compound libraries · 4 chemical genomics available libraries: chemical genomics bml-2840 iccb...

COMPOUND LIBRARIES

Chemical GenomicsICCB Known Bioactives

Kinase InhibitorsPhosphatase Inhibitors

Protease InhibitorsIon Channel Ligands

Receptor De-orphaningBioactive Lipids

EndocannabinoidsFatty Acids

NeurotransmittersNuclear Receptor Ligands

Orphan Ligands

Drug Repurposing FDA Approved Drug Library

Natural ProductsNatural Products

Rare Natural Products

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www.enzolifesciences.com

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ENZO LIFE SCIENCES, INC.

Enzo Life Sciences, Inc. is a subsidiary of Enzo Biochem, Inc. organ-ized to lead in the development, production, marketing, and sales of innovative life science research reagents worldwide based on over 30 years of successful experience in building strong international market recognition, implementing outstanding operational capabili-ties, and establishing a state-of-the-art electronic information and ordering marketplace.

Enzo Life Sciences, Inc. is a recognized leader in labeling and de-tection technologies across research and diagnostic markets. A strong portfolio of labeling probes and dyes provides life science environments with tools for target identifi cation/validation and high content analysis via gene expression analysis, nucleic acid detec-tion, protein biochemistry and detection, molecular biology, and cellular analysis.

Now incorporating the skills, experience and products of ALEXIS® Biochemicals, acquired in 2007, and BIOMOL® International, ac-quired in 2008, the Enzo® Life Sciences brand now provides 25 years of business experience in the supply of research biochemi-cals and biologicals “Enabling Discovery in Life Science™”.

• Genomic Analysis • Cellular Analysis

• Post-translational Modification • Signal Transduction

• Cancer & Immunology • Drug Discovery

In addition to our wide range of catalog products, a full range of highly specialized custom services are also offered to provide tailor-made solutions for researchers, including peptide synthesis, anti-body production, protein expression, organic synthesis and cus-tom-labeled FISH probes. Industry-wide there is an unmet demand for such expertise on a custom/contract basis.

International Edition 04/2009

Enabling Discovery in Life ScienceTM

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International Edition

Chemical Genomics

ICCB Known Bioactives 5

Kinase Inhibitors 6

Phosphatase Inhibitors 6

Ion Channel Ligands 7

Protease Inhibitors 7

Receptor De-orphaning

Bioactive Lipids 9

Endocannabinoids 9

Neurotransmitters 10

Orphan Ligands 10

Fatty Acids 11

Nuclear Receptor Ligands 11

Drug Repurposing

FDA Approved Drug Library 12

Natural Products

Natural Products 13

Rare Natural Products 14

International Distributors

Content

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8

12

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Chemical Genomics Chemical Genomics

Available libraries:

Chemical GenomicsBML-2840 ICCB Known Bioactives Library – 480 compounds of known biological activity BML-2832 Kinase Inhibitor Library – 80 kinase inhibitorsBML-2834 Phosphatase Inhibitor Library – 33 phosphatase inhibitors BML-2805 Ion Channel Ligand Library – 72 ion channel agonists and antagonists BML-2833 Protease Inhibitor Library – 53 protease inhibitors

Receptor de-orphaningBML-2800 Bioactive Lipid Library – 200 bioactive lipids ideal for screening or identifying recombinant receptors BML-2801 Endocannabinoid Library – 60 compounds with defined, putative, potential or speculative activity at cannabinoid (CB) receptors and TRPV channels BML-2802 Nuclear Receptor Ligand Library – 76 compounds with defined and potential activity at nuclear receptors BML-2803 Fatty Acid Library – 68 fatty acids of various chain length and saturationBML-2825 orphan Ligand Library – 84 compounds with biological activity but no known receptor BML-2810 Neurotransmitter Libraries – 700 neurotransmitters on 10 plates according to receptor class

Drug repurposingBML-2841 FDA Approved Drug Library – 640 FDA Approved Drugs

Natural productsBML-2865 Natural Product Library – 502 known natural productsBML-2866 Rare Natural Product Library – 84 known natural products whose supply may be limited

