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.
- C3996 PRL-3 InhibitorSummary: phosphatase of regenerating liver 3 (PRL-3) inhibitor
- C3668 GSK6853Summary: BRPF1 inhibitor
- C3829 Cl-Amidine (trifluoroacetate salt)Summary: PAD4 deimination activity inhibitor
- C3776 MS049 (hydrochloride)Summary: PRMT4 and PRMT6 inhibitor
- C4097 NI-57Summary: bromodomains of BRPF proteins inhibitor
- C4018 4-iodo-SAHASummary: class I and class II histone deacetylase (HDAC) inhibitor
- C4229 UMB-32Summary: inhibitor of the BET bromodomain BRD4 and the bromodomain-containing transcription factor TAF1 and TAF1L
- C4247 RN-1 (hydrochloride)Summary: LSD1 inhibitor
- C4119 2',3',5'-triacetyl-5-AzacytidineSummary: prodrug form of 5-azacytidine, a DNA methyltransferase inhibitor
- C4347 β-Glycerophosphate (sodium salt hydrate)Summary: protein phosphatase inhibitor