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.
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A4096 Belinostat (PXD101)2 CitationTarget: Histone Deacetylases (HDACs)Summary: Hydroxamate-type HDAC inhibitor -
A4120 MK-5108 (VX-689)Summary: Aurora-A kinase inhibitor,highly selective -
A4545 TCS 401Summary: Selective PTP1B inhibitor -
B1498 I-BET-7624 CitationTarget: BromodomainsSummary: BET inhibitor,highly potent -
B5686 GSK J5Summary: inactive isomer of GSK J4, KDM inhibitor -
C3208 CPTH2 (hydrochloride)Summary: inhibitor of HAT activity of Gcn5 -
A8182 3-Deazaneplanocin A (DZNep) hydrochloride6 CitationTarget: EZH2Summary: SAHH and EZH2 inhibitor -
B7323 AGK 2Summary: SIRT2 inhibitor, potent and selective -
A4136 TG101348 (SAR302503)2 CitationTarget: FLT3|JAK|c-RETSummary: JAK-2 inhibitor,potent and selective -
A4163 UPF 1069Target: PARPSummary: Selective PARP2 inhibitor
