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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.

Items 1-10 of 18

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  1. Rocilinostat (ACY-1215)
    A4083 Rocilinostat (ACY-1215)
     1 Citation
    Target: Histone Deacetylases (HDACs)
    Summary: Selective HDAC6 inhibitor
      ≥21.675 mg/mL
  2. Vorinostat (SAHA, MK0683)
    A4084 Vorinostat (SAHA, MK0683)
     9 Citation
    Target: Histone Deacetylases (HDACs)
    Summary: HDAC inhibitor
      insoluble in EtOH; insoluble in H2O; ≥4.41 mg/mL
  3. Mocetinostat (MGCD0103, MG0103)
    A4089 Mocetinostat (MGCD0103, MG0103)
     2 Citation
    Target: Histone Deacetylases (HDACs)
    Summary: HDAC inhibitor,isotype-selective and potent
      insoluble in EtOH; insoluble in H2O; ≥19.8 mg/mL
  4. JNJ-26481585
    A4090 JNJ-26481585
     3 Citation
    Target: Histone Deacetylases (HDACs)
    Summary: Potent HDAC inhibitor
      insoluble in H2O; insoluble in EtOH; ≥19.2 mg/mL
  5. MC1568
    A4094 MC1568
     3 Citation
    Target: Histone Deacetylases (HDACs)
    Summary: Class II HDAC inhibitor,potent and selective
      insoluble in EtOH; insoluble in H2O; ≥15.7 mg/mL
  6. Belinostat (PXD101)
    A4096 Belinostat (PXD101)
     2 Citation
    Target: Histone Deacetylases (HDACs)
    Summary: Hydroxamate-type HDAC inhibitor
      insoluble in H2O; ≥15.92 mg/mL
  7. CUDC-907
    A4097 CUDC-907
    Target: Histone Deacetylases (HDACs)|PI3K
    Summary: Potent PI3K/HDAC inhibitor
      ≥25.45 mg/mL
  8. Valproic acid sodium salt (Sodium valproate)
    A4099 Valproic acid sodium salt (Sodium valproate)
    Target: Histone Deacetylases (HDACs)
    Summary: HDAC inhibitor
      ≥8.35 mg/mL
  9. CI994 (Tacedinaline)
    A4102 CI994 (Tacedinaline)
     1 Citation
    Target: Histone Deacetylases (HDACs)
    Summary: HDAC inhibitor
      insoluble in H2O; insoluble in EtOH; ≥50 mg/mL
  10. AR-42 (OSU-HDAC42)
    A4104 AR-42 (OSU-HDAC42)
     2 Citation
    Target: Histone Deacetylases (HDACs)
    Summary: HDAC inhibitor,novel and potent
      insoluble in EtOH; insoluble in H2O; ≥15.62 mg/mL

Items 1-10 of 18

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