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Chromatin/Epigenetics - Type 2 Diabetes - Non-small Cell Lung Cancer - Myeloma - Bladder Cancer

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.

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  1. BAY 87-2243
    B1115 BAY 87-2243
    Target: Hypoxia Inducible Factors (HIFs)
    Summary: 有效的HIF-1选择性抑制剂
      ≥8.76 mg/mL
      insoluble in H2O
  2. SRT2104 (GSK2245840)
    A3821 SRT2104 (GSK2245840)
     1 Citation
    Target: Sir2-like Family Deacetylases (Sirtuins)
    Summary: SIRT1激活剂
      ≥6.46 mg/mL
      insoluble in H2O
  3. OTX-015
    A3692 OTX-015
     3 Citation
    中文名: 比拉瑞塞
    Target: Bromodomains
    Summary: BRD抑制剂
      ≥24.6 mg/mL
      insoluble in H2O
  4. CI994 (Tacedinaline)
    A4102 CI994 (Tacedinaline)
     1 Citation
    中文名: 乙酰地那林,他地那兰
    Target: Histone Deacetylases (HDACs)
    Summary: HDAC抑制剂
      ≥50 mg/mL
      insoluble in H2O
  5. Valproic acid sodium salt (Sodium valproate)
    A4099 Valproic acid sodium salt (Sodium valproate)
    中文名: 丙戊酸钠
    Target: Histone Deacetylases (HDACs)
    Summary: HDAC抑制剂
      ≥8.35 mg/mL
      ≥88.2 mg/mL
  6. CUDC-907
    A4097 CUDC-907
    中文名: 非美诺司他
    Target: Histone Deacetylases (HDACs)|PI3K
    Summary: PI3K/HDAC抑制剂
      ≥25.45 mg/mL
      insoluble in H2O
  7. Belinostat (PXD101)
    A4096 Belinostat (PXD101)
     2 Citation
    中文名: 贝利司他
    Target: Histone Deacetylases (HDACs)
    Summary: 羟肟酸型HDAC抑制剂
      ≥15.92 mg/mL
      insoluble in H2O
  8. SRT1720 HCl
    A4180 SRT1720 HCl
     3 Citation
    Target: Sir2-like Family Deacetylases (Sirtuins)
    Summary: SIRT1激活剂
      ≥25.3 mg/mL
      ≥15.37 mg/mL
  9. 3-Deazaneplanocin A (DZNep) hydrochloride
    A8182 3-Deazaneplanocin A (DZNep) hydrochloride
     1 Citation
    中文名: 3-去氮腺嘌呤A盐酸盐
    Target: EZH2
    Summary: SAHH和EZH2抑制剂
      ≥14.94 mg/mL
      ≥18.32 mg/mL
  10. Entinostat (MS-275,SNDX-275)
    A8171 Entinostat (MS-275,SNDX-275)
     2 Citation
    中文名: 恩替诺特
    Target: Histone Deacetylases (HDACs)
    Summary: HDAC1和HDAC3抑制剂
      ≥18.8 mg/mL
      insoluble in H2O

10 件产品

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