Chromatin/Epigenetics
Epigenetics is the heritable modifications in gene expression that is not associated with changes in DNA sequence. Epigenetic modifications occur mostly on DNA or on the histone octamer. There are several types of epigenetics modifications, DNA methylation by DNA-methyl transferase (DNMT) and covalent modification of histones (e.g. acetylation, methylation, phosphorylation and ubiquitination). Histone acetylation by histone acetyltransferases (HATs) is involved in transcriptional activation, whereas histone deacetylation by histone deacetylases (HDACs) is connected with transcriptional repression. Histone demethylation is associated with lysine-specific demethylase (LSD) and JmjC domain containing histone demethylase (JHDM).
The nucleosome is consisted of four histone proteins (H2A, H2B, H3, and H4), they are primary building block of chromatin. The addition and removal of specific chemical groups refers to as epigenetic marks, it regulates chromatin structure and affects gene expression. Moreover, RNA is intimately involved in the formation of a repressive chromatin state.
Epigenetic mechanism responds to environmental changes at the cellular level and thus influences cellular plasticity. Chromatin and epigenetic regulation play a significant role in the programming of the genome during development and stress response, defects in epigenetics can lead to cancer, inflammation and metabolic disorders etc.
- A8173 Romidepsin (FK228, depsipeptide)7 CitationTarget: Histone Deacetylases (HDACs)Summary: HDAC1/HDAC2 inhibitor, potent and selective
- A8176 Apicidin2 CitationTarget: Histone Deacetylases (HDACs)Summary: Potent HDAC inhibitor
- N1315 ParthenolideTarget: Histone Deacetylases (HDACs)|MDM2|DNA Methyltransferases|p53|5-HT
- B4890 HPOB1 CitationTarget: Histone Deacetylases (HDACs)Summary: HDAC6 inhibitor, potent and selective
- B5916 Chidamide1 CitationTarget: HDACSummary: Novel HDAC inhibitor
- B5936 ACY-241Summary: Selective and orally active HDAC6 inhibitor
- B3704 Nexturastat ATarget: Histone Deacetylases (HDACs)Summary: HDAC6 inhibitor,highly potent and selective
- B4106 4SC-202Summary: Class I HDAC inhibitor
- B4655 BMS-345541(free base)Summary: IKK-1/IKK-2 inhibitor,potent and selective
- A8547 Tubastatin A HCl1 CitationTarget: Histone Deacetylases (HDACs)Summary: HDAC6 inhibitor,potent and selective