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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- PFI-2 (hydrochloride)Catalog No. :B8210
- MG 149Catalog No. :B3276HAT inhibitor
MG 149 is an inhibitor of histone acetyltransferases (HAT) with IC50 values of 74μM and 47μM for Tip60 and MOF, respectively .
- CCT007093Catalog No. :B3274PPM1D inhibitorCCT007093 is a small-molecule chemical inhibitor of PPM1D with IC50 value of 8.4μM .
- InauhzinCatalog No. :B3272SIRT1 inhibitorInauhzin is a small-molecule inhibitor of SIRT1 with IC50 value of 0.7-2μM .
- OG-L002 HClCatalog No. :A8766LSD1 inhibitor,potent and specificOG-L002 is a specific and potent inhibitor of lysine (K)-specific demethylase 1A (LSD1) with IC50 value of 20 nM.
- CTPBCatalog No. :C5773selective activator of the histone acetyltransferase (HAT) p300
- AGK7Catalog No. :C5709cell-permeable, selective inhibitor of SIRT2
- BRD6688Catalog No. :C5334HDAC inhibitor
- JFD00244Catalog No. :C5180inhibitor of SIRT2
- BizineCatalog No. :C5162LSD1 inhibitor