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EBCL-0015

Epigenetics Related Ligands

Cancer epigenetics is the study of epigenetic changes to the DNA of cancer cells. These changes provide a way for cells to control and regulate gene activity without changing the genes permanently. Epigenetic control relies on small, reversible, changes to the DNA and proteins such as: DNA methylation, changes in the structure of histone proteins or gene regulation by small noncoding microRNAs. Controlling epigenetic changes may provide us with helpful tools for cancer prevention, detection, and therapy.

Library of Cancer Epigenetics Related Ligands contains 960 small ligands, some representative molecules are given below: TMP269, HDAC inhibitor; XD14, BDR inhibitor; KDM5-IN-1, KDM5 inhibitor; Progesterone, Progesterone receptor agonist.

Related terms: poly(ADP-ribose) polymerase, histone deacetylase, tankyrase, aurora kinase, bromodomain, nuclear receptor coactivator

Library image

Epigenetic process in cancer(Created by BioRender.com)

Preplated options

Dry powder/solution (DMSO)Dry powder
Number of compounds960
Comment
Dry powder/solution (DMSO)DMSO
Number of compounds628
Comment

Highlights

Molecule highlight
EBC-12824CAS: 1314890-29-3

TMP269, HDAC inhibitor EBC-12824

Molecule highlight
EBC-08691CAS: 1370888-71-3

XD14, BDR inhibitor EBC-08691

Molecule highlight
EBC-09069CAS: 1628210-26-3

KDM5-IN-1, KDM5 inhibitor EBC-09069

Molecule highlight
EBC-06111CAS: 57-83-0

Progesterone, Progsterone receptor agonist EBC-06111

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Disclaimer

All our products are for research purpose only. Any personal or non-scientific use is strictly prohibited.

Note

All the compounds with solubility below 10 mM are shipped as 2 mM solutions.

Product Features

  • A set of 960 epigenetics in cancer relevant molecules with sub-10 micromolar activity coefficient values for HTS/HCS programs.
  • The library is composed of ligands that target all major pharmaceutically relevant epigenetics in cancer targets.
  • Library of Cancer Epigenetics Related Ligands covers novel promising preclinical lead compounds, clinical candidates and approved drugs.
  • Calculated structural diversity of the collection: 0.85.
  • Comprehensive documentation with structures, trivial names, synonyms, activity coefficient values, types of action on target and references to original literature.
  • NMR and LCMS validated purity.
  • All the compounds are available in stock for hit follow-up.
  • The library is continuously updated.

Product Details

  • Format: 10 - 100 µL of 10 mM DMSO stock solutions; dry powders (1 mg);
  • Container: 384-well microplates;
  • Storage: - 18 °C;
  • Shipping: Dry ice.

Utility

  • High throughput screening (HTS);
  • High content screening (HCS);
  • Cherry picking.

Library Composition

Name
Occurrence in the library, times

Histone deacetylases (HDACs)

154

154

Number of compounds

154

Aurora kinase (Aur) family

113

113

Number of compounds

113

Poly ADP-ribose polymerases

107

107

Number of compounds

107

Bromodomain kinase (BRDK) family

80

80

Number of compounds

80

Protein arginine N-methyltransferases

50

50

Number of compounds

50

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