SCREEN-WELL™ LIBRARIES • Focused collections of known actives• Dissolved in biocompatible solvents• Ready-to-screen• In stock for rapid delivery• Compounds available for resupply

The Enzo Life Sciences Screen-Well™ libraries are focused collections of compounds ideal for receptor de-orphaning, assay development and chemical genomics. Each compound is dissolved in 100 or 500 μl of DMSO and aliquotted to a 96-well plate. This format, together with the focus of each library on a defi ned group of compounds makes the Screen-Well™ librar-ies convenient and cost-effective collections of compounds suitable for individual assays or high-throughput screening. Each library includes supporting data and a structure fi le for incorporating into your database. All compounds are available individu-ally for resupply.

Focused collections of known actives Dissolved in biocompatible solvents

Compounds available for resupply

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Chemical Genomics 5 Chemical Genomics


Chemical genomics (or chemical genetics or chemical biology) uses target-specific chemical ligands to modulate and under-stand the cellular or physiological function of all proteins. Small molecule modulation of cell function offers the advantages of temporal and spatial control not easily achieved with traditional molecular genetic approaches and can provide a first step to-ward the development of new therapeutic agents. While synthesis of new chemical entities is one aspect of chemical genom-ics, the development of new sophisticated screens employing proteomics and noninvasive imaging techniques has allowed new functions to be ascribed to well-characterized small molecules. In addition, the development of new assays for chemical genomics approaches requires characterization and testing using standard sets of known actives. Enzo Life Sciences offers a growing selection of libraries designed to meet your chemical genomics screening needs.

ICCB Known Bioactives Library• 480 compounds with defined biological activity• Ready-to-screen

Enzo Life Sciences has created a novel library of biologically ac-tive small organic molecules in cooperation with the Harvard Institute of Chemistry and Cell Biology (ICCB; now the Broad In-stitute Chemical Biology Program (BCBP) and ICCB-Longwood). Known active compounds are indispensable tools for target vali-dation, biological mechanism profiling and assay validation. The ICCB Known Bioactives Library serves as a widely used standard set of actives for high content screening.

DMSO solutions (concentrations vary) 6 x 96-well plates

Activity descriptions, plate positions, physical information, and a structure database (SD) file for integration into your compound database.

Inquire with [email protected] for a compound list and ordering information

CytoskeletonApoptosis

Nitric oxide and free radicalsEndocannabinoids

Phosphodiesterase inhibitors

CNS ligands

Protease inhibitors

Gene regulation, chromatin,

DNA metabolism

Nuclear receptor ligands

Lipid biosynthesis

Miscellaneouscell signaling

Phosphorylation

Ion channel modulators

Bioactive lipids

Distribution of pharmacological activities in the ICCB Known Bioactives Library

Includes compounds that affect most cellular processes and drug targets:

GPCR ligands Second messenger modulators

Nuclear receptor ligands Actin & tubulin modulators

Kinase inhibitors Protease inhibitors

Ion channel blockers Gene regulation agents

Lipid biosynthesis inhibitors Phosphodiesterase inhibitors

. . . many other classes

Product Compounds Prod. No. Size

ICCB Known Bioactives Library 480 BML-2840-0100 100 ml/well

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Chemical Genomics Chemical Genomics

Kinase Inhibitor Library• An important tool for phosphorylation research• 80 known kinase inhibitors • Ready-to-screen

The Screen-Well™ Kinase Inhibitor Library contains 80 known kinase inhibitors of well-defi ned activity. The library is ideal for chemical genomics, assay development or as a reference set for secondary screening.

FORMAT SUPPORTING INFORMATION

10 mM DMSO solutions1 x 96-well plate



Phosphatase Inhibitor Library• 33 known phosphatase inhibitors • An important tool for phosphorylation research• Ready-to-screen

The Screen-Well™ Phosphatase Inhibitor Library contains 33 known phosphatase inhibitors of well-defi ned activity. The li-brary is ideal for chemical genomics, assay development and as a reference set for secondary screening.





