表观遗传学相关配体
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.
Epigenetics in Cancer Ligands Library contains 367 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
Epigenetic process in cancer(Created by BioRender.com)
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Highlights
TMP269, HDAC inhibitor
XD14, BDR inhibitor
KDM5-IN-1, KDM5 inhibitor
Progesterone, Progsterone receptor agonist
Product Features
A set of 367 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.
Epigenetics in Cancer Ligands Library 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.
