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Epigenetics


Product Name: Format/Size Descriptions Download
Epigenetic Library 5391 compounds
For cherry-picking
Update: 2020-07
The file contains all available Epigenetic compounds selected from our Signature & BioDesign Libraries.
SL#031
EZH2 inhibitors
80 compounds
Pre-Plated Set
Release: 2016
Using a combination of structure and ligand based design, ASINEX has created a library of aminomethyl quinolone-2 derivatives decorated by ortho-substituted heteroaromatic acids. The resulting amides share some similarity with published EZH2 inhibitors and may provide useful molecular probes for understanding EZH2 functional activity and developing novel, potent anti-cancer agents.
SL#042
Protein-lysine-
methyltransferase
80 compounds
Pre-Plated Set
Release: 2016
The Protein Data Bank has more than 1300 different PKMT entries in their apo- or small molecule-bound forms which provides a significant amount of information for de novo design of novel selective inhibitors. Additionally, new compounds with validated in vitro inhibitory activity toward PKMTs represent an attractive starting point for the rational creation of more effective inhibitors. In this library we highlight several compounds that demonstrate a μM range of activity against SETD8 – an emerging target for anti-cancer intervention.
SL#045
HDAC inhibitors
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has screened a library of 50000 small molecules and identified a number of hits with significant HDAC (HeLa cell lysate) inhibitory activity.
SL#047
BET inhibitors
80 compounds
Pre-Plated Set
Release: 2016
By utilizing a combination of ligand-based and structure-based design methods, ASINEX has created a library of novel compounds that were shown to inhibit BRD2 and BRD4 proteins in vitro.
SL#086
Histone demethylases
(KDMs) inhibitors
80 compounds
Pre-Plated Set
Release: 2018
A series of thieno[3,2-b]pyrrole-5-carboxamides derivatives have been identified as µM inhibitors of KDM1A using an HTS workflow and supported by subsequent structure-based design studies.
A similarity search through ASINEX’s compound collection identified several close analogs of the reported inhibitors that could be interesting for KDM-related research and drug discovery.

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Product Name: Format/Size Descriptions Download
Nucleoside Mimetics 3118 compounds
For cherry-picking
Update: 2020-07
ASINEX has developed a number of stereo- and enantio-selective methods for the synthesis of nucleoside-like core intermediates (e. g. mimics of adenosine). These unique intermediates have been extensively decorated by various long chain amines, acids and amino acids.
Dinucleoside Mimetics
for RNA
842 compounds
For cherry-picking
Update: 2020-10
Systematic analysis of published small molecules with declared RNA activity has revealed several prominent structural elements that can be used as design templates for the creation of novel chemical libraries for RNA drug discovery. In particular, a combination of aromatic heterocyclic rings such as nucleobases or bioisosteric analogs with a saturated linear or ring component connected via a carbon-carbon bond are very common motifs among RNA-bound ligands with favorable drug-like properties. This observation confirms earlier published data suggesting that molecules having a favorable carbon bond saturation (defined by Fsp3) represent “biologically relevant chemical space” . In the case of RNA ligands, the right balance of aromaticity and saturation embedded in the RNA-compatible molecular framework may enhance binding probability. ASINEX have identified several such advantageous combinations.
Nucleoside-mimetics
Pre-Plated Set
3826 compounds
Pre-Plated Set
Amount: 0.01-2.0 mg
Update: 2018-04
ASINEX ‘s Nucleoside-mimetics Pre-plated Sets are designed to provide popular screening libraries in a convenient and cost-effective manner.
SL#010, 052, 098
Purine-based Nucleosides
80 compounds x 3
Pre-Plated Set
Release: 2016-2018
Compounds targeting the SAM/SAH site of these enzymes offer great potential, yet very few such molecules are currently described in literature or commercially available in compound collections. To address this market need, ASINEX has used a modular approach to synthesize a library of purine-based nucleosides. The main challenge was to develop stereo- and enantio-selective methods for the synthesis of nucleotide-like cores which both mimic adenosine and are metabolically stable.
SL#099
Pyrimidine-based
Nucleosides
80 compounds
Pre-Plated Set
Release: 2018
Nucleoside mimetics are the class of small molecule drugs with antitumor, antiviral, and antibacterial activity. Alterations in the base or sugar moieties can lead to significant changes in pharmacokinetic and pharmacodynamic properties of these molecules. Many convenient synthetic methods have been developed for modification of naturally occurring nucleosides, but synthetic analogs would require non-conventional approaches involving stereo- and enantio-selective reactions. In this library, a variety of pyrimidine nucleobases was linked to a number of synthetic glycomimetic cores, followed by modifications of the terminal amino group. The resulting nucleoside mimetic molecules do not have a glycosidic linkage which may be beneficial for optimizing metabolic properties.
Contact
Global

Ludmila Sadovenko

lsadovenko@asinex.com
North America

Mark Parisi

mparisi@asinex.com

Toll Free: +1 877 ASINEX1

Tel: +1 336 721 1617

Fax: +1 336 721 1618

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USA

Europe

Galina Afanasyeva

gafanasyeva@asinex.com

Tel: +31 (0) 203416183

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Amsterdam, The Netherlands

Japan

Shingo Ota

sota@asinex.com

Tel: 080-3401-9097

30-2 Higashihazu, Nishio,

Aichi Japan

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