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Histone Demethylases(组蛋白去甲基化酶)

Histone demethylases are a diverse group of enzymes catalyzing a process to reverse histone methylation, in which methyl (CH3-) groups are removed from instead of being transferred to histone.  So far, two evolutionarily conserved histone demethylase families have been identified, including LSD demethylases and JMJC demethylases. LSD1 and LSD2 are two well-established members of LSD demethylase family, which catalyze demethylation through a flavin adenine dinucleotide (FAD)-dependent amine oxidation reaction. LSD1 has been found to demethylate H3K4mel, H3K4me2, H3K9me1, H3K9me2 and a few non-histone targets; while LSD2 has been found to demethylate only H3K4me1 and H3K4me2. Members of JMJC demethylase family is characterized by containing the catalytic JMJC domain, which demethylate substrates, including H3K4, H3K9, H3K27, H3K36 and H4K20, through a Fe(II)- and α-ketogutarate-dependent dioxygenase reaction.

  1. Cat.No. 产品名称 Information
  2. GC25305 CPI-455 HCl CPI-455 HCl is a specific KDM5 inhibitor with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!
  3. GC25304 CP2 CP2 is a cyclic peptide that inhibits the JmjC histone demethylases KDM4 with IC50 values of 42 nM and 29 nM for KDM4A and KDM4C, respectively.
  4. GC67921 Bomedemstat ditosylate
  5. GC65879 Bomedemstat hydrochloride
  6. GC65456 T-448
  7. GC65254 MC4355
  8. GC65138 NCDM-32B
  9. GC64902 S2157
  10. GC64865 Bomedemstat
  11. GC64841 JQKD82 trihydrochloride
  12. GC64303 S2116
  13. GC63456 Seclidemstat mesylate
  14. GC63437 TAK-418
  15. GC49116 Prohexadione A plant growth regulator
  16. GC62719 GSK2879552 dihydrochloride An LSD1 inhibitor
  17. GC62678 PFI-90 PFI-90 is a selective inhibitor of the histone demethylase KDM3B. PFI-90 induces apoptosis and cell differentiation resulting in delayed tumor progression in vivo.
  18. GC62434 LSD1/HDAC6-IN-1
  19. GC47586 Lysine-specific Demethylase Inhibitor (1C) (hydrochloride) An LSD1 inhibitor
  20. GC60004 (rel)-Tranylcypromine D5 hydrochloride
  21. GC50136 NSC 636819 NSC 636819 是 KDM4A/KDM4B 的竞争性和选择性抑制剂。 KDM4A/KDM4B 是前列腺癌的潜在进展因素。 NSC 636819 具有研究癌症疾病,尤其是前列腺癌的潜力。
  22. GC38709 KDOAM-25 citrate
  23. GC37956 YUKA1
  24. GC36818 ORY-1001(trans)
  25. GC36485 LSD1-IN-6
  26. GC36484 LSD1-IN-5
  27. GC36389 KDM4-IN-2
  28. GC36388 KDM2A/7A-IN-1
  29. GC36195 GSK-J1 lithium salt GSK-J1 is a highly potent inhibitor of H3K27 histone demethylase JMJD3 (KDM6B) and UTX (KDM6A) with IC50 of 60 nM in cell-free assays for JMJD3 (KDM6B) , respectively, >10-fold selectivity over other tested demethylases, with IC50 of 0.95μM and 1.76μM towards JARID1B/C.
  30. GC35624 CBB1007 trihydrochloride
  31. GC35623 CBB1007 hydrochloride
  32. GC35622 CBB1003 hydrochloride
  33. GC35621 CBB1003
  34. GC44184 Methylstat (hydrate) A cell-permeable demethylase inhibitor
  35. GC43794 GSK-J5 (hydrochloride) A negative control compound for GSK-J4
  36. GC43792 GSK-J2 (sodium salt) A negative control compound for GSK-J1
  37. GC42075 2,4-Pyridinedicarboxylic Acid (hydrate) An inhibitor of 2-oxoglutarate-dependent enzymes
  38. GC34604 GSK467 GSK467 is a cell penetrant and selective inhibitor of KDM5B (JARID1B/PLU1) with Ki of 10 nM. GSK467 shows apparent 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other JmJ family members.
  39. GC34314 GSK 690 Hydrochloride
  40. GC34296 DDP-38003 trihydrochloride
  41. GC34165 Corin
  42. GC33339 S 2101
  43. GC33038 T-3775440 hydrochloride T-3775440 HCl is an irreversible LSD1 inhibitor that is highly selective for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B), with an IC50 value of 2.1 nmol/L.
  44. GC33013 DDP-38003 dihydrochloride
  45. GC32896 NCGC00247743
  46. GC32842 KDM5A-IN-1
  47. GC32820 Seclidemstat (SP-2577) Seclidemstat (SP-2577) is a potent and orally bioavailable inhibitor of lysine-specific demethylase 1 (LSD1/KDM1A) with IC50 of 13 nM. Seclidemstat (SP-2577) has potential antineoplastic activity.
  48. GC32790 KDM5-IN-1
  49. GC32764 GSK-LSD1 Dihydrochloride An LSD1 inhibitor
  50. GC32699 QC6352
  51. GC31887 KDM4D-IN-1 KDM4D-IN-1 is a potent inhibitor of KDM4D with an IC50 of 0.41 μM.

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