Compound Libraries | Tocriscreen Small Molecule Screening

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Trust Tocris’ 35 year leadership in small molecule production to further your research with expertly selected chemical libraries of annotated, bioactive compounds.</p></div> </div> </div> </div> <div class="layout__region layout__region--second"> <div class="hero-content-wrap"> <div class="field_block:paragraph:h1_2_2_text_to_media:field_indv_media"> <div> <img src="https://resources.bio-techne.com/bio-techne-assets/images/banners/tocriscreen_plate_2.png" alt="Tocriscreen plate and molecules for compound libraries page" fetchpriority="high" > </div> </div> </div> </div> </div> </div> </div> </div> </div> </section> </div> </div> </header> </div> <div id="main" class="container-fluid container-wide"> <div class="row"> <div class="col-md-12"> <div> <div id="block-bio-techne-global-breadcrumbs" class="system_breadcrumb_block"> <nav role="navigation" aria-labelledby="system-breadcrumb"> <h2 id="system-breadcrumb" class="visually-hidden">Breadcrumb</h2> <ol> <li> <a href="/">Home</a> </li> <li> <a href="/reagents">Bio-Techne Reagents</a> </li> <li> Compound Libraries </li> </ol> </nav> </div> </div> </div> </div> <main> <section class="section"> <div> <div id="block-bio-techne-global-content" class="system_main_block"> <article> <div> <div> <div> <div class="paragraph paragraph--type--freeform mb-4 paragraph--view-mode--default"> <div><p><a href="#why">Why Tocriscreen?</a> | <a href="#available">Off-The-Shelf Libraries</a> | <a href="#custom">Custom Compound Libraries</a> | <a href="#applications">Applications</a> | <a href="#related">Related Products</a> | <a href="#inquire">Inquire</a></p></div> </div> </div> <div> <div class="paragraph paragraph--type--freeform mb-4 paragraph--view-mode--default"> <div><p><a name="why"></a></p></div> </div> </div> <div> <div class="paragraph paragraph--type--_-2-media-to-text mb-4 paragraph--view-mode--default"> <div class="container-fluid container-wide"> <div class="layout layout--twocol-section layout--twocol-section--50-50"> <div class="layout__region layout__region--first"> <div class="hero-content-wrap"> <div class="field_block:paragraph:2_2_media_to_text:field_indv_media"> <div> <a href="https://www.bio-techne.com/t/compound-libraries" title="View All Compound Libraries" > <img src="https://resources.bio-techne.com/bio-techne-assets/images/research-areas/compound_library_features.jpg" alt="Tocriscreen Bioactive Compound Libraries" loading="lazy" > </a> </div> </div> </div> </div> <div class="layout__region layout__region--second"> <div class="hero-content-wrap"> <div class="field_block:paragraph:2_2_media_to_text:field_header_2_global"> <div><h2>Why Tocriscreen?</h2></div> </div> <div class="field_block:paragraph:2_2_media_to_text:field_lg_sngl_frmtd_text_global"> <div><p>Safeguard your research success by ensuring you have the right bioactive compounds for your research. Our carefully crafted <strong>Tocriscreen Compound Libraries</strong> are unique collections of ready-to-screen compounds, ideal to kick-start your project.</p><ul><li><strong>Boost innovation</strong> with a mix of gold standards, Tocris exclusives, and the latest probes</li><li><strong>Guarantee integrity</strong> with small molecules that cover a wide range of pharmacological targets and research areas</li><li><strong>Trust your results</strong> - our expertly-curated, biologically active compounds have proven pharmacological activity</li><li><strong>Ensure reproducibility </strong>with rigorously quality-controlled compounds</li><li><strong>Be fully informed</strong> with detailed biological and chemical information for each compound</li><li><strong>Save time</strong> with ready-to-screen, pre-solubilized compounds (DMSO, 10 mM)</li><li><strong>Safeguard continuity</strong> with easy and consistent re-supply from the Tocris catalog</li><li><strong>Adapt libraries to your requirements</strong> with our Tocriscreen PRO Custom Library Service - over 3000 compounds to choose from.