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.
- A4125 CYC116Target: Aurora Kinases|FLT3|VEGFRSummary: Potent Aurora A/B inhibitor
- A4127 GSK1070916Target: Aurora KinasesSummary: Aurora B/C inhibitor
- A4128 PF-03814735Target: Aurora KinasesSummary: Aurora A/B inhibitor
- A4193 SMI-4aTarget: PimSummary: Potent Pim inhibitor
- A4203 Tenovin-1Target: Sir2-like Family Deacetylases (Sirtuins)|p53|p21Summary: SIRT2 inhibitor, activates p53
- A4170 EPZ004777Target: DOT1LSummary: DOT1L inhibitor
- A4186 Bromosporine1 CitationTarget: BromodomainsSummary: Bromodomain inhibitor,non-selective
- A4152 BMS-911543Target: JAKSummary: JAK2 inhibitor,selective small molecule
- A1905 3-Deazaneplanocin,DZNep6 CitationTarget: HydrolaseSummary: S-adenosylhomocysteine and EZH2 inhibitor
- A1907 5-Azacytidine6 CitationTarget: DNA MethyltransferasesSummary: DNA methyltransferase inhibitor.