Epigenetics

Epigenetics research delves into the molecular mechanisms that control gene expression and cellular traits without altering the underlying DNA sequence. One crucial aspect of this field is the role of small molecules, which act as powerful regulators of epigenetic modifications. These small compounds, typically comprising a few dozen to a few hundred atoms, have emerged as essential tools in understanding and manipulating the epigenome.

  • DNA Methylation Inhibitors: Small molecules like 5-azacytidine and 5-aza-2'-deoxycytidine are DNA methyltransferase inhibitors. They block the addition of methyl groups to DNA, leading to DNA demethylation. This can reactivate silenced genes, potentially offering therapeutic avenues for conditions like cancer.
  • HDAC inhibitors: HDACs remove acetyl groups from histone proteins, contributing to gene repression. Small molecule HDAC inhibitors, such as Vorinostat and Romidepsin, can reverse this process by increasing histone acetylation, allowing genes to be more accessible for transcription. These inhibitors are being explored for cancer therapy and other conditions.
  • Histone Methyltransferase Inhibitors: Small molecules like GSK126 inhibit specific histone methyltransferases, affecting histone methylation patterns. This can alter gene expression, making them promising candidates for cancer and other diseases with epigenetic dysregulation.
  • RNA Modulators: Small molecules can also target non-coding RNAs involved in epigenetic regulation. For instance, small molecules called small interfering RNAs (siRNAs) can be designed to target and degrade specific long non-coding RNAs, influencing gene expression.
  • Epigenetic Reader Domain Inhibitors: These small molecules target proteins that recognize and bind to specific epigenetic marks. Examples include inhibitors of bromodomain-containing proteins (BET inhibitors), which can disrupt gene regulation by interfering with protein-DNA interactions.

Small molecules in epigenetics research not only provide insights into the fundamental biology of gene regulation but also hold immense promise for developing novel therapeutics. Their ability to selectively modulate specific epigenetic marks and pathways has led to ongoing clinical trials and drug development efforts for various diseases, including cancer, neurological disorders, and inflammatory conditions. Understanding and harnessing the power of these small molecules is at the forefront of modern epigenetics research, offering new hope for precision medicine and targeted therapies.


3 key components involved in the regulation of epigenetic modifications

Epigenetics Writer

Epigenetics writers are enzymes responsible for adding chemical marks or modifications to DNA or histone proteins. These marks include DNA methylation (addition of methyl groups to DNA) and histone modifications (such as acetylation, methylation, phosphorylation, etc.).

Epigenetics Reader

Function: Epigenetics readers are proteins that can recognize and bind to specific epigenetic marks on DNA or histones. These reader proteins interpret the epigenetic code and facilitate downstream cellular processes, such as gene activation or repression.

Epigenetics Eraser

Function: Epigenetics erasers are enzymes responsible for removing or reversing epigenetic marks on DNA or histones. This process allows for the dynamic regulation of gene expression and the resetting of epigenetic states during various stages of development and in response to environmental changes.

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Catalog No.
Product Name
Application
Product Information
Product Citation
  1. KDM5A inhibitor

    YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM.
  2. Bromodomain inhibitor

    BET-IN-1 is a bromodomain inhibitor extracted from patent WO/2013024104A1, compound example 2, has a plC50 in the range 6.0 - 7.0. IC50 value: 6.0 - 7.0 (plC50) Target: bromodomain
  3. HDAC inhibitor

    Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of histone deacetylase enzymes (HDAC) which is under development for the treatment of cutaneous T-cell lymphoma.
  4. Sirtuin-1 (SIRT1) activator

    SRT 2183 is a selective Sirtuin-1 (SIRT1) activator with an EC1.5 value of 0.36 μM. SRT 2183 induces growth arrest and apoptosis, concomitant with deacetylation of STAT3 and NF-κB, and reduction of c-Myc protein levels.
  5. dual inhibitor of PRMT4 and PRMT6

    MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively.
  6. KDM4A inhibitor

    Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex, also acts as an inhibitor of KDM4A, with antitumor activity.
  7. HDAC inhibitor

    CRA-026440 is a potent, broad-spectrum HDAC inhibitor.
  8. JAK2/JAK3 inhibitor

    JAK2-IN-4 (compound 16h) is a selective JAK2/JAK3 inhibitor, with IC50 values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively.
  9. G9a inhibitor

    CPUY074020 is a potent G9a inhibitor with an IC50 of 2.18 μM, and possesses anti-proliferative activity .
  10. sirtuin inhibitor

    Sirtinol is a cell-permeable, specific inhibitor of sirtuin NAD-dependant histone deacetylases. It is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively.
  11. HDAC inhibitor

    CXD101 is a class I-selective HDAC inhibitor (HDAC1 (IC50, 63 nM), HDAC2 (IC50, 570 nM), HDAC3 (IC50, 550 nM). CXD101 has no activity against HDAC class II.
  12. PAD inhibitor

    Cl-amidine is a peptidylarginine deminase (PAD) inhibitor, with an IC50 5.9 μM for PAD4.
  13. Sirt1/Sirt2 inhibitor

    Salermide is an inhibitor of Sirt1 and Sirt2; can cause strong cancer-specific apoptotic cell death.
  14. CARM1 inhibitor

    SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 50 nM.
  15. miR-544 inhibitor

    SID 3712249 (MiR-544 Inhibitor 1) is an inhibitor of the biogenesis of microRNA-544 (miR-544).
  16. p53 activator