</li></ul></div> </div> <div class="field_block:paragraph:2_2_media_to_text:field_call_to_action_global"> <a href="/t/compound-libraries" class="btn btn-primary" type="link"> View All Compound Libraries </a> </div> </div> </div> </div> </div> </div> </div> <div> <section class="paragraph paragraph--type--full-width-banner-with-image mb-4 paragraph--view-mode--default paragraph-background-color--"> <div class="banner_background_image" data-bgimage="https://resources.bio-techne.com/bio-techne-assets/images/banners/kinase_background_banner_new.png" style="background-repeat: no-repeat;"> <div> <div> <div> <div class="paragraph paragraph--type--_-2-text-to-media mb-4 paragraph--view-mode--default"> <div class="container-fluid container-wide"> <div class="layout layout--twocol-section layout--twocol-section--50-50"> <div class="layout__region layout__region--first"> <div class="hero-content-wrap"> <div class="field_block:paragraph:2_2_text_to_media:field_header_2_global"> <div><h2>Shed light on the kinome with confidence</h2></div> </div> <div class="field_block:paragraph:2_2_text_to_media:field_lg_sngl_frmtd_text_global"> <div><p>An expertly-curated selection of 210 kinase inhibitors targeting more than 60 kinases, including improved coverage of the dark kinome and novel targets such as Haspin and DYRK. Perfect for applications in high throughput screening, high-content screening and chemical biology.</p></div> </div> <div class="field_block:paragraph:2_2_text_to_media:field_call_to_action_global"> <a href="/p/small-molecules-peptides/tocriscreen-kinase-inhibitor_7844%20" class="btn btn-primary" type="link"> View Kinase Inhibitor 3.0 Library </a> </div> </div> </div> <div class="layout__region layout__region--second"> <div class="hero-content-wrap"> <div class="field_block:paragraph:2_2_text_to_media:field_indv_media"> <div> <img src="https://resources.bio-techne.com/bio-techne-assets/images/resources/kinase_tree_2.png" alt="Kinase Tree" loading="lazy" > </div> </div> </div> </div> </div> </div> </div> </div> </div> </div> </div> </section> </div> <div> <div class="paragraph paragraph--type--freeform mb-4 paragraph--view-mode--default"> <div><p><a name="available"></a></p></div> </div> </div> <div> <div class="paragraph paragraph--type--freeform mb-4 paragraph--view-mode--default"> <div><h2>Available Tocriscreen Bioactive Compound Libraries</h2> <figure class="responsive-figure-table"><table class="table table-bordered"> <caption>A comparison of application and format for 'off the shelf' compound libraries. Click on the product names for more information.</caption> <thead> <tr> <th> <p><strong>Product Name</strong></p> </th> <th> <p><strong>Catalog #</strong></p> </th> <th> <p><strong>Research Area/Application</strong></p> </th> <th> <p><strong>No. of Compounds</strong></p> </th> <th> <p><strong>Volume (10 mM DMSO)</strong></p> </th> </tr> </thead> <tbody> <tr> <td> <p><a href="/p/small-molecules-peptides/tocriscreen-2-0-micro_7152">Tocriscreen 2.0 Micro</a></p> </td> <td> <p>7152</p> </td> <td> <p>All Research Areas</p> </td> <td> <p>1280</p> </td> <td> <p>15 µL</p> </td> </tr> <tr> <td> <p><a href="/p/small-molecules-peptides/tocriscreen-2-0-mini_7151">Tocriscreen 2.0 Mini</a></p> </td> <td> <p>7151</p> </td> <td> <p>All Research Areas</p> </td> <td> <p>1280</p> </td> <td> <p>50 µL</p> </td> </tr> <tr> <td> <p><a href="/p/small-molecules-peptides/tocriscreen-2-0-max_7150">Tocriscreen 2.0 Max</a></p> </td> <td> <p>7150</p> </td> <td> <p>All Research Areas</p> </td> <td> <p>1280</p> </td> <td> <p>250 µL</p> </td> </tr> <tr> <td> <p><a href="/p/supplemental/tocriscreen-antiviral-library_7350">Antiviral Library</a></p> </td> <td> <p>7350</p> </td> <td> <p>Virology & Immune Response</p> </td> <td> <p>240</p> </td> <td> <p>100 µL</p> </td> </tr> <tr> <td> <p><a href="/p/small-molecules-peptides/tocriscreen-epigenetics-3-0_7578">Tocriscreen Epigenetics 3.0</a></p> </td> <td> <p>7578</p> </td> <td> <p>Epigenetics</p> </td> <td> <p>160</p> </td> <td> <p>100 µL</p> </td> </tr> <tr> <td> <p><a href="/p/small-molecules-peptides/tocriscreen-fda-approved-drugs_7200">FDA-Approved Drug Library</a></p> </td> <td> <p>7200</p> </td> <td> <p>Drug