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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B8380 KG-501Summary: A compound that inhibits CREB, with an IC50 of 6.89μM. -
B8471 Gambogenic acidSummary: Naturally derived; can covalently bind EZH2 and induce its ubiquitination and degradation. -
C3351 GSK484 (hydrochloride)Summary: A small molecule that reversibly and selectively inhibits PAD4-mediated protein citrullination. -
C3808 GSK199 (hydrochloride)Summary: A reversible, selective PAD4 inhibitor for inflammation research. -
C4419 NaphthofluoresceinSummary: Inhibitor of furin -
C8434 NudifloramideSummary: PARP-1 inhibitor -
A9936 OnametostatSummary: A inhibitor of the protein arginine methyltransferase 5 (PRMT5) -
C8445 CWI1-2 hydrochloride -
C8448 AMPK activator 2 -
BA2726 dBET6Summary: dBET6 is a highly efficient, selective, cell-permeable, ligand- and ligand-linked PROTAC.

