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Mk 0752

Manufactured by MedChemExpress
Sourced in United States

MK-0752 is a chemical compound used in laboratory research. It is a potent and selective inhibitor of the enzyme 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). 11β-HSD1 plays a role in the regulation of glucocorticoid levels within cells. The primary function of MK-0752 is to serve as a research tool for studying the effects of 11β-HSD1 inhibition in various experimental models.

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2 protocols using mk 0752

1

High-Throughput Compound Screening for Drug Discovery

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Two collections of compounds assembled at the NCATS were screened A collection of 44,420 diverse small molecule drugs; and the Mechanism Interrogation PlatE 4.0 collection of 386 pharmacologically active small molecules (22 (link)). The active compounds were re-purchased for repeat and secondary assays. Milciclib (catalog #PHA-848125), MK-0752 (#HY-10974) and PP-121 (#HY-10372) were purchased from MedChem Express. Ouabain (#1076) and AMG-51 (#SYN-111) were purchased from Fisher Scientific. Vardenafil (#Y0001647) and Oridonin (#O9639) were purchased from Sigma-Aldrich. Peruvoside (# P227570) was purchased from Toronto Research Chemicals. NCGC00117362 (#D233–0871), NCGC00111761 (#C686–0165), NCGC00117328 (#D233–0834), NCGC00117505 (#D244–0327), NCGC00117477 (#D244–0252), NCGC00117166 (#D233–0497), NCGC00115018 (#D053–0260), NGC00117330 (#D233–0835) and NCGC00117364 (#D233–0885) were purchased from ChemDiv. Collagen type I (rat-tail), and fibronectin (human) were purchased from BD Biosciences. Rabbit anti-phospho m-TOR against Ser2448 (#2971), rabbit anti-mTOR (#2972), rabbit anti-phospho Rb against Ser807/811 (#8516, clone D20B12), mouse anti-Rb (#9309), mouse anti-Cdk6 (#3136), lysis buffer (#9803), and 3x Blue Loading Buffer (#56036) were purchased from Cell Signaling Technology. Mouse anti-Cdk1/Cdk2 (#sc-53219) was purchased from Santa Cruz Biotechnology Inc.
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2

Inhibition of γ-secretase in uLMS Cells

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Two human uLMS cancer cell lines, SK-UT-1B (ATCC HTB-115™) and SK-LMS-1 (ATCC HTB-88™), and one human uterine smooth muscle cell line HUt-SMC (ATCC PCS-460-011™), were purchased from ATCC (Manassas, VA, USA). uLMS cell lines were cultured in Eagle’s Minimum Essential Medium (EMEM) (ATCC) with 10% Fetal Bovine Serum (FBS) and 1% Pen-Strep. HUt-SMC was cultured in Vascular Smooth Muscle Cell Growth Kit (ATCC) as per the manufacturer’s instructions. All cells were maintained in a humidified incubator under standard culture conditions of 21% O2 and 5% CO2 at 37 °C.
γ-secretase activity was blocked by DAPT (Sigma-Aldrich, St. Louis, MO, USA) or MK-0752 (MedChemExpress, Monmouth, NJ, USA) dissolved in DMSO. SK-UT-1B and SK-LMS-1 cells were grown to greater than 80% confluence in 60 mm plates or 6-well plates and treated with DAPT or MK-0752. Vehicle control (DMSO) was used at equal volume to treatment.
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