Includes inhibitors of these important kinases:

BTK Insulin receptor PDGFR

CaM Kinase II JAK PKA

CDK JNK PKC

CKI & II MAPK RAF

EGFR MEK SAPK

GSK MLCK Src-family

IKK PI 3-Kinase VEGFR

. . . and more

Includes inhibitors of these important phosphatases:

Calcineurin (PP2B) JSP-1 PRL-1

CD45 PP1 PRL-3

CDC25 PP2A PTEN

. . . and more


Kinase Inhibitor Library 80 BML-2832-0100 100 ml/well

Kinase Inhibitor Library 80 BML-2832-0500 500 ml/well


Phosphatase Inhibitor Library 33 BML-2834-0100 100 ml/well

Phosphatase Inhibitor Library 33 BML-2834-0500 500 ml/well

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Chemical Genomics 7 Chemical Genomics


Ion Channel Ligand Library• 72 ligands in a 96-well format• Antagonists & agonists• Ready-to-screen

The Screen-Well™ Ion Channel Ligand Library contains 72 ion channel agonists and antagonists of well-defined activity. The library is ideal for chemical genomics, assay develop-ment or as a reference set for secondary screening.


10 mM DMSO solutions 1 x 96-well plate


Inquire with [email protected] for a compound list and ordering information*A second ion channel ligand plate is in development. Inquire for details.

Protease Inhibitor Library• An important tool for protease research• 53 known protease inhibitors • Ready-to-screen

The Screen-Well™ Protease Inhibitor Library contains 53 known protease inhibitors of well-defined activity. The library is ideal for chemical genomics, assay development and as a reference set for secondary screening.





Includes modulators of the following ion channel classes:

Calcium channels Potassium channels

Chloride channels Sodium channels

. . . and more

Includes inhibitors of these important proteases:

ACE DPPIV Neutrophil elastase

Aminopeptidase B Furin Proteasome

Calpains Granzyme B g-Secretase

Caspases Kallikrein Thrombin

Cathepsins MMPs TPPII

. . . and more


Protease Inhibitor Library 53 BML-2833-0100 100 ml/well

Protease Inhibitor Library 53 BML-2833-0500 500 ml/well


Ion Channel Ligand Library 72 BML-2805-0500 500 ml/well


8Receptor De-orphaningReceptor De-orphaningThe Enzo Life Sciences Screen-Well™ libraries are ideal tools for receptor de-orphaning approaches. The Screen-Well™ li-braries for receptor de-orphaning include plates of bioactive lipids, endocannabinoids, fatty acids, neurotransmitters, nuclear receptor ligands, and orphan ligands, compounds with defi ned or speculative biological activity but whose binding partner has not been identifi ed. Each compound is dissolved in a biocompatible solvent and aliquotted to a 96-well plate. This format, together with the focus of each library on a defi ned group of ligands, make the Screen-Well™ libraries convenient and cost-effective collections of related compounds suitable for performing individual assays or high-throughput screening.

The human genome project revealed over 207 novel GPCRs for which endogenous ligands remained to be identifi ed. 86 of these receptors have been de-orphaned over the last 15 years1 revealing a great deal of interesting biology. Many of the com-pounds recently identifi ed as ligands for orphan receptors are contained in the Enzo Life Sciences Screen-Well™ Libraries (see table). In addition to matching many ligands with known biological activity, such as melanin concentrating hormone2,3 or urotensin II4,5, to orphan GPCRs, the reverse pharmacology approach has identifi ed at least fi ve novel peptide families6. Characterization of these new peptide hormones has identifi ed new signaling systems that regulate hormone release, immune responses in neonates, feeding, sleep and other behavioral responses6. Several lipids, including sphingosine-1-phosphate, lysophosphatidic acid, sphingosylphosphorylcholine and lysophosphatidylcholine, previously thought to act as intracellular second-messengers, have been identifi ed as extracellular ligands for orphan GPCRs7,8. In addition, this approach has identi-fi ed a few novel neurotransmitters such as UDP-glucose9 and the biogenic amine tyramine10 raising the possibility that meta-bolic intermediates might be an under-investigated source of signaling molecules.