Repurposing</p> </td> <td> <p>190</p> </td> <td> <p>100 µL</p> </td> </tr> <tr> <td> <p><a href="/p/small-molecules-peptides/tocriscreen-kinase-inhibitor_7844">Kinase Inhibitor 3.0</a></p> </td> <td> <p>7844</p> </td> <td> <p>Kinases</p> </td> <td> <p>210</p> </td> <td> <p>100 µL</p> </td> </tr> <tr> <td> <p><a href="/p/small-molecules-peptides/tocriscreen-stem-cell-library_7340">Stem Cell Library</a></p> </td> <td> <p>7340</p> </td> <td> <p>Stem Cells</p> </td> <td> <p>120</p> </td> <td> <p>100 µL</p> </td> </tr> <tr> <td> <p><a href="/p/small-molecules-peptides/tocriscreen-gpcr-compound-library_8100">GPCR Library</a></p> </td> <td> <p>8100</p> </td> <td> <p>GPCRs</p> </td> <td> <p>240</p> </td> <td> <p>100 µL</p> </td> </tr> </tbody> </table></figure></div> </div> </div> <div> <div class="thin-banner banner_wrapper"> <div class="banner-dark"> <div> <div>For detailed compound lists for any of the Tocriscreen compound libraries, submit your inquiry here</div> <a href="#inquire" > <button type="button" class="btn btn-primary"> Submit Inquiry </button> </a> </div> </div> </div> </div> <div> <div class="paragraph paragraph--type--freeform mb-4 paragraph--view-mode--default"> <div><p><a name="custom"></a></p></div> </div> </div> <div> <section class="paragraph paragraph--type--full-width-banner-with-image mb-4 paragraph--view-mode--default paragraph-background-color--light"> <div class="banner_background_image" data-bgimage="" style="background-repeat: no-repeat;"> <div> <div> <div> <div class="paragraph paragraph--type--_-2-text-to-media mb-4 paragraph--view-mode--default"> <div class="container-fluid container-wide"> <div class="layout layout--twocol-section layout--twocol-section--50-50"> <div class="layout__region layout__region--first"> <div class="hero-content-wrap"> <div class="field_block:paragraph:2_2_text_to_media:field_header_2_global"> <div><h2>Tocriscreen PRO Custom Compound Libraries Service</h2></div> </div> <div class="field_block:paragraph:2_2_text_to_media:field_lg_sngl_frmtd_text_global"> <div><p>A library that always fits your needs!</p> <p>Cherry-pick from over 3,000 compounds from the Tocris catalog, and customize quantities and format to create a compound library for your exact screening requirements.</p></div> </div> <div class="field_block:paragraph:2_2_text_to_media:field_call_to_action_global"> <a href="/services/custom-compound-library-service" class="btn btn-primary" type="link"> Learn More About Custom Compound Libraries </a> </div> </div> </div> <div class="layout__region layout__region--second"> <div class="hero-content-wrap"> <div class="field_block:paragraph:2_2_text_to_media:field_indv_media"> <div> <img src="https://resources.bio-techne.com/bio-techne-assets/images/banners/tocriscreen-plate-10-update.png" alt="tocriscreen_plate" loading="lazy" > </div> </div> </div> </div> </div> </div> </div> </div> </div> </div> </div> </section> </div> <div> <div class="paragraph paragraph--type--_-3-media-to-text paragraph--view-mode--default mb-4"> <div class="container-fluid container-wide"> <div class="layout layout--twocol-section layout--twocol-section--25-75"> <div class="layout__region layout__region--first"> <div class="hero-content-wrap"> <div class="field_block:paragraph:1_3_media_to_text:field_indv_media"> <div> <a href="https://www.bio-techne.com/resources/literature/compound-libraries-product-listing" title="Download Brochure" > <img src="https://resources.bio-techne.com/bio-techne-assets/images/literature/tociscreen_literature.png" alt="A guide to the products in the Tocriscreen range of compound libaries, key product features, current research and applications in drug screening." loading="lazy" > </a> </div> </div> </div> </div> <div class="layout__region layout__region--second"> <div class="hero-content-wrap"> <div class="field_block:paragraph:1_3_media_to_text:field_header_2_global"> <div><h3>Brochure: Tocriscreen Compound Libraries</h3></div> </div> <div class="field_block:paragraph:1_3_media_to_text:field_lg_sngl_frmtd_text_global"> <div><p>Compound libraries can be used in all areas of research, for drug reprofiling, receptor de-orphaning, target validation, tool compound identification and assay development. This brochure highlights the key features and services provided as part of the Tocriscreen™ range to support your research. Featuring all of our off-the-shelf compound libraries, including Tocriscreen 2.0, a library of 1280 ready-to-use compounds, and the Tocriscreen PRO Custom Compound Library service.