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.
- B7816 ITSA-1 (ITSA1)Summary: HDAC activator via Trichostatin A (TSA) suppression
- B7819 CPI-1205Summary: EZH2 inhibitor
- C3208 CPTH2 (hydrochloride)Summary: inhibitor of HAT activity of Gcn5
- C3209 Butyrolactone 3Summary: histone acetyltransferase Gcn5 inhibitor
- C3505 5-(N,N-dimethyl)-Amiloride (hydrochloride)Summary: NHE1, NHE2, and NHE3 inhibitor
- C3076 AZD 5153Summary: orally available, bivalent inhibitor of the bromodomain and extraterminal (BET) protein BRD4.
- C3503 MS023 (hydrochloride)Summary: type I PRMTs inhibitor
- C3591 PTP Inhibitor IISummary: protein tyrosine phosphatase (PTP) inhibitor
- C3552 4'-bromo-Resveratrol1 CitationSummary: Sirt1 and Sirt3 inhibitor
- C3584 PBITSummary: JARID1 family demethylases inhibitor