Ligands of recently de-orphaned GPCRs found in Enzo Life Sciences Screen-Well™ Libraries

Orphan Receptor(s) Ligand Function Library Ref.

ORL-1 Nociceptin/Orphanin FQ Pain, Anxiety, Memory BML-2814 11,12

OGR-1 Sphingosylphosphorylcholine Proliferation BML-2800 13

HG57(Cys-LT1R) Leukotriene D4

Bronchial constriction BML-2800 14

PSECO146 (Cys-LT2R) Leukotriene C4, D

4Bronchial constriction BML-2800 15,16

BLT1,2 Leukotriene B4

Bronchial constriction BML-2800 17-20

Edg1,3,5,6,8 Sphingosine-1-phosphate Cell differentiation, growth BML-2800 21-25

Edg2,4,7 Lysophosphatidic Acid Cell differentiation, growth BML-2800 26-29

TA1, TA2 Trace Amines (tyramine) Unknown BML-2825 10

CRTH2 Prostaglandin D2

Vasodilation, immunity, sleep BML-2800 30

GPR3,6,12 Sphingosine-1-phosphate Cell differentiation, growth BML-2800 31

TG1019/OXE 5-Oxo-ETE (5-KETE) Eosinophil activation BML-2800 32

GPR40 Fatty acids Insulin secretion BML-2803 33

GPR119 Oleoylethanolamide Satiety BML-2800 34

GPR18 N-Arachidonylglycine Unknown BML-2800 35

G2A 9-HODE Lymphocyte homeostasis BML-2800 36

GPR35 Kynurenic acid Unknown BML-2817 37

GPR109B D-Phenylalanine Leukocyte chemoattractant BML-2825 38

REFERENCES: [1] D.Y. Oh; Int. Rev. Cytol. 252,163 (2006) [2] Y. Saito et al.; Nature 400, 265 (1999) [3] Y. Shimomura et al.; BBRC 261, 622 (1999) [4] H. P. Nothacker et al.; Nature Cell Biol. 1, 383 (1999) [5] M. Mori et al.; BBRC 265, 123 (1999) [6] O. Civelli; Trends Neurosci. 24, 230 (2001) [7] T. Hla; Science 294, 1781 (2001) [8] E. Kostenis; Pharmcol. Ther. 102, 243 (2004) [9] J. K. Chambers et al.; J. Biol. Chem. 275, 10767 (2000)[10] B. Borowsky et al.; PNAS 98, 8966 (2001)[11] R. K. Reinscheid et al.; Science 270, 792 (1995)[12] J. C. Meunier et al. Nature 377, 532 (1995)[13] Y. Xu et al.; Nat. Cell Biol. 2, 261 (2000)[14] K. R. Lynch et al.; Nature 399, 789 (1999)[15] C. E. Heise et al.; J. Biol. Chem. 275, 30531 (2000)[16] H.P. Nothacker et al.; Mol. Pharmacol. 58, 1601 (2000)[17] Y. Tryselius et al.; BBRC 274, 377 (2000)[18] M. Kamohara et al.; J. Biol. Chem. 275, 27000 (2000)[19] S. Wang et al.; J. Biol. Chem. 275, 40686 (2000)