</p></div> </div> <div class="field_block:paragraph:1_3_media_to_text:field_call_to_action_global"> <a href="/resources/literature/compound-libraries-product-listing" class="btn btn-primary" type="link"> Download Brochure </a> </div> </div> </div> </div> </div> </div> </div> <div> <div class="paragraph paragraph--type--freeform mb-4 paragraph--view-mode--default"> <div><p><a name="applications"></a></p></div> </div> </div> <div> <div class="paragraph paragraph--type--section paragraph--view-mode--default mb-4"> <div> <div> <div class="paragraph paragraph--type--header"> <div> <div><h3> How To Use A Bioactive Compound Library</h3></div> </div> </div> </div> <div> <div class="paragraph paragraph--type--freeform mb-4 paragraph--view-mode--default"> <div><p>Bioactive compound libraries are composed of small molecules and can be used for high-throughput screening in biomedical research, medicinal chemistry and chemical biology. These screening libraries provide researchers with bioactive compounds spanning a wide range of targets or research areas, or may be focused on a particular target type, research area or application.</p> <p>Compound libraries can be used in a multitude of different assays and experimental paradigms, with differing biological outcomes and endpoints. The following sections provide examples of how compound libraries can be used for target validation, model/assay development, drug repurposing and identifying tool compounds.</p></div> </div> </div> <div> <div class="paragraph accordion mb-4 paragraph--type--extendable-paragraph paragraph--view-mode--default"> <div class="card-header rounded-top bg-white"> <a class="collapsed" data-toggle="collapse" href="#expPara-assaymodel-development23" role="button" aria-expanded="false" aria-controls="expPara"> <h5>Assay/Model Development</h5> </a> </div> <div class="collapse" id="expPara-assaymodel-development23" aria-expanded="false" aria-controls="expPara"> <div class="card-body p-4"> <br/> <div><p>When using a compound library during model or assay development, researchers aim to validate the utility of their model/assay using compounds with known action.</p> <p>The blood-brain barrier (BBB) prevents conventional chemotherapeutic agents from reaching brain tumors such as gliomas, making them very hard to treat with drugs. Traditional methods for testing BBB permeability of compounds in high throughput screening is limited to assessing radio- or fluorescently-labeled compounds passing through a monolayer cell culture. However, in most cases, this does not accurately recapitulate the physical environment of a glioma. Sherman & Rossi (2019) developed a 3D ‘BBB plus tumor’ model to allow label-free investigation of brain permeability alongside tumor toxicity. To validate this model they screened compounds from a previous version of the <a href="/p/small-molecules-peptides/tocriscreen-kinase-inhibitor_7844">Tocriscreen Kinase Inhibitor Library</a> for their cytotoxicity against LN-229 glioma spheroids alone and with the BBB model. They identified 27 compounds that showed tumor cytotoxicity in LN-229 glioma spheroids, however addition of the BBB in the 3D ‘BBB plus tumor’ model narrowed this number to 9, showing 18 compounds would not penetrate the BBB and so are unsuitable for treatment of gliomas.</p> <p><strong>Sherman & Rossi</strong> (2019) <a href="https://www.ncbi.nlm.nih.gov/pubmed/31131260" target="_blank" title="View Abstract">A novel three-dimensional glioma blood-brain barrier model for high-throughput testing of tumoricidal capability.