Histone Demethylases

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  1. 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.
  2. 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).
  3. plant growth regulator

    Daminozide(DMASA; DIMG; B 995), a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily.
  4. Histone demethylase inhibitor

    GSK J1 is a potent and selective inhibitor of the H3K27 histone demethylases JMJD3 and UTX
  5. LSD1 inhibitor

    OG-L002 is a potent and specific LSD1 inhibitor with IC50 of 20 nM, exhibiting 36- and 69-fold selectivity over MAO-B and MAO-A, respectively.
  6. LSD1/BHC110 & MAO inhibitor

    Tranylcypromine hydrochloride is a non-selective MAO-A/B inhibitor.
  7. Histone Demethylase inhibitor

    JIB-04 is a pan-selective Jumonji histone demethylase inhibitor with IC50 of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.
  8. 2OG oxygenases Inhibitor

    IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases.
  9. JARID1 inhibitor

    PBIT is a reversible, cell-permeable inhibitor of JARID1 family demethylases (IC50s = 6, 3, 4.9, and 28 uM for JARID1A, JARID1B, JARID1C, and JARID1D, respectively).
  10. LSD1 inhibitor

    SP2509 is a novel histone demethylase LSD1 (KDM1A) antagonist with IC50 of 13 nM; no inhibition on MAO-A and MAO-B.
  11. LSD1 inhibitor

    GSK2879552 is an orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
  12. JMJD2 inhibitor?€?

    ML-324 is a potent JMJD2 demethylase inhibitor with demonstrated antiviral activity.
  13. KDM5 demethylases inhibitor

    CPI 4203 is a selective inhibitor of KDM5 demethylases, structurally related to CPI 455 but ~25-fold less potent (IC50 value 250 nM for inhibition of full length KDM5A).
  14. KDM5 inhibitor

    CPI 455 possesses the target specificity required for an in vitro tool compound for exploring KDM5-dependent disease biology, including drug tolerance.
  15. KDM5 inhibitor.

    AS8351 is a histone demethylase inhibitor.
  16. KDM inhibitor

    2,4-Pyridinedicarboxylic Acid (2,4-PDCA) is an inhibitor of histone lysine-specific demethylases that targets on JMJD2A (KDM4A), KDM4C, KDM4E (IC50, 1.4 μM), KDM5B (IC50, 3 μM), KDM6A and other 2-oxogynases.
  17. Procaine hydrochloride is a local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block.
  18. Eicosapentaenoic Acid (EPA; Timnodonic acid) is an omega-3 fatty acid.
  19. LSD1 inhibitor

    S 2101 is a lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s.
  20. LSD1 inhibitor

    Seclidemstat (SP-2577) is a potent and orally bioavailable LSD1 inhibitor, with a mean IC50 of 127 nM.
  21. KDM1A/LSD1 inhibitor

    ORY-1001 trans is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.
  22. LSD1 inhibitor

    GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC50 of 16 nM.
  23. Jumonji histone demethylase inihibitor

    Z-JIB-04 (NSC 693627, JIB-04 Z-isomer) is an isomer of JIB-04. JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50 of 230 nM, 340 nM, 855 nM, 445 nM, 435 nM, 1100 nM and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.
  24. epigenetic modifier

    L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium, L-2-Hydroxyglutarate disodium, LGA, L-2HG) is an epigenetic modifier and a putative oncometabolite in kidney cancer that inhibits histone demethylases and hence promotes histone methylation.

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