compound libraries | Signalway Antibody

Approved Drug Library

(L1000)

Brief: Traditional de novo drug discovery and development involves an HTS campaign for de novo candidate hits and requires highly specialized screening facilities and compound libraries containing several million compounds.It is a time consuming and expensive process. As the regulation for drug safety and efficacy is increasingly getting complex, the cost of developing new drugs is keeping skyrocket. Drug repositioning, also known as old drugs for new uses, is an effective strategy to find new indications for existing drugs and has recently drawn attention and has led to several blockbuster drugs because of its high efficiency and low-cost. High-content screens, new biomarkers, noninvasive imaging techniques, and advanced in bioinformatics have created new opportunities for pursuing novel indications for approved compounds. Approved drugs all have known and well-characterized bioactivities, safety and bioavailability -C properties which could dramatically accelerate drug development and optimization. Hits from this set will provide a significant head start in any drug optimization program. In addition, a growing number of compounds have been identified from this library that can functionally replace reprogramming transcription factors, enhance efficiency of iPSC generation and accelerate the reprogramming process by single use or a combination of several molecules.

JAK/STAT Compound Library

(L3700)

Brief: Cell signal transductionis the transmission of molecular signals via various proteins in asignaling cascade, which carries and amplifies the signal. TheJAK-STAT signaling pathwaycommunicates information from chemical signals outside of a cell to thecell nucleus, resulting in the activation of genes through a process calledtranscription. There are three key parts of JAK-STAT signaling:Janus kinases(JAKs),Signal Transducer and Activator of Transcription proteins(STATs), and receptors (which bind the chemical signals). JAK-STAT signaling pathway is a chain of interactions between proteins in a cell, and is involved in processes such asimmunity,cell division,cell deathandtumor formation. Disrupted JAK-STAT signaling may lead to a variety of diseases, such as skin conditions,cancers, and disorders affecting the immune system. There are 4 JAK proteins:JAK1,JAK2,JAK3andTYK2, and there are 7 STAT proteins:STAT1,STAT2,STAT3,STAT4,STAT5A,STAT5BandSTAT6. JAK/STAT Compound Library from SAB, a unique collection of 145 compounds targeting JAK/STAT signaling, can be used for research in JAK/STAT signaling and related drug screening (high throughput and high content screening).

Protease Inhibitor Library

(L1100)

Brief: Protease inhibitorsaremoleculesthat inhibit the function ofproteases(enzymesthat aidthe breakdown of proteins), including proteins protease inhibitors, natural protease inhibitors, and synthetic protease inhibitors. (1). Antiprotozoal activity: protease inhibitors could be used against malaria and gastrointestinal protozoal infections; (2). Antiretrovirals: protease inhibitors were the second class of antiretroviral drugs developed widely used to treat HIV/AIDS and hepatitis C; (3). Anticancer activity: Researchers are investigating whether protease inhibitors could possibly be used to treat cancer. For example, nelfinavir and atazanavir are able to kill tumor cells in culture. Inhibitors of theproteasome, such asbortezomibare now front-line drugs for the treatment ofmultiple myeloma. Marimastat and batimastatare two of thematrix metalloproteinase inhibitorsthat can be used to treat cancer. The Protease Inhibitor Library by SAB, containing 162 small protease and proteasome inhibitors, can be used for research in Chemical Genomics and drug screening.

Epigenetics Compound Library

(L1200)

Brief: Epigenetics is the study of molecular processes that influence the flow of information between a constant DNA sequence and variable gene expression patterns. This includes investigation of nuclear organization, DNA methylation, histone modification and RNA transcription. Epigenetic processes can result in intergenerational (heritable) effects as well as clonal propagation of cell identity without any mutational change in DNA sequence. Epigenetics has the potential to be a key element in a paradigm change of our understanding of aging, development, cancer, heart disease, psychological disorders, and other diseases. For example, Epigenetic modifications have a considerable effect on cancer. Changes in the pattern of histone modificationsin the promoter sequences as epigenetic regulation lead to changes in chromatin structure thus may be the cause of altered gene expression by activation of oncogenes. The Epigenetics Compound Library by SAB, containing 380 compounds related to epigenetic regulation, can be used for research in epigenetics, high throughput screening and high content screening for new drugs in epigenetic modification

PI3K/Akt/mTOR Compound Library

(L1300)

