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Bioactive compound library

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The Bioactive Compound Library is a comprehensive collection of chemical compounds with known biological activity. It is designed to facilitate drug discovery and research in various fields, including pharmaceutical, agrochemical, and academic applications. The library contains a diverse range of small molecules with documented therapeutic or research potential, providing researchers with a valuable resource for screening and lead identification.

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Lab products found in correlation

Lopac library, by Merck Group (2 mentions) Vinblastine, by Selleck Chemicals (2 mentions) Sorafenib, by Selleck Chemicals (2 mentions) Bazedoxifene, by Selleck Chemicals (2 mentions) Camptothecin, by Selleck Chemicals (2 mentions) Rapamycin, by Thermo Fisher Scientific (2 mentions) Etoposide, by Thermo Fisher Scientific (2 mentions) Raloxifene, by Selleck Chemicals (2 mentions) Bortezomib, by Thermo Fisher Scientific (2 mentions) Gcn2ib, by MedChemExpress (2 mentions) Jtc 801, by Selleck Chemicals (2 mentions) Ink128, by Selleck Chemicals (2 mentions) D arginine, by Merck Group (2 mentions) Buthionine sulfoximine, by Thermo Fisher Scientific (2 mentions) Azd8055, by Selleck Chemicals (2 mentions) L arginine, by Merck Group (2 mentions) L citrulline, by Merck Group (2 mentions) Dimethyl sulfoxide (dmso), by Merck Group (2 mentions) Cycloheximide (chx), by Merck Group (2 mentions) Thapsigargin, by Merck Group (2 mentions)

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Compound library (4 citations) L1700 bioactive compound library (2 citations)

7 protocols using bioactive compound library

1

Screening of Biologically Active Compounds

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The screen was performed at the Case Western Reserve University School of Medicine Small Molecule Drug Development Core facility on 10K “pre-aged” (precultured for 45–50 PD) NHDF. The collection of biologically active molecules was compiled from LOPAC library (Sigma) and Bioactive Compound Library (Selleck Chemicals). A total of 2684 mechanistically annotated compounds were used for the screening. A set of redox catalysts were added to the screen, including: VA, dimethyl-nitrosoaniline, diethyl-nitrosoaniline, 1-nitroso-2-naphthol, 2-nitroso-1-naphthol, CYPMPO, DMPO, methylene blue and coniferron (Sigma-Aldrich). Stock solutions were prepared in DMSO at 10 mM. For screening, 384-well assay plates were prepared with final drug concentrations of 5 μM using a Janus liquid handling platform (Perkin Elmer) equipped with 50 nL pin transfer tool (V&P Scientific). For concentration–response studies, lead compounds were retested at eight concentrations in two-fold dilutions. A final DMSO concentration of 0.1% was not exceeded in the screening assay and in hit validation. The negative controls contained the same percentage of vehicle/DMSO. In each screening plate two vehicle columns (32 wells) served as controls. In each titration plate, four vehicle columns (64 wells) served as controls.
Vatolin S., Radivoyevitch T, & Maciejewski J.P. (2019). New drugs for pharmacological extension of replicative life span in normal and progeroid cells. NPJ Aging and Mechanisms of Disease, 5, 2.
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2

Compound Library Screening for Bioactive Inhibitors

Cited 1 time
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An 1,833-member bioactive compound library, and an independent 86-member PI3K signaling inhibitor library comprising mTOR, PI3K and AKT pathway inhibitors, were obtained from Selleck Chemicals and stored at −80°C. Erastin2, annotated as compound 35MEW28 (Ref.51 (link)) and ML162 were synthesized by Acme Bioscience. Erastin was the kind gift of B. Stockwell (Columbia). Chemical used (supplier) were: DMSO, ferrostatin-1, thapsigargin, tunicamycin, cycloheximide, L-arginine, D-arginine and L-citrulline (Sigma-Aldrich Corporation); bortezomib, rapamycin, etoposide and buthionine sulfoximine (Thermo-Fisher Scientific); INK 128, AZD8055, vinblastine, camptothecin, sorafenib, bazedoxifene, raloxifene and JTC-801 (Selleck Chemicals); and GCN2iB (MedChemExpress). buthionine sulfoximine was dissolved directly into cell media. All other drugs were prepared as stock solutions in DMSO. Stock solutions were stored at −20˚C.
Conlon M., Poltorack C.D., Forcina G.C., Armenta D.A., Mallais M., Perez M.A., Wells A., Kahanu A., Magtanong L., Watts J.L., Pratt D.A, & Dixon S.J. (2021). A Compendium of Kinetic Modulatory Profiles Identifies Ferroptosis Regulators. Nature chemical biology, 17(6), 665-674.
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3

