Sgx523

Manufactured by Bio-Techne

SGX523 is a small molecule inhibitor developed by Bio-Techne. It targets the receptor tyrosine kinase MET. The core function of SGX523 is to inhibit the enzymatic activity of the MET protein.

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2 protocols using sgx523

Hepatic S9 Fraction Procurement and Characterization

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Potassium phosphate, formic acid, NADPH, MgCl₂, zaleplon, O⁶-benzylguanine, and hydralazine hydrochloride were purchased from Sigma-Aldrich (St. Louis, MO). Zoniporide dihydrochloride, BIBX1382 dihydrochloride, and SGX523 were purchased from Tocris Bioscience (R&D Systems, Minneapolis, MN). Pooled human hepatic S9 (150-donor, mixed gender pool) was obtained from BD Biosciences (San Diego, CA), and male Sprague-Dawley rat (n=36 pool), cynomolgus monkey (n=2, pool), and CD-1 mouse (n=170 pool) hepatic S9 were obtained from Corning Inc. (Tewksbury, MA). Male rhesus monkey (n= 6 pool) and Hartley guinea pig (n=50 pool) hepatic S9 were purchased from XenoTech (Lenexa, KS), and male Gottingen minipig (n= 7 pool) hepatic S9 was purchased from BioreclamationIVT (Baltimore, MD). All solvents used for bioanalysis were purchased from Sigma-Aldrich or Fisher Scientific (Waltham, MA) and were of high-performance liquid chromatography (HPLC) grade.

Crouch R.D., Hutzler J.M, & Daniels J.S. (2017). A novel in vitro allometric scaling methodology for aldehyde oxidase substrates to enable selection of appropriate species for traditional allometry. Xenobiotica; the fate of foreign compounds in biological systems, 48(3), 219-231.

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Listeria Infection Assay with Drugs

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Hoechst (Thermofisher; D1306) was dissolved at 1 mg/ml in DMSO and used at 1:1000. Drugs were dissolved in DMSO (Sigma; D2650) at the stock concentrations indicated: 10 mM FAK inhibitor-14 (FAK-14; Tocris Bioscience; 3414), 100 mM PF573228 (Tocris Bioscience; 3239), 20 mM SGX 523 (Tocris Bioscience; 5356), 42 mM withaferin (Sigma-Aldrich; W4394). Primary antibody used for staining of extracellular Lm was rabbit polyclonal anti-Listeria genus-specific antibody (ABCAM; ab35132). Primary antibody used for staining Li was goat polyclonal BacTrace anti-Listeria genus-specific antibody (SeraCare Life Sciences; 01-90-90). For incubation of cells with vimentin antibodies prior to infection or immunostaining of surface vimentin, rabbit polyclonal H-84 vimentin antibody (Santa Cruz Biotechnologies; sc-5565) was used. For isotype controls, cells were incubated with rabbit immunoglobulin G (IgG) (Sigma; I5006). For Western blotting, the following antibodies were used: rabbit polyclonal phospho-FAK Tyr397 (ThermoFisher; 44-624G), mouse monoclonal anti-FAK (EMD Millipore, 05-182), rabbit monoclonal anti-Met (cMet) antibody (Abcam; ab51067), and anti-GAPDH antibody (Cell Signaling; 140C10).

Bastounis E.E., Yeh Y.T, & Theriot J.A. (2018). Matrix stiffness modulates infection of endothelial cells by Listeria monocytogenes via expression of cell surface vimentin. Molecular Biology of the Cell, 29(13), 1571-1589.

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