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.
-   B5913 C7280948Summary: Novel PRMT1 inhibitor B5913 C7280948Summary: Novel PRMT1 inhibitor
-   B6197 PF-CBP1 hydrochlorideSummary: CBP/p300 bromodomain inhibitor B6197 PF-CBP1 hydrochlorideSummary: CBP/p300 bromodomain inhibitor
-   C4347 β-Glycerophosphate (sodium salt hydrate)7 CitationSummary: protein phosphatase inhibitor C4347 β-Glycerophosphate (sodium salt hydrate)7 CitationSummary: protein phosphatase inhibitor
-   A4152 BMS-911543Target: JAKSummary: JAK2 inhibitor,selective small molecule A4152 BMS-911543Target: JAKSummary: JAK2 inhibitor,selective small molecule
-   A4493 KD 51701 CitationSummary: HDAC inhibitor A4493 KD 51701 CitationSummary: HDAC inhibitor
-   A4489 TC-A 2317 hydrochlorideTarget: Aurora KinasesSummary: Aurora kinase A inhibitor,potent and selective A4489 TC-A 2317 hydrochlorideTarget: Aurora KinasesSummary: Aurora kinase A inhibitor,potent and selective
-   A8893 Rucaparib (free base)Target: PARPSummary: Potent PARP inhibitor A8893 Rucaparib (free base)Target: PARPSummary: Potent PARP inhibitor
-   B4989 EPZ015666Target: Protein Arginine MethyltransferasesSummary: PRMT5 inhibitor B4989 EPZ015666Target: Protein Arginine MethyltransferasesSummary: PRMT5 inhibitor
-   B6196 BI-7273Summary: BRD9 bromodomain inhibitor B6196 BI-7273Summary: BRD9 bromodomain inhibitor
-   C3996 PRL-3 InhibitorSummary: phosphatase of regenerating liver 3 (PRL-3) inhibitor C3996 PRL-3 InhibitorSummary: phosphatase of regenerating liver 3 (PRL-3) inhibitor
