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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 31

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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. PCI-34051
    A4091 PCI-34051
     1 Citation
    Target: Histone Deacetylases (HDACs)
    Summary: HDAC8 inhibitor,potent and selective
      insoluble in H2O; insoluble in EtOH; ≥14.8 mg/mL
  6. CUDC-101
    A4092 CUDC-101
     1 Citation
    Target: Histone Deacetylases (HDACs)|EGFR|ErbB
    Summary: Multitargeted HDAC inhibitor
      ≥21.7 mg/mL
  7. ITF2357 (Givinostat)
    A4093 ITF2357 (Givinostat)
     2 Citation
    Target: Histone Deacetylases (HDACs)
    Summary: HDAC inhibitor
      ≥23.8 mg/mL
  8. Scriptaid
    A4106 Scriptaid
     1 Citation
    Target: Histone Deacetylases (HDACs)
    Summary: HDAC inhibitor,novel and cell-permeable
      insoluble in H2O; ≥13.1 mg/mL
  9. Sodium Phenylbutyrate
    A4107 Sodium Phenylbutyrate
    Target: Histone Deacetylases (HDACs)
    Summary: Histone deacetylase inhibitor
      ≥27.65 mg/mL
  10. 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

Items 1-10 of 31

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