Histone Demethylase

Sigaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S7070 GSK J4 HCl <1 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 <1 mg/mL 10 mg/mL 2 mg/mL
S7574 GSK-LSD1 2HCl 57 mg/mL 57 mg/mL
S7234 IOX1 <1 mg/mL 37 mg/mL <1 mg/mL
S7795 ORY-1001 (RG-6016) 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
Catalog No. Information Product Use Citations Product Validations
S7070

GSK J4 HCl

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.

S7237

OG-L002

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.

S7281

JIB-04

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.

S7296

ML324

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

S8287New

CPI-455

CPI-455 is a specific KDM5 inhibitor, 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.

S7574

GSK-LSD1 2HCl

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).

S7234

IOX1

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

S7795

ORY-1001 (RG-6016)

ORY-1001 (RG-6016) 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.

S7581

GSK J1

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.

S7796

GSK2879552 2HCl

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

S7680

SP2509

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.

Catalog No. Information Product Use Citations Product Validations
S7070

GSK J4 HCl

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.

S7237

OG-L002

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.

S7281

JIB-04

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.

S7296

ML324

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

S8287New

CPI-455

CPI-455 is a specific KDM5 inhibitor, 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.

S7574

GSK-LSD1 2HCl

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).

S7234

IOX1

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

S7795

ORY-1001 (RG-6016)

ORY-1001 (RG-6016) 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.

S7581

GSK J1

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.

S7796

GSK2879552 2HCl

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

S7680

SP2509

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.