[20] M. J. Lee et al.; Science 279, 1552 (1998)[21] J. R. Van Brocklyn et al.; J. Biol. Chem. 274, 4626 (1999)[22] Y. Yamazaki et al.; BBRC 268, 583 (2000)[23] H. Okamato et al.; BBRC 260, 203 (1999)[24] S. An et al.; J. Biol. Chem. 275, 288 (2000)[25] D. S. Im et al.; J. Biol. Chem. 275, 14281 (2000)[26] D. S. Im et al.; Mol. Pharmacol. 57, 57 (2000)[27] N. Fukushima et al.; PNAS 95, 6151 (1998)[28] J. R. Erickson et al.; J. Biol. Chem. 273, 1506 (2000)[29] S. An et al.; J. Biol. Chem. 273, 7906 (2000)[30] H. Hirai et al.; J. Exp. Med. 193, 255 (2001)[31] K. Uhlenbrock et al.; Cellular Signaling 14, 941 (2002)[32] T. Hosoi et al.; J. Biol. Chem. 277, 31465 (2002)[33] C.P. Brisco et al.; J. Biol. Chem. 278, 11303 (2003)[34] H. Overton et al.; Cell Metab. 3, 167 (2006)[35] M. Kohno et al.; Biochem. Biophys. Res. Commun. 347, 827 (2006)[36] H. Obinata et al.; J. Biol. Chem. 280, 40676 (2005)[37] J. Wang et al.; J. Biol. Chem. 281, 22021 (2006)[38] Y. Irukayama-Tomobe et al.; PNAS 106, 3930 (2009)

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Receptor De-orphaning 9Receptor De-orphaning


Bioactive Lipid Library• 201 bioactive lipids in a 96-well format• Useful for receptor de-orphaning • Ready-to-screen

Contains 201 bioactive lipids aliquotted to 3 x 96-well plates. Ideal for screening or identifying orphan G protein-coupled receptors (GPCRs) and nuclear receptors. Also useful for receptor de-orphaning, assay development, secondary screening and other pharmacological applications.


1.0 or 0.1 mM DMSO solutions (depending on compound) 3 x 96-well plates

Physical information, plate positions, and a structure database (SD) file for integration into your compound database.

Inquire with [email protected] for a compound list and ordering information*An additional plate of bioactive lipids is in development. Inquire for details.

Endocannabinoid Library• 60 compounds with defined or potential

activity at cannabinoid receptors• Useful for receptor de-orphaning• Ready-to-screen

The Screen-Well™ Endocannabinoid Library contains 60 compounds with defined, putative, potential or speculative activity at cannabinoid (CB) receptors and TRPV channels. The library is an array of 10 different fatty acids and 6 differ-ent polar head groups. The library is a source of known and novel compounds for receptor de-orphaning, assay develop-ment and as a reference set for secondary screening.





Library includes:

Agonists & antagonists LPA & phosphatidic acids

Cannabinoids Octadecanoids

Farnesyl/geranylgeranyl derivatives

PAFs

HETEs, deHETEs and hepoxilins Prostaglandins & thromboxanes

Polyunsaturated fatty acids Retinoids and vitamin D metabolites

Leukotrienes and lipoxins Sphingolipids

. . . and more

Library includes:

Acyl-dopamines Ethanolamides

Acyl-GABAs Lipo-amino acids

Amides

. . . and more


Bioactive Lipid Library 201 BML-2800-0100 100 ml/well

Bioactive Lipid Library 201 BML-2800-0500 500 ml/well


Endocannabinoid Library 60 BML-2801-0500 500 ml/well


10Receptor De-orphaningReceptor De-orphaning

Neurotransmitter Library• 650 neurotransmitters and drugs• 13 classes of neurotransmitters in 10 deep

well plates • Ready-to-screen

Contains >650 CNS receptor ligands, including endogenous neurotransmitters, agonists, antagonists and marketed drugs in a 96-well format. The library is ideal for screening orphan G protein-coupled receptors, target validation, secondary screening, assay development, and for other pharmacological applica-tions. The library contains 13 classes of ligands in 10 deep-well plates. Plates are available individually or as a complete set.


10 mM DMSO solutions (a few compounds are supplied in H2O)10 x 96-well plates (available individually or as a complete set)


Inquire with [email protected] for compound lists and ordering information* The libraries are regularly updated with the latest ligands and the # of compounds is subject to change. Inquire for details.

