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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 131-140 of 368

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  1. 2-hexyl-4-Pentynoic Acid
    B5969 2-hexyl-4-Pentynoic Acid
    Summary: Potent and robust HDACs inhibitor
      insoluble in H2O; ≥15.45 mg/mL
  2. Sanguinarine chloride
    B5970 Sanguinarine chloride
    Summary: Inhibitor of PP2C and MKP-1
      insoluble in H2O; insoluble in EtOH; ≥3.68 mg/mL
  3. PFI 4
    B5973 PFI 4
    Summary: Potent and selective BRPF1 Bromodomain inhibitor
      insoluble in H2O; ≥13.3 mg/mL
  4. Triacetyl Resveratrol
    B5971 Triacetyl Resveratrol
    Summary: Cell-permeable resveratrol prodrug
      insoluble in EtOH; insoluble in H2O; ≥13.85 mg/mL
  5. CHZ868
    B5980 CHZ868
     1 Citation
    Summary: Type II JAK2 inhibitor
      Soluble in DMSO
  6. GSK2801
    B5998 GSK2801
    Summary: inhibitor of BAZ2A and BAZ2B bromodomains
      insoluble in H2O; ≥18.55 mg/mL
  7. PX-478 2HCl
    B6004 PX-478 2HCl
     6 Citation
    Target: Hypoxia Inducible Factors (HIFs)
    Summary: HIF-1α inhibitor
      ≥19.7 mg/mL
  8. Peficitinb (ASP015K, JNJ-54781532)
    B6005 Peficitinb (ASP015K, JNJ-54781532)
    Summary: JAK inhibitor
      ≥23.2 mg/mL
  9. BI-847325
    B6014 BI-847325
    Summary: dual inhibitor of MEK and Aurora kinases
      ≥24.1 mg/mL
  10. UNC3866
    A8725 UNC3866
    Summary: a potent antagonist of CBX4 and CBX7 chromodomains
      Soluble in DMSO

Items 131-140 of 368

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Relate Categories
Category
  1. Bromodomain34item
  2. Aurora Kinase30item
  3. DNA Methyltransferase7item
  4. HDAC59item
  5. Histone Acetyltransferases17item
  6. Histone Demethylases24item
  7. Histone Methyltransferase47item
  8. HIF12item
  9. JAK41item
  10. MBT Domains1 item
  11. PARP30item
  12. Pim8item
  13. Protein Ser/Thr Phosphatases30item
  14. RNA Polymerase4item
  15. Sirtuin19item
  16. Sphingosine Kinase-21 item
  17. Polycomb repressive complex2item
  18. SUMOylation2item
  19. PAD1 item
Specificity
  1. Selective105item
Reversibility
  1. Reversible7item
  2. Irreversible2item
Target
  1. Cyclin-Dependent Kinases1 item
  2. Histone Deacetylases (HDACs)33item
  3. PI3K1 item
  4. Aurora Kinases21item
  5. MDM21 item
  6. EZH23item
  7. Bromodomains8item
  8. FLT35item
  9. PLK1 item
  10. VEGFR3item
  11. RET1 item
  12. Hydrolase1 item
  13. MEK1 item
  14. DOT1L3item
  15. FGFR2item
  16. Nrf21 item
  17. Pim3item
  18. Sir2-like Family Deacetylases (Sirtuins)6item
  19. PP11 item
  20. PP2A1 item
  21. Src5item
  22. Trk Receptors1 item
  23. STAT2item
  24. EGFR2item
  25. Hypoxia Inducible Factors (HIFs)2item
  26. Tankyrases1 item
  27. JAK20item
  28. p3001 item
  29. Syk1 item
  30. EZH11 item
  31. Topoisomerases1 item
  32. ErbB1 item
  33. DNA Methyltransferases3item
  34. Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitors (HIF-PHIs)1 item
  35. SMYD21 item
  36. CREBBP2item
  37. EP3002item
  38. LRRK21 item
  39. PARP8item
  40. ALK1 item
  41. Bromodomain and Extra-Terminal motif (BET)1 item
  42. phosphatases1 item
  43. COX1 item
  44. NAT101 item
  45. G9a2item
  46. Hck1 item
  47. SETD71 item
  48. Histone Demethylases1 item
  49. MNK1 item
  50. AChE1 item
  51. Catechol O-Methyltransferase (COMT)1 item
  52. O6-methylguanine-DNA-methyl-transferase (MGMT)1 item
  53. Protein Arginine Methyltransferases1 item
  54. PP41 item
  55. c-RET1 item
  56. VEGFR3/FLT41 item
  57. NTRK1/TRKA1 item
  58. CSF-1R/c-Fms1 item
  59. PTP1 item
  60. Protein polybromo-11 item
  61. SMARCA41 item
  62. SMARCA21 item
  63. p532item
  64. HDAC2item
  65. KDM2item
  66. LOX1 item
  67. Adenylyl cyclase1 item
  68. Quinone reductase1 item
  69. Histone Acetyltransferases (HATs)2item
  70. Trx1 item
  71. HIF-PH1 item
  72. L3MBTL1 item
  73. TYK22item
  74. MUSK1 item
  75. MAP3K1 item
  76. Lck1 item
  77. p211 item
  78. 5-HT1 item
  79. PHF1 item
  80. FGR1 item
  81. YES1 item
  82. Fyn1 item
  83. ARG1 item
  84. LSD1 item
  85. PRMT1 item
  86. GLP1 item
  87. SK1 item
  88. Sirtuin1 item
Reported Experiments
  1. Animal Experiments120item
  2. Cell Experiments100item
Related Disease
  1. Acute Myelogenous Leukemia1 item
  2. Acute Myeloid Leukemia9item
  3. Bladder Cancer2item
  4. Breast Cancer18item
  5. Cancer83item
  6. Castration-resistant Prostate Cancer1 item
  7. Cervical Cancer2item
  8. Chronic Lymphocytic Leukemia1 item
  9. Colon Cancer11item
  10. Colorectal Cancer4item
  11. Diabetes2item
  12. Diffuse Large B-cell Lymphoma1 item
  13. Dyskinesia1 item
  14. Epilepsy1 item
  15. Friedreich's Ataxia1 item
  16. Glioblastoma2item
  17. Glioma2item
  18. Hepatic Cancer1 item
  19. Hepatocellular Carcinoma1 item
  20. HIV2item
  21. HIV Infections1 item
  22. Immunological Diseases1 item
  23. Inflammatory Bowel Disease1 item
  24. Inflammatory Diseases3item
  25. Leukemia7item
  26. Lung Cancer6item
  27. Lymphoma5item
  28. Melanoma5item
  29. Mixed Lineage Leukemia3item
  30. Multiple Myeloma5item
  31. Myelofibrosis1 item
  32. Myeloma1 item
  33. Neuroblastoma2item
  34. Neuronal Protection1 item
  35. Non-small Cell Lung Cancer4item
  36. Ovarian Cancer5item
  37. Pancreatic Cancer3item
  38. Prostate Cancer12item
  39. Psoriasis1 item
  40. Renal Cancer1 item
  41. Renal Cell Carcinoma2item
  42. Rheumatoid Arthritis3item
  43. Thyroid Cancer1 item
  44. Type 2 Diabetes2item