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DYNA001 Sigma-Aldrich

DyNAbind® DNA-Encoded Fragment Library

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Properties

form   pellets
storage temp.   −20°C

Description

Application

Product Features and Benefits:

• Off-the-shelf, affordable access to DEL technology
• Dynamic fragment library provides a revolutionary approach to DELs offering unprecedented library and data quality
• High level quality control with every single member individually purified and validated to maximize data reliability and chances for finding good hits
• Rule of Three used in library design ensures compounds are in favorable fragment space with good ligand efficiency and plenty of room for optimization (Congreve et al. 2003, Jhoti et al. 2013)
• Ability to perform and validate initial DEL screening internally before engaging service provider
• A library with maximized diversity, ready to deploy against nearly any druggable target

Product Overview:

• Dynamic fragment-based DEL as alternative or complement to existing screening technologies
• Consumable, off-the-shelf product for immediate use
• 5 vials, each containing a single-use library for one experimental condition
• Detailed protocol accessible to most drug discovery labs
• A dedicated analysis portal and protocol to identify hits

Application Statement:

DNA-encoded library (DEL) technology is a drug discovery tool containing small DNA-barcoded compounds (Satz 2018). The DyNAbind fragment DEL contains small molecular weight compounds. The high ligand efficiency of fragment molecules is harnessed to effectively probe a target′s binding site and increase the likelihood of discovering binders (Murray and Rees 2009, Murray et al. 2012). Moreover, this library uses DyNAbind′s proprietary Dynamic Library technology to drive binder optimization and reveal not only individual fragments, but also joined fragment pairs for over 370,000 highly diverse structures (Reddavide et al. 2015). DyNAbind′s proprietary Dynamic Library technology reshuffles fragment pairs to automatically optimize the affinity of binders and increase the chances of finding good hits. After a pooled screening approach, bound fragments can be determined using next-generation sequencing of the barcodes. Analysis of the sequencing data is provided at no additional cost through a portal on our website which will generate a list of the fragments that bind the target. These fragments can be used as structural starting points to develop larger, more drug-like compounds. Analysis Portal: www.SigmaAldrich.com/DELanalysis


Detailed Packaging Overview:

5 tubes with 1 lyophilized pellet in each.

The kit contains five tubes, each with an identical copy of the library. The amount of library in each tube is optimized for one experimental condition. For example, this could allow setting up duplicates of one condition of the library with His-tagged protein and His-tag pulldown beads. Then duplicates of a negative control without the His-tagged protein could be set up. One tube of the library would be left over. Note that the amount of each fragment-DNA per tube is 0.1 pmol. While this may seem low compared to some screening methods, DEL technology allows working with such a low amount of compound.

Legal Information

Product of DyNAbind GmbH

DyNAbind is a registered trademark of DyNAbind GmbH

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
Protocols & Articles

Articles

Fragment-Based DNA-Encoded Library for Drug Discovery

DNA-Encoded Library (DEL) technology is an increasingly mature and prominent approach to early-stage drug discovery. As opposed to traditional high-throughput screening approaches where compounds are...
Keywords: Biochemistry, Drug discovery, Medicinal chemistry, Molecular biology, Polymerase chain reaction, Sequencing

Related Content

Limited Use Label License for DyNAbind Products

The use of this DyNAbind Product (the “Product”) is covered by European Patents EP 3 094 745 B1 and EP 3 169 832 B1 and corresponding applications pending in the US, Canada, and Japan. Purchaser is g...

Peer-Reviewed Papers
15

References

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