MK-0752
For research use only. Not for use in humans.
Catalog No.S2660
10 publications
Molecular Weight(MW): 442.9
MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2.
4 Customer Reviews
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HES1 expression after treatment with clinically available GSIs R04929097, BMS-708163, LY450139, and MK-0752 as determined by qRT-PCR.
Oncotarget 2014 5(2), 363-74. MK-0752 purchased from Selleck.
Spontaneous migration in the “wound-healing assay.” Representative images of wound closure 16 hours after the scratch. Original magnification: ×200. Bar graphs represent migrated cells/field expressed as mean ± S.D.
Neoplasia, 2018, 21(1):93-105. MK-0752 purchased from Selleck.
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Western blot for Notch receptors in B5725 and C0321 cells treated with 6 μM of MK-0752 for 24 h. Control was incubation with DMSO.
Cancer Biol Ther, 2014, 15(5):633-42. MK-0752 purchased from Selleck.
Jurkat cells were treated with (D) TRAIL (20 ng/ml), MK-0752 (50 µM) or a combination of the two for 48 h. Vehicle control for (D), 0.1% (v/v) dimethyl sulfoxide. Data shown are the mean ± standard error of the mean of ≥3 independent experiments. *P≤0.05, **P≤0.01. TRAIL, tumour necrosis factor-related apoptosis-inducing ligand.
Oncol Lett, 2016, 12(4):2900-2905. MK-0752 purchased from Selleck.
Purity & Quality Control
Choose Selective Gamma-secretase Inhibitors
Biological Activity
| Description | MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2. | ||||
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| Features | A moderately potent γ-secretase inhibitor. | ||||
| Targets |
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| In vitro |
MK-0752 is identified as a moderately potent γ-secretase inhibitor, which reduces Aβ40 in a dose-dependent manner with an IC50 of 5 nM in human SH-SY5Y cells. [1] In vitro, MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation. [2] |
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| In vivo | MK-0752 (240 mg/kg) reduces the generation of newly produced Aβ with 90% decrease of AUV in the brain of rhesus monkeys. 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] In guinea-pigs, oral administration of MK-0752 (10 mg/kg -30 mg/kg) results in the dose-dependent reduction of Aβ40 in plasma, brain and cerebrospinal fluid (CSF) with IC50 of 440 nM in brain. [2] |
Protocol
| Animal Research:[1] |
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Solubility (25°C)
| In vitro | DMSO | 89 mg/mL (200.94 mM) |
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| Ethanol | 45 mg/mL (101.6 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% propylene glycol, 5% Tween 80, 65% D5W For best results, use promptly after mixing. |
30 mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 442.9 |
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| Formula | C21H21ClF2O4S |
| CAS No. | 471905-41-6 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
| Smiles | OC(=O)CCC1CCC(CC1)(C2=C(F)C=CC(=C2)F)[S](=O)(=O)C3=CC=C(Cl)C=C3 |
Bio Calculators
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Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
Frequently Asked Questions
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Question 1:
Would you happen to have the half-life information for the drug when used in cell culture?
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Answer:
The half life of S2660 in patients is about 15 hours. But its half-life time in different cell culture might be various and we generally recommend replenishing with fresh drug every 24-48 hours.
