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.
- A4107 Sodium PhenylbutyrateTarget: Histone Deacetylases (HDACs)Summary: Histone deacetylase inhibitor
- A4111 VX-680 (MK-0457,Tozasertib)Target: Aurora KinasesSummary: Aurora kinase inhibitor
- A4112 Barasertib (AZD1152-HQPA)3 CitationTarget: Aurora KinasesSummary: Aurora Kinase B inhibitor, Potent and selective
- A4130 ENMD-2076Target: Aurora Kinases|FLT3|RET|Src|VEGFR3/FLT4|NTRK1/TRKA|CSF-1R/c-FmsSummary: Selective Aurora A/Flt3 inhibitor
- A4132 CCT137690Target: Aurora KinasesSummary: Aurora A/B/C inhibitor
- A4094 MC15683 CitationTarget: Histone Deacetylases (HDACs)Summary: Class II HDAC inhibitor,potent and selective
- A4095 Pracinostat (SB939)2 CitationTarget: Histone Deacetylases (HDACs)Summary: Pan-HDAC inhibitor
- A4096 Belinostat (PXD101)2 CitationTarget: Histone Deacetylases (HDACs)Summary: Hydroxamate-type HDAC inhibitor
- A4097 CUDC-907Target: Histone Deacetylases (HDACs)|PI3KSummary: Potent PI3K/HDAC inhibitor
- A4098 PCI-24781 (CRA-024781)Target: Histone Deacetylases (HDACs)Summary: Pan-HDAC inhibitor