Screening FDA-Approved Drugs Against L. donovani

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The Selleckchem Bio-Active Compound Library (Catalog# Selleck_L1700, was comprised of a 4718-member Bioactive Compound Library-I as of May, 2019 which included 1622 FDA approved compounds and the rest were advanced investigational compounds at different stages in drug development and was subjected to curation based on known activity against different intracellular parasites. The sources for the data were gathered from all known available resources including journals, patents, and other published literature. To associate known activity against protozoan parasites within the FDA-approved compound library, data mining was performed using text-, structure-, and activity- etc. based queries on CHEMBL [15 (link)] and ChemSpider servers [16 ]. The FDA-approved library was thus shortlisted to 96 compounds. These compounds were subjected to initial exploratory screening against L. donovani amastigotes with two concentrations of 100 μM and 10 μM(from 10mM stocks) in triplicate for each compound using live-cell fluorescence imaging as described in detail under the drug susceptibility assay heading below.
Gupta Y., Goicoechea S., Romero J.G., Mathur R., Caulfield T.R., Becker D.P., Durvasula R, & Kempaiah P. (2022). Repurposing Lansoprazole and Posaconazole to treat leishmaniasis: Integration of in vitro testing, pharmacological corroboration, and mechanisms of action. Journal of Food and Drug Analysis, 30(1), 128-149.
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4

Screening of Bioactive Compound Libraries

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The Collection of Biologically Active Molecules (Collection3115) was compiled from the LOPAC library (Sigma, St. Louis, MO, USA) and Bioactive Compound Library (Selleck Chemicals, Houston, TX, USA). A total of 3115 mechanistically annotated and partially redundant compounds were subjected to screening. All compounds were dissolved in DMSO to a stock concentration of 10 mM. The final DMSO concentration did not exceed 0.1 % in the screening assay or during hit validation, and the negative and positive controls contained the same vehicle percentage. Upon hit identification, all compounds were retested as 10 mM stock solutions purchased from Selleck Chemicals.
Zhang L., Fedorov Y., Andams D, & Lin F. (2018). Identification of complement inhibitory activities of two chemotherapeutic agents using a high-throughput cell imaging-based screening assay. Molecular immunology, 101, 86-91.
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5

Diverse Bioactive Compound Screening

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All chemical compounds used in this study are from the Selleckchem Bioactive Compound library (Cat. number: Catalog No. L1700) and were selected to represent diverse MOAs and effects on different cellular targets. Detailed information for each compound and the dilution series are provided in Supplementary Data 4, including information on MOAs and/or known biological targets, as well as specific functional annotations (e.g., topoisomerase, mitochondrial enzymes, HDAC inhibitor).
Pearson Y.E., Kremb S., Butterfoss G.L., Xie X., Fahs H, & Gunsalus K.C. (2022). A statistical framework for high-content phenotypic profiling using cellular feature distributions. Communications Biology, 5, 1409.
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6

Compound Library Screening for Bioactive Inhibitors

Cited 1 time
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An 1,833-member bioactive compound library, and an independent 86-member PI3K signaling inhibitor library comprising mTOR, PI3K and AKT pathway inhibitors, were obtained from Selleck Chemicals and stored at −80°C. Erastin2, annotated as compound 35MEW28 (Ref.51 (link)) and ML162 were synthesized by Acme Bioscience. Erastin was the kind gift of B. Stockwell (Columbia). Chemical used (supplier) were: DMSO, ferrostatin-1, thapsigargin, tunicamycin, cycloheximide, L-arginine, D-arginine and L-citrulline (Sigma-Aldrich Corporation); bortezomib, rapamycin, etoposide and buthionine sulfoximine (Thermo-Fisher Scientific); INK 128, AZD8055, vinblastine, camptothecin, sorafenib, bazedoxifene, raloxifene and JTC-801 (Selleck Chemicals); and GCN2iB (MedChemExpress). buthionine sulfoximine was dissolved directly into cell media. All other drugs were prepared as stock solutions in DMSO. Stock solutions were stored at −20˚C.
Conlon M., Poltorack C.D., Forcina G.C., Armenta D.A., Mallais M., Perez M.A., Wells A., Kahanu A., Magtanong L., Watts J.L., Pratt D.A, & Dixon S.J. (2021). A Compendium of Kinetic Modulatory Profiles Identifies Ferroptosis Regulators. Nature chemical biology, 17(6), 665-674.
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7

Chemical Screen in E2F1 Knockout Cells

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Chemical screen was performed at Duke University Genetic and Chemical Screening Services. Wildtype or E2F1 knockout H1299 cells were plated using a Matrix WellMate onto 384-well plates that had been stamped using a Labcyte Echo Acoustic Dispenser with the Bioactive compound library (Selleckchem), for a final concentration of 1.25 μM in duplicate plates. Cells were incubated for 48 hours and assayed for cell viability with Cell Titer-Glo (Promega). All well values were normalized to the average of DMSO control wells found on each plate. Figure 1A shows average normalized values of duplicate plates. Full screen results can be found in Table S1.
Shats I., Williams J.G., Liu J., Makarov M.V., Wu X., Lih F.B., Deterding L.J., Lim C., Xu X., Randall T.A., Lee E., Li W., Fan W., Li J.L., Sokolsky M., Kabanov A.V., Li L., Migaud M.E., Locasale J.W, & Li X. (2020). Bacteria boost mammalian host NAD metabolism by engaging the deamidated biosynthesis pathway. Cell metabolism, 31(3), 564-579.e7.
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