The inhibition of Kit autophosphorylation by OSI-930 is assayed by incubation of the nonphosphorylated enzyme at 30 °C in the presence of 200 μM ATP and various concentrations of OSI-930. The reaction is stopped by removal of aliquots into SDS-PAGE sample buffer followed by heating to 100 °C for 5 minutes. The degree of phosphorylation of Kit is then determined by immunoblotting for both total Kit and phosphorylated Kit.

Synonyms	MK0752
Molecular Weight	442.9
Formula	C21H21ClF2O4S
CAS No.	471905-41-6

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: <1 mg/mL

DMSO: 89 mg/mL (200.94 mM)

Ethanol: 45 mg/mL (101.6 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Cook JJ, et al. J Neurosci, 2010, 30(19), 6743-6750. 2. Harrison H, et al. Cancer Res, 2010, 70(2), 709-718.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Autophagy Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Anti-Alzheimer's Disease Compound Library Fluorochemical Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Breast Cancer Compound Library Stem Cell Differentiation Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

MK-0752 471905-41-6 蛋白酶体干细胞神经科学 Beta Amyloid Gamma-secretase Aβ40 MK 0752 inhibit barrier γ-secretase blood-brain Inhibitor CNS MK0752 Gamma secretase inhibitor

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