</a> Front Oncol <strong>9</strong> PMID: 31131260</p></div> </div> </div> </div> </div> <div> <div class="paragraph accordion mb-4 paragraph--type--extendable-paragraph paragraph--view-mode--default"> <div class="card-header rounded-top bg-white"> <a class="collapsed" data-toggle="collapse" href="#expPara-drug-repurposing24" role="button" aria-expanded="false" aria-controls="expPara"> <h5>Drug Repurposing</h5> </a> </div> <div class="collapse" id="expPara-drug-repurposing24" aria-expanded="false" aria-controls="expPara"> <div class="card-body p-4"> <br/> <div><p>Drug repurposing, also known as drug repositioning, involves investigating new therapeutic uses for drugs that already have clinical approval. By leveraging validated safety and efficacy data, this process aims to bring a drug to market faster, with reduced cost. Compound libraries consisting of FDA-approved drugs are an essential starting point for drug repurposing studies.</p> <p>First identified in the early 2000s, Middle East Respiratory Syndrome is a viral respiratory disorder, caused by the MERS coronavirus (MERS-CoV), with the potential to progress into acute respiratory distress. Shin <em>et al</em> (2018) used the <a href="https://www.tocris.com/products/tocriscreen-fda-approved-drugs_7200" target="_blank">Tocriscreen FDA-approved Drugs Library</a> to identify compounds that have antiviral action against MERS-CoV in a cell-based antiviral screening assay. Huh-7 cells were infected with MERS-CoV and treated with compounds, which identified Saracatinib, a potent and selective Src tyrosine kinase family inhibitor, as having antiviral activity against MERS-CoV.</p> <p><strong>Shin</strong> <em>et al</em> (2018) <a href="https://www.ncbi.nlm.nih.gov/pubmed/29795047" target="_blank" title="View Abstract">Saracatinib inhibits Middle East Respiratory Syndrome-coronavirus replication <em>in vitro</em>.</a> Viruses <strong>10</strong> 283 PMID: 29795047</p></div> </div> </div> </div> </div> <div> <div class="paragraph accordion mb-4 paragraph--type--extendable-paragraph paragraph--view-mode--default"> <div class="card-header rounded-top bg-white"> <a class="collapsed" data-toggle="collapse" href="#expPara-identifying-tool-compounds20" role="button" aria-expanded="false" aria-controls="expPara"> <h5>Identifying Tool Compounds</h5> </a> </div> <div class="collapse" id="expPara-identifying-tool-compounds20" aria-expanded="false" aria-controls="expPara"> <div class="card-body p-4"> <br/> <div><p>Bioactive compound libraries can be used to identify compounds that enhance the efficiency of experimental techniques and processes, such as stem cell differentiation and reprogramming, and molecular biology techniques.</p> <p>CRISPR-Cas9 technology has emerged as a powerful tool for sequence-specific gene knockout through non-homologous end joining. However, the experimental process required is inefficient for the precise editing of genome sequences. Yu <em>et al</em> (2015) screened compounds from the Tocriscreen Plus Library, a precursor to <a href="/p/small-molecules-peptides/tocriscreen-2-0-max_7150">Tocriscreen 2.0 Max</a>, to identify small molecules that enhance the efficiency of CRISPR-Cas9 mediated homology-directed repair, and identified a range of compounds in diverse cell types.</p> <p>Induced pluripotent stem cells can be directed to differentiate into all cell types, and so provide an unlimited source of cells for <em>in vitro</em> disease modeling. Differentiation of pluripotent stem cells into myotubes produces myotubes with an embryonic identity, which does not accurately model skeletal disease phenotypes. Selvaraj <em>et al</em> (2019) used the <a href="/p/small-molecules-peptides/tocriscreen-stem-cell-library_7340">Tocriscreen Stem Cell Library</a> to identify compounds that would enhance the maturation of myotubes during differentiation, and found a combination of compounds that enable the generation of mature muscle constructs from pluripotent stem cells.</p> <p><strong>Selvaraj</strong> <em>et al</em> (2019) <a href="https://pubmed.ncbi.nlm.nih.gov/31710288/" target="_blank">Screening identifies small molecules that enhance the maturation of human pluripotent stem cell-derived myotubes</a>. Elife <strong>8</strong> e47970 PMID: 31710288</p> <p><strong>Yu</strong> <em>et al</em> (2015) <a href="https://www.ncbi.nlm.nih.gov/pubmed/25658371" target="_blank" title="View Abstract">Small molecules enhance CRISPR genome editing in pluripotent stem cells.