Brief: ThePI3K/AKT/mTOR pathwayis an intracellular signaling pathway important in regulating thecell cycle. Therefore, it is directly related to cellularquiescence,proliferation,cancer, and longevity. Phosphatidylinositol 3-kinase (PI3K), AKT, a serine/threonine protein kinase also known as protein kinase B (PKB), and mammalian target of rapamycin (mTOR) are 3 major nodes in the pathway. PI3Kactivationphosphorylatesand activatesAKT, localizing it in theplasma membrane.AKT can have a number of downstream effects such as activatingCREB,inhibitingp27,localizingFOXOin the cytoplasm,activatingPtdIns-3ps,and activatingmTORwhich can affect transcription of p70 or 4EBP1. mTOR is a component of the PI3K/AKT cell survival pathway that monitors the availability of nutrients, mitogenic signals and cellular energy and oxygen levels, a major regulator of the autophagic process, and alterations in components of the mTOR pathway have a major role in tumor progression. Therefore, mTOR is an appealing therapeutic target in many tumors. Encouraging data from preclinical studies have offered new opportunities to fully exploit the therapeutic potential of mTOR targeting in cancer. The PI3K/Akt/mTOR Compound Library by SAB, containing 190 compounds targeting PI3K/Akt/mTOR signaling, can be used for high throughput screening and high content screening for new drugs.

MAPK Inhibitor Library

(L1400)

Brief: Mitogen-activated protein kinases (MAPKs) are a highly conserved family of serine/threonine protein kinases involved in a variety of fundamental cellular processes such as proliferation, differentiation, motility, stress response, apoptosis, and survival.A broad range of extracellular stimuli including mitogens, cytokines, growth factors, and environmental stressors stimulate the activation of one or more MAPKK kinases (MAPKKKs) via receptor-dependent and -independent mechanisms. MAPKKKs then phosphorylate and activate a downstream MAPK kinase (MAPKK), which in turn phosphorylates and activates MAPKs. The MAPK Inhibitor Library by SAB, containing 140 compounds targeting MAPK signaling, can be used for research in MAPK signaling, and drug screening for related diseases

GPCR Compound Library

(L1500)

Brief: G-protein-coupled receptors(GPCRs) are the largest and most diverse group of membrane receptors in eukaryotes that detectmoleculesoutside thecelland activate internalsignal transductionpathways and, ultimately, cellular responses.GPCRs are involved in nearly every aspect of animal life, from early development and heart function to neuronal activity. Mutations in GPCRs are linked to a number of human diseases. GPCRs are an important drug target and approximately 34%of the marketed drugs target 108 members of this family, with an additional 66 receptors targeted by agents that are/were in clinical trials.GPCR-based drug discovery remains active campaigns in major pharmaceutical companies. To date more than 140 orphan GPCRs, whose endogenous ligands are unknown, are the focus of an intense drug discovery effort in many programs. Specifically, the optimal ligands to GPCRs need to possess high affinity and specificity for the target protein, and reasonable membrane permeability for biological activity in whole cell assays and in vivo models. GPCR Compound Library from SAB, a focused small molecule libraries developed against particular GPCRs containing 730 GPCR-active agents for GPCR drug discovery

Nuclear-receptor inhibitors library

(L1510)

Brief: Nuclear receptorsare a class ofproteins, different from membrane receptors located in the cell membrane,found within cells that are responsible for sensingsteroidandthyroidhormonesand certain other molecules.Nuclear receptors have the ability to directly bind toDNAand regulate the expression of adjacent genes, hence these receptors are classified astranscription factors, thereby controlling thedevelopment,homeostasis, andmetabolism of the organism. Over the last 15 years a growing number of nuclear receptors have been identified that coordinate genetic networks regulating lipid metabolism and energy utilization andunderlie the pathogenesis of metabolic diseases, such as obesity, type II diabetes, hypertension, and cardiovascular disease. SAB collects 239 reported compounds targeting nuclear receptors as Nuclear Receptor Compound Library, which can be used for research in nuclear receptor signaling and related diseases, and high throughput and high content screening for drug discovery

Kinase Inhibitor library

(L1600)

Brief: In biochemistry, a kinase is an enzyme that catalyzes the transfer of phosphate groups from high-energy, phosphate-donating molecules (ATP) to specific substrates. This process is known as phosphorylation. The protein kinases make up the majority of all kinases and are widely studied. Aprotein kinasemodifies other molecules, mostly proteins, by phosphorylation to regulate the majority of cellular pathways, especially those involved insignal transduction. Various other kinases act on small molecules such aslipids,carbohydrates,amino acids, andnucleotides, either for signaling or to prime them for metabolic pathways. SABs Kinase Inhibitors Library, containing 900 kinase inhibitors, can be used for research in chemical genomics, pharmacological study, and drug screening for related diseases

Anti-virus Compound library

(L1700)

Brief: Virus is a small infectious agent thatreplicatesonly inside the livingcellsof otherorganisms through various pathways, and causes the damage to the host cells. Common diseases caused by virus include smallpox, the common cold, chickenpox, influenza, shingles, hanta fever, herpes, etc. AIDS, polio, and Ebola are examples of life threatening serious viral diseases caused by HIV, poliovirus, and Ebola virus, respectively. The anti-virus compound library from SAB contains 157 compounds with anti-virus bioactivity, and is an appropriate tool for drug repurposing for new anti-virus drug discovery based on the fact that these viruses rely on common host cellular mechanisms to promote discrete stages of their life cycles