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RNA Targeted Library

RNA Targeted LibraryThe recent substantial progress in RNA biology underscores the importance of RNA in normal and aberrant cellular functions. Rather, it is now recognized that RNA is essential for transcriptional regulation, translational regulation, protein function, and catalysis, responsibilities that have classically been reserved for proteins.

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Natural Product-Like Library
Natural Product-Like LibraryNatural Product-Like Library has been designed as a special screening library containing synthetic compounds similar to natural.
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PARP1 Focused Library

PARP1 Focused Library Poly [ADP-ribose] polymerase 1 (PARP-1) also known as NAD+ ADP-ribosyltransferase 1 or poly[ADP-ribose] synthase 1 is an enzyme that modifying nuclear proteins by poly ADP-ribosylation. PARP1 is involved in modulating DNA repair, DNA replication, transcription, DNA methylation and chromatin remodeling through PARylation of downstream proteins. Also it is involved in differentiation, proliferation, tumor transformation and may participate in the pathophysiology of type I diabetes [1, 2].

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iPPI Focused Libraries

Protein-Protein Interaction Focused LibrariesTargeting protein protein interaction (PPI) is a new challenge to current drug discovery. Due to growing interest in PPI inhibitors we represent focused compound libraries covering chemical space of PPI inhibitors.

 

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Calcium Channel Blockers

Calcium Channel Blockers focused libraryCalcium channel blockers (CCBs) disrupt the movement of calcium (Ca2+) through calcium channels. They are used as antihypertensive drugs, i.e., as medications to decrease blood pressure in patients with hypertension. CCBs are particularly effective against large vessel stiffness, one of the common causes of elevated systolic blood pressure in elderly patients.

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Kv1.5 Potassium Channel Blockers

Kv1.5 Potassium Channel BlockerAtrial fibrillation is the most common sustained cardiac rhythm disorder, and confers a substantial mortality and morbidity from stroke, thromboembolism, heart failure, and impaired quality of life. With the increasingly elderly population in the developed world, the prevalence of atrial fibrillation is increasing, resulting in a major public-health problem.

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HCN Channel Blocker Library

HCN Channel BlockerThe current produced by hyperpolarization-activated cyclic nucleotide-gated (HCN) channels (termed If, cardiac pacemaker “funny” current, and Ih in neurons) is also considered a “pacemaker current” because it plays a key role in controlling the rhythmic activity of cardiac pacemaker cells and spontaneously firing neurons.

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Solubility Fragment Library

Solubility Fragment Library

The Solubility Fragment Library consists of about 1,000 low molecular fragments with "Rule-of-Three" compliance and assured solubility in both DMSO (200mM) and PBS buffer (1mM). The library design included diversity filtering in order to provide chemical structure variety for your fragment screening program.
 
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CREBBP focused library

CREBBP focused libraryCREB binding protein (CREBBP) is a coactivator of transcription factor CREB that activates genes in cAMP transcriptional pathway. The coactivator binds to transcription factor activation domains positions histone acetyltransferases near specific nucleosomes in target gene promoter regions, recognizing the acetylated lysine residue.

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Halogen-Enriched Fragments

Halogen-Enriched Fragment LibraryOur Halogen-Enriched Fragment Library comprises 618 brominated fragments that can explore binding sites for favorable halogen bond interactions to identify unique binding modes that are complementary to those obtained from classical fragment-based screening.
 

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SGLT2 Focused Library

Sodium Glucose Cotransporter 2 Focused Library

The sodium glucose cotransporter 2 (SGLT2) reabsorbs most of the glucose filtered by the kidneys. SGLT2 inhibitors reduce glucose reabsorption, thereby lowering blood glucose levels in patients with diabetes [1]. Type 2 diabetes is a chronic disease with disabling micro- and macrovascular complications that lead to excessive morbidity and premature mortality.

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Peptidomimetic Libraries

Peptidomimetic LibrariesThe interaction of proteins are critical to nearly all biological processes, including cellular signaling [1]. We offer special screening Peptidomimetic Libraries: β-Turn Peptidomimetic Library containing synthetic compounds which mimic beta-turns of proteins and a-Helix Peptidomimetic Library of compounds mimic alpha-helixes of proteins. These libraries are intended for research and drug discovery projects focused on protein-protein interactions.

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DPP4 Focused Library

DPP4 Focused LibraryDipeptidyl peptidase-4 (DPP4), also known as adenosine deaminase binding protein or cluster of differentiation 26 (CD26), is a serine exopeptidase able to recognizes an amino acid sequence having proline at the N-terminal penultimate position and inactivate this oligopeptides through the removal of N-terminal proline dipeptides [1, 2].

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HMG-CoA Reductase Library

HMG-CoA focused libraryThe enzyme 3-hydroxy-3-methyl-glutaryl-CoA reductase (3-hydroxy-3-methylglutaryl-coenzyme A, HMG-CoA, HMGCR) catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis. The HMG-CoA reductase inhibitors, also known as statins, are the most effective class of drugs for lowering serum low-density lipoprotein cholesterol concentrations.

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Hsp90 Focused Library

Hsp90 focused libraryHsp90 (heat shock protein 90) is a highly abundant and ubiquitous molecular chaperone which plays an important role in the folding of newly synthesized proteins or stabilizing and refolding denatured proteins after stress. Its expression is associated with many types of tumors including breast cancer, pancreatic carcinoma, human leukemia and others.

 

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Glycomimetics Focused Library

Glycomimetics Focused LibrarySeveral glycoprocessing enzymes and glycoreceptors have been recognized as important targets for therapeutic intervention. This concept has inspired the development of important classes of therapeutics, such as anti-influenza, anti-inflammatory, Gaucher’s disease, hepatitis and cancer drugs.

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GCR Antagonist Library

Glucocorticoid Receptor Antagoniat focused libraryGlucocorticoids (GCs) are secreted from the adrenal gland in response to exposure to emotional and physiologic stressors and are responsible for modulating essential metabolic, cardiovascular, immune, and behavioral functions [1–3]. The glucocorticoid receptor (GR) belongs to a family of nuclear hormone receptors that are ligand-dependent transcription factors.

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11β-HSD1 Focused Library

11beta-hydroxysteroid dehydrogenase type I focused library11β-hydroxysteroid dehydrogenase type I (11β-HSD1, cortisone reductase, HSD11B1, 11beta-hydroxysteroid dehydrogenase type I,11beta-HSD1) is an enzyme that is involved in glucocorticoid regulation by catalyzing the conversion of inactive cortisone to its active form cortisol. These hormones regulate several physiological processes, and modulation of glucocorticoid action has been implicated as a potential treatment for a variety of diseases.

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Histamine Receptor library

Histamine receptor focused libraryIt is generally acknowledged that histamine is an important regulator of a plethora of (patho) physiological conditions and exerts its actions through the interaction with four histamine receptor subtypes. All these receptors belong to the family of heptahelical GPCR's and are considered as a promising molecular targets for drug development.

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HATs Focused Library

Histone Acetyltransferase target-focused libraryPost-translational modifications, such as acetylation or phosphorylation, play a crucial role in the regulation of gene transcription in eukaryotes. Different subtypes of histone acetyltransferases (HATs) catalyze the acetylation of histones on specific lysine residues. 

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