Orphan Ligands• 84 potential receptor ligands• Useful for receptor de-orphaning

Contains 84 compounds with defi ned, putative, potential or speculative activity but whose protein binding partners have not been identifi ed. The library is a rich source of potential ligands for receptor de-orphaning.



Physical information, descriptions, plate positions, and a structure database (SD) file for integration into yourcompound database.

Inquire with [email protected] for compound lists and ordering information

Library includes:

D-Amino acid derivatives Nicotine congeners

Endogenous β-carbolines Urinary metabolites

Neurotransmitter metabolites Endo-Alkaloids

Novel Actives . . . and more

Library includes the following plates of neurotransmitters:

Adrenergics Metabotropic glutamatergics

Cholinergics Histaminergics (& melatonin ligands)

Dopaminergics Opioids (& sigma ligands)

GABAergics Purinergics

Ionotropic glutamatergics Serotonergics


Orphan Ligand Library 84 BML-2825-0500 500 ml/well

Product Compounds* Prod. No. Size

Neurotransmitter Library (10-plate set) >650 BML-2810-0500 500 ml/well

Adrenergics 84 BML-2811-0500 500 ml/well

Dopaminergics 81 BML-2812-0500 500 ml/well

Serotonergics 83 BML-2813-0500 500 ml/well

Opioids (& Sigma Ligands) 79 BML-2814-0500 500 ml/well

Cholinergics 74 BML-2815-0500 500 ml/well

Histaminergics (& Melatonin Ligands) 42 BML-2816-0500 500 ml/well

Ionotropic Glutamatergics 64 BML-2817-0500 500 ml/well

Metabotropic Glutamatergics 56 BML-2818-0500 500 ml/well

GABAergics 58 BML-2819-0500 500 ml/well

Purinergics (& Adenosines) 52 BML-2820-0500 500 ml/well

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Receptor De-orphaning 11Receptor De-orphaning


Fatty Acids• 68 fatty acids of various chain length

and saturation• Useful for receptor de-orphaning,

inhibitor and high content screening• Ready-to-screen

The Screen-Well™ Fatty Acid Library contains 68 fatty acids of varying saturation and chain length. Many free fatty acids and their metabolites serve as precursors to important signaling systems (e.g. prostaglandins), act directly as receptor ligands or enzyme inhibitors, and have pro- or anti-atherosclerotic and anti-hypertensive properties through mechanisms that are still being characterized. Therefore, a diverse set of fatty acids can be a rich source of compounds for receptor de-orphaning, inhibitor screening, and high content screening. This set contains both fatty acids with defined activities and fatty acids with putative biological activities.





Nuclear Receptor Ligands• 76 known nuclear receptor ligands• Useful for de-orphaning nuclear receptors• Ready-to-screen

The Screen-Well™ Nuclear Receptor Ligand Library contains 76 compounds with defined, putative and potential activity at nuclear receptors. Receptor agonists and antagonists are in-cluded. The library is an ideal tool for receptor de-orphaning, assay development and other pharmacological applications.





Library includes ligands for the following receptors:

AHR ER LXR PXR RXR

CAR FXR PPAR RAR VDR

...and other steroid receptors

Library includes:

Unsaturated & saturated fatty acids Arachidonic acid

C10-24 chain length Linolenic acid

E and Z isomers g-Linolenic acid

. . . and more


Nuclear Receptor Ligand Library 76 BML-2802-0100 100 ml/well

Nuclear Receptor Ligand Library 76 BML-2802-0500 500 ml/well


Fatty Acid Library 68 BML-2803-0100 100 ml/well

Fatty Acid Library 68 BML-2803-0500 500 ml/well

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Drug RepurposingDrug Repurposing


FDA Approved Drug Library 640 BML-2841-0100 100 ml/well

FDA Approved Drug Library 640 BML-2841-0500 500 ml/well

FDA Approved Drug Library• 100% known bioactivity• Greatest degree of drug-likeness available• Known safety & bioavailability• Compounds available individually and in bulk for resupply

The Enzo Life Sciences FDA Approved Drug Library contains 640 FDA approved drugs, carefully selected to maximize chemical and pharmacological diversity. The library contains clinically-relevant pharmacophores for SAR or toxicity studies and provides an ideal starting point for drug repurposing or repositioning programs.