    Tenovin-6 is a analog of tenovin-1. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 in vitro with IC50 values of 21, 10, and 67 uM, respectively.
  17. p300 inhibitor

    Histone Acetyltransferase Inhibitor II is a potent and cell permeable p300 inhibitor, with an IC50 of 5μM; Histone Acetyltransferase Inhibitor II can be used in cancer research.
  18. SIRT1/SIRT2 inhibitor

    Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 and 59 μM, respectively.
  19. PARP Inhibitor

    AZD2461 is a novel and potent PARP inhibitor with lower affinity to P-glycoprotein.
  20. JAK2 inhibitor

    XL019 is an orally bioavailable inhibitor of Janus-associated kinase 2 (JAK2) with potential antineoplastic activity.
  21. PKC inhibitor

    Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.
  22. EZH2 inhibitor

    EPZ005687 is a potent inhibitor of EZH2 (K(i) of 24 nM)
  23. inhibitor of the BRPF bromodomain

    GSK9311 is a potent inhibitor of the BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively.
  24. HDAC6 inhibitor

    ACY-775 is a potent and selective inhibitor of the of histone deacetylase 6 (HDAC6) with an IC50 of 7.5?nM.
  25. CBP/EP300 Inhibitor

    GNE-272 is a potent and selective in vivo probe for the bromodomains of CBP/EP300 with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively.
  26. HDAC1/HDAC2 inhibitor

    BRD-6929 (Cpd-60) is a brain-penetrant, selective inhibitor of HDAC1 and HDAC2 (IC50=?1 and 8 nM), extracted from patent US2018360927.
  27. SIRT1 inhibitor

    Inauhzin is a potent SIRT inhibitor, which effectively reactivates p53 by inhibiting SIRT1 activity, promotes p53-dependent apoptosis of human cancer cells without causing apparently genotoxic stress.
  28. GSK 4027 is a chemical probe for the PCAF/GCN5 bromodomain with an pIC50 of 7.4??0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
  29. BET inhibitor

    PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4.
  30. Dot1L inhibitor

    Dot1L-IN-1 is a highly potent, selective and structurally novel Dot1L inhibitor with a Ki of 2 pM.
  31. HDAC inhibitor

    Resminostat, also known as RAS2410, is a potent inhibitor of histone deacetylase (HDAC) classes I and II. It binds to and inhibits HDACs leading to an accumulation of highly acetylated histones.
  32. pan-JAK inhibitor

    PF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively.
  33. PRMT1 inhibitor

    MS023 is a potent inihbitor of PRMTs 1,3,4,6,and 8 (IC50 = 30, 119, 83, 8, and 8 nM, respectively), which are responsible for asymmetric dimethylation of arginine residues.
  34. calcineurin inhibitor

    Ascomycin is a potent immunosuppressive agent that could be used as a potential therapeutic agent for autoimmune diseases.
  35. HDAC4 inhibitor

    Tasquinimod is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling.
  36. CBP/P300 benzoxazepine bromodomain inhibitor

    TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
  37. PARP inhibitor

    PJ 34 hydrochloride is a potent inhibitor of poly(ADP-ribose) polymerase (PARP) (EC50 = 20 nM).
  38. JAK2/FLT3 inhibitor

    Pacritinib, also known as SB1518, is an orally bioavailable inhibitor of Janus kinase 2 (JAK2) and the JAK2 mutant JAK2V617F with potential antineoplastic activity. Pacritinib competes with JAK2 for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and so caspase-dependent apoptosis.
  39. Pan PI3K inhibitor

    SF1126 is a water soluble, small-molecule prodrug containing the pan-PI3K/mTOR inhibitor LY294002/SF1101 conjugated to the RGD-containing tetra-peptide SF1174 with potential antineoplastic and antiangiogenic activities.
  40. EZH2 inhibitor

    EI1 is a potent and selective small molecule inhibitor of EZH2 with IC50 values of 15 nM and 13 nM for wild type EZH2 and EZH2 Y641F mutant, respectively.
  41. EZH2 inhibitor

    EPZ-6438 is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. It induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells.
  42. DNA methyltransferase inhibitor

    Zebularine (NSC309132; 4-Deoxyuridine) is a DNA methyltransferase inhibitor.
  43. HDAC inhibitor

    Scriptaid is an HDAC inhibitor (histone deacetylase).
  44. BET Inhibitor

    (+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor.
  45. Demethylase Inhibitor

    GSK J4 is a cell permeable prodrug rapidly hydrolyzed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor; attenuates lipopolysaccharide (LPS)-induced proinflammatory cytokine production in primary human macrophages (IC50 = 9 uM for the inhibition of TNF?? release).
  46. LSD1 inhibitor

    CBB1003 is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
  47. DOT1L Inhibitor

    EPZ-5676 is a small molecule inhibitor of histone methyltransferase with potential antineoplastic activity.
  48. DNMT inhibitor

    SGI-110 is a second generation DNA-hypomethyating agent.
  49. HDAC inhibitor

    Apicidin is a a potent histone deacetylases (HDAC) inhibitor with potential anticancer activity.
  50. PARP2 inhibitor

    UPF 1069 is a selective poly(ADP-ribose) polymerase (PARP) 2 inhibitor (IC50 values are 0.3 and 8.0 μM for PARP-2 and PARP-1 respectively).

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