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MK-0752

Catalog No. T2625 CAS 471905-41-6

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

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MK-0752, CAS 471905-41-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 54.00
2 mg	In stock	$ 96.00
5 mg	In stock	$ 173.00
10 mg	In stock	$ 260.00
25 mg	In stock	$ 466.00
50 mg	In stock	$ 683.00
100 mg	In stock	$ 973.00
1 mL * 10 mM (in DMSO)	In stock	$ 183.00

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Purity: 99.19%

Purity: 98.99%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	MK-0752, a γ-secretase inhibitor, reduces Aβ40 production(IC50=5 nM).
Targets&IC50	β-Amyloid:5 nM
In vitro	In guinea pigs, oral administration of MK-0752 (10-30 mg/kg) resulted in a dose-dependent reduction of Aβ40 in the plasma, brain, and cerebrospinal fluid. Similarly, in monkeys, MK-0752 (240 mg/kg) was capable of reducing the production of Aβ in the brain.
In vivo	In human SH-SY5Y cells, MK-0752 significantly reduces Aβ40 in a dose-dependent manner with an IC50 of 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.

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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 89 mg/mL (200.94 mM)

Ethanol: 45 mg/mL (101.6 mM)

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 Drug Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library NO PAINS Compound Library Stem Cell Differentiation Compound Library Protease Inhibitor Library Orally Active Compound Library

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PE859 PBD-150 β-Amyloid (1-15) δ-secretase inhibitor 11 Rutin hydrate β-Amyrin Neoechinulin A Hoechst 34580

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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 Neuroscience Proteases/Proteasome Stem Cells Gamma-secretase Beta Amyloid Aβ40 inhibit barrier γ-secretase blood-brain Inhibitor MK 0752 CNS MK0752 Gamma secretase inhibitor

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