2 mg/ml DMSO solutions8 x 96-well plates


Inquire with [email protected] for compound lists and ordering information

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Drug Repurposing:

In addition to classic methods of drug discovery, drug repositioning or repurposing can be an important supplemental pathway for the discovery of new drugs. Many pharmaceuticals have created “Drug Repurposing” or “Drug Indications” departments. The strategy has already shown tremendous promise. For example, penicillin and its family of beta-lactam antibiotics are some of the most widely used and success-ful pharmaceuticals ever discovered and are about to be reinvented as therapeutics for treating neurological diseases; an old antihistamine, dimebon, has recently been shown to be effective for Alzheimer’s disease; and betahistine is currently being in-vestigated as an antiobesity drug.

The key advantage of drug repurposing is that the drugs have already undergone extensive safety & bioavailability testing. Being approved by regulatory agencies, approval of compounds repurposed for new indications should be easier, faster and free of toxicity hurdles. In addition, high-content screens, new biomarkers and non-invasive imaging techniques have created new opportunities for pursuing novel in-dications for approved compounds.

The FDA Approved Drug Library provides one of the richest sources of bioactives and offers the greatest degree of drug-likeness available. Being FDA approved and in use in the clinics, all of the compounds in the FDA Approved Drug Library have known and well characterized bioactivities and have undergone extensive safety & bioavailability testing, which could dramatically accelerate your drug development program.

Includes the following classes of drugs:

Analgesics Antineoplastics

Antiacnes Antianginals

Antibacterials Anticholinergics

Anticonvulsants Antidepressants

Antihistaminergics Antihyperlipidemics

Anti-inflammatories Antimalarials

Antiprotozoals Antipsychotics

Adrenergics Bronchodilators

COX2 inhibitors LO inhibitors

Erectile dysfunction Estrogens

Muscle relaxants Vasoconstrictors

Antihypertensives Anthelmintics

Antiarrhythmics Antiasthmatics

Anticholinesterases Anticoagulants

Antidiabetics Antifungals

Antihypertensives Antiinfectants

Antiparasitics Antiplatelet

Antiulceratives Antivirals

Chelating agents Cholinergics

Antiarthritics Diuretics

Glucocorticoids Antihistamines

Vasodilators Vitamins

And more. . .

Drug Repurposing 13Drug Repurposing


Natural products are an unsurpassed source of chemical diversity and are an ideal starting point for any screening program in the search for pharmacologically active small molecules1,2. Historically, natural products have been the most successful source of new drugs3. Over 49% of all New Chemical Entities introduced between 1981 and 2002 were natural products or based on natural product pharmacophores3. Designing a bias toward biological targets and “drug-like” character into a syn-thetic or combinatorial library requires significant efforts. In contrast, natural products inherently offer chemical diversity and biological specificity resulting from evolutionary pressures to interact with diverse biological targets.

Enzo Life Sciences maintains two growing libraries of highly purified natural products of known structure. The Natural Product Library (BML-2865) includes compounds from microbial, plant and marine sources including many compounds identified from ethnopharmacology (traditional medicine)4. The compounds are of low molecular weight and are supplied as highly pure pow-ders or oils. No extracts or mixtures are included in the collection. Each compound is available for resupply. The Rare Natural Product Library (BML-2866) contains compounds whose supply is limited and the sample size is 100μg. Many interesting, rare marine natural products5-7 are included in this unique collection.

Natural Product Library• Over 500 highly pure natural products, no

extracts• Low molecular weights• Purchase the full set from stock or custom

subsets

The Natural Product Library contains over 500 well-characterized natural products which are available in mg to gram quantities. The entire collection is available from stock at 1 mg per compound. Quantities greater or less than 1 mg or subsets are available as custom libraries.