</a> Cell Stem Cell <strong>16</strong> 142 PMID: 25658371</p></div> </div> </div> </div> </div> <div> <div class="paragraph accordion mb-4 paragraph--type--extendable-paragraph paragraph--view-mode--default"> <div class="card-header rounded-top bg-white"> <a class="collapsed" data-toggle="collapse" href="#expPara-target-validation1" role="button" aria-expanded="false" aria-controls="expPara"> <h5>Target Validation</h5> </a> </div> <div class="collapse" id="expPara-target-validation1" aria-expanded="false" aria-controls="expPara"> <div class="card-body p-4"> <br/> <div><p>When using a compound library for target validation, researchers aim to demonstrate that their hypothesis about a target and its involvement in a cellular or disease process is correct, by using compounds with a known target protein.</p> <p>For example, Markussen <em>et al</em> (2018) used a previous version of the <a href="/p/small-molecules-peptides/tocriscreen-kinase-inhibitor_7844" target="_self">Tocriscreen Kinase Inhibitor Library</a> to identify glycogen synthase kinase 3 (GSK3) as a negative regulator of fibroblast growth factor 21 (FGF21) in brown adipose tissue (BAT). BAT activity has beneficial metabolic functions that may have therapeutic potential in disorders such diabetes and obesity, as it is able to improve systemic insulin sensitivity and glucose homeostasis, and increase tissue oxygen consumption. This paper investigated the signaling pathways that regulate expression of <em>Fgf21</em> in BAT, and identified two GSK3 inhibitors that increased <em>Fgf21</em> expression and oxygen consumption in brown adipocytes.</p> <p>Sartori <em>et al</em> (2019) showed that expression of BIN1, a commonly identified risk factor gene for Alzheimer's disease, modulates its interaction with Tau, possibly through signaling pathways that regulate phosphorylation. To investigate these pathways further, they developed a high-throughput screening approach using primary hippocampal neurons. They tested compounds from the Tocriscreen Mini Library (a precursor of <a href="/p/small-molecules-peptides/tocriscreen-2-0-mini_7151">Tocriscreen 2.0 Mini</a>), with subsequent cellular assays for validation, and identified two compounds that modulate the BIN1-Tau interaction in neurons. This interaction has previously been shown to be inhibited by Tau phosphorylation, and both compounds identified target regulators of phosphorylation, one via calcineurin and one via the MEK-dependent signaling pathways.</p> <p>The Hippo signaling pathway exhibits regulatory cross-talk with multiple signaling networks via the transcriptional cofactor YAP. This pathway is dysregulated in many types of cancer, but how YAP is controlled in tumorigenesis is poorly understood. Yang <em>et al</em> (2019) screened compounds from a previous version of the <a href="/p/small-molecules-peptides/tocriscreen-kinase-inhibitor_7844" target="_self">Tocriscreen Kinase Inhibitor Library</a> to identify Hippo pathway regulators. They show that nerve growth factor receptor tyrosine kinase (NTRK1) regulates YAP oncogenic activity <em>in vitro</em> and <em>in vivo</em>.</p> <p><strong>Markussen</strong> <em>et al </em>(2018) <a href="https://www.ncbi.nlm.nih.gov/pubmed/29472592" target="_blank" title="View Abstract">GSK3 is a negative regulator of the thermogenic program in brown adipocytes. </a>Sci Rep <strong>22</strong> 3469 PMID:29472592</p> <p><strong>Sartori</strong> <em>et al</em> (2019) <a href="https://www.ncbi.nlm.nih.gov/pubmed/31065832" target="_blank" title="View Abstract">BIN1 recovers tauopathy-induced long-term memory deficits in mice and interacts with Tau through Thr<sup>348</sup> phosphorylation.</a> Acta Neuropathol <strong>138</strong> 631 PMID:31065832</p> <p><strong>Yang</strong> <em>et al</em> (2019) <a href="https://pubmed.ncbi.nlm.nih.gov/30542115/" target="_blank" title="View Abstract">NTRK1 is a positive regulator if YAP oncogenic function</a>. 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