Histone Demethylase

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S7070 GSK J4 HCl 90 mg/mL 90 mg/mL 90 mg/mL
S7237 OG-L002 <1 mg/mL 45 mg/mL 19 mg/mL
S7281 JIB-04 <1 mg/mL 25 mg/mL <1 mg/mL
S7296 ML324 <1 mg/mL 43 mg/mL 3 mg/mL
S8287 CPI-455 HCl <1 mg/mL 10 mg/mL 2 mg/mL
S4800 Daminozide -1 mg/mL 32 mg/mL -1 mg/mL
S7574 GSK-LSD1 2HCl 57 mg/mL 57 mg/mL -1 mg/mL
S7234 IOX1 <1 mg/mL 37 mg/mL <1 mg/mL
S7795 ORY-1001 (RG-6016) 2HCl 61 mg/mL 5 mg/mL 4 mg/mL
S7581 GSK J1 <1 mg/mL 77 mg/mL <1 mg/mL
S7796 GSK2879552 2HCl 44 mg/mL 29 mg/mL <1 mg/mL
S7680 SP2509 <1 mg/mL 38 mg/mL <1 mg/mL
S8601 CP2 100 mg/mL -1 mg/mL -1 mg/mL
Catalog No. Information Product Use Citations Product Validations


GSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family.



OG-L002 is a potent and specific LSD1 inhibitor with IC50 of 20 nM in a cell-free assay, exhibiting 36- and 69-fold selectivity over MAO-B and MAO-A, respectively.



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 in cell-free assays, respectively.



ML324 is a selective inhibitor of jumonji histone demethylase (JMJD2) with IC50 of 920 nM.


CPI-455 HCl

CPI-455 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.



Daminozide, a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily with IC50 of 1.5±0.7 μM for KDM2A. It is at least 100-fold selective as an inhibitor of the KDM2/7 subfamily over the other demethylase subfamily members tested, with IC50s of 2 μM or less against KDM2A, PHF8, and KIAA1718 and IC50s of 127 μM for KDM3A or greater (mM range) against other demethylases.



GSK-LSD1 2HCl is an irreversible, and selective LSD1 inhibitor with IC50 of 16 nM, > 1000 fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B).



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


ORY-1001 (RG-6016) 2HCl

ORY-1001 (RG-6016) 2HCl is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor with IC50 of <20 nM, with high selectivity against related FAD dependent aminoxidases. Phase 1.



GSK-J1 is a highly potent H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM in cell-free assays for JMJD3 (KDM6B) and UTX (KDM6A), respectively, >10-fold selectivity over other tested demethylases.


GSK2879552 2HCl

GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1.



SP2509 is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase.



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.