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.
-
A4158 AG-143611 CitationSummary: Potent PARP1 inhibitor -
A4171 EPZ0056872 CitationTarget: EZH2Summary: EZH2 inhibitor,potent and selective -
A4115 JNJ-77066211 CitationTarget: Cyclin-Dependent Kinases|Aurora KinasesSummary: Potent CDK/Aurora kinase inhibitor -
A3794 SB1317Summary: CDK,JAK and FLT inhibitor -
A4540 Okadaic acidSummary: Protein phosphatase 1 inhibitor -
A8567 Tenovin-3Summary: p53 activator -
B4894 SP2509Target: Histone DemethylasesSummary: Demethylase 1 (LSD1) antagonist, novel Lysine-specific -
B1115 BAY 87-2243Target: Hypoxia Inducible Factors (HIFs)Summary: HIF-1 inhibitor,potent and selective -
A8181 (-)-JQ116 CitationTarget: BromodomainsSummary: Stereoisomer of (+)-JQ1, used as negative control -
B6987 CI 976Summary: acyl-coenzyme A:cholesterol acyltransferase (ACAT) inhibitor
