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.
- C3505 5-(N,N-dimethyl)-Amiloride (hydrochloride)Summary: NHE1、NHE2和NHE3抑制剂
- C3209 Butyrolactone 3Summary: 组蛋白乙酰转移酶Gcn5抑制剂
- C3208 CPTH2 (hydrochloride)Summary: Gcn5的HAT活性抑制剂
- B7819 CPI-1205Summary: EZH2抑制剂
- B7816 ITSA-1 (ITSA1)Summary: HDAC激活剂,通过抑制Trichostatin A (TSA)
- B7811 CPI-455 HClSummary: KDM5抑制剂
- B7806 HLCL-61Summary: PRMT5抑制剂
- B7801 CPI-637Summary: CBP/EP300 bromodomain抑制剂
- B6197 PF-CBP1 hydrochlorideSummary: CBP/p300 bromodomain抑制剂
- B6196 BI-7273Summary: BRD9 bromodomain抑制剂