2 mg/ml DMSO solutions 6 x 96-well plates


This library is available as a full set from stock or custom subsets can be purchased on a custom basis.Inquire with [email protected] for a compound list and ordering information*New natural products are added regularly. Inquire quarterly for updates.

Rare Natural Product LibraryThe Rare Natural Products Library contains 84 compounds whose supply is limited.


1 mg/ml DMSO solutions 1 x 96-well plate


This library is available as a full set from stock or custom subsets can be purchased on a custom basis.Inquire with [email protected] for a compound list and ordering information

[1] M. Tulp et al.; Drug Discov. Today 9, 450 (2004)[2] A. Harvey; Drug Discov. Today 5, 294 (2000)[3] D.J. Newman et al.; J. Nat. Prod. 66, 1022 (2003)

[4] M. Heinrich et al.; J. Pharm. Pharmacol. 53, 425 (2001)[5] A.M.S. Mayer et al.; Pharmacologist 42, 62 (2000)[6] P. Proksch et al.; Appl. Microbiol. Biotechnol. 59, 125

(2002)[7] B. Haefner; Drug Discov. Today 8, 536 (2003)

Library includes the following classes of natural products:

Terpenoids Peptolides Flavones Coumarins

Alkaloids Macrolides Isoflavones Synthetic deriv-atives

. . . and more

Natural Products

Product Compounds* Prod. No. Size

Natural Product Library 502 BML-2865-0500 500 ml/well


Rare Natural Product Library 84 BML-2866-0100 100 ml/well

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GUARANTEED QUALITY AND SUPPORTEnzo Life Sciences’ libraries have the quality you would expect from a company with over 25 years experience of making and storing compounds. Each compound is carefully QC’d and stored under ideal conditions. Libraries are supplied with a search-able structure fi le and an Excel fi le listing supporting information for each compound. Finally, the libraries are supported by a team of Ph.D. chemists who are available to assist with any questions that you may have.

Didn’t fi nd the library you need?Directed, focused libraries can be produced based on your structural requirements. Contact [email protected] with your requests.

Many new libraries are in development:

• Lipid Metabolism Inhibitors • Apoptosis Inducers • Cox Inhibitors

• TRP Channel Ligands • Steroids • Receptor Agonists

• Stem Cell Modulators . . . and more

Visit www.enzolifesciences.com regularly for an up-to-date listing

incorporating

15GUARANTEED QUALITY AND SUPPORT


International Distributors

Didn’t find the library you need?Directed, focused libraries can be produced based on your structural requirements. Contact [email protected] with your requests.

Many new libraries are in development:

• Lipid Metabolism Inhibitors • Apoptosis Inducers • Cox Inhibitors

• TRP Channel Ligands • Steroids • Receptor Agonists

• Stem Cell Modulators . . . and more

Visit www.enzolifesciences.com regularly for an up-to-date listing

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LAB SCIENTIFIC, INC. (USA)Tel: (305) 716-9922Fax: (305) 716-9923E-mail: [email protected]

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A-Ž LAB D.O.O.Tel: +386 (0)1 433 63 22 / +386 (0)1 230 18 84Fax: +386 (0)1 230 19 85E-mail: [email protected]

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LGC BIOTECHNOLOGIATel: (0)21 2583 4268 / (0)21 3273 5828Fax: (0)21 3273 5896E-mail: [email protected]

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Canada

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Chile

BIOCANT Ltda.Tel: (0)2 683 2437Fax: (0)56 2 683 8823E-mail: [email protected]

China

BEIJING BITAB BIOTECH Co. Ltd.Tel: (0)10 8201 5225Fax: (0)10 6201 5131E-mail: [email protected]

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Cyprus

SB BIOTECHNOLOGY SUPPLIERS SATel: +30 210 823 3373 / +30 210 691 0148Fax: +30 210 825 9987E-mail: [email protected]

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Indonesia

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Italy

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Japan

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Russia


Singapore

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Slovakia

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Slovenia

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South Africa

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Taiwan

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Thailand

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Turkey

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Ukraine


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