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.
- B3272 InauhzinTarget: Sir2-like Family Deacetylases (Sirtuins)Summary: SIRT1 inhibitor
- A3962 AZD1208Target: PimSummary: PIM kinase inhibitor
- A4501 Tubacin3 CitationTarget: Histone Deacetylases (HDACs)Summary: HDAC6 inhibitor,potent,selective,reversible,cell-permeable
- A4512 Cucurbitacin ITarget: STAT|JAKSummary: STAT3/JAK2 signaling inhibitor
- A4536 Fostriecin sodium saltTarget: PP1|PP2A|Topoisomerases|PP4Summary: Antitumor antibiotic
- A4489 TC-A 2317 hydrochlorideTarget: Aurora KinasesSummary: Aurora kinase A inhibitor,potent and selective
- A4490 I-CBP 112Target: CREBBP|EP300Summary: CBP/EP300 bromodomain inhibitor
- A4491 SGC-CBP302 CitationTarget: CREBBP|EP300Summary: Inhibitor of CREBBP/EP300 bromodomain,potent
- A4492 NU 9056Target: Histone Acetyltransferases (HATs)Summary: KAT5 (Tip60) HAT inhibitor
- A4506 DMOGTarget: Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors (HIF-PHIs)Summary: Competitive HIF-PH inhibitor, cell-permeable