Histone Demethylase

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Histone Demethylase Inhibitors (9)


Cat.No. Product Name Information Product Use Citation Customer Product Validation
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.
  • Nat Med, 2015, 10.1038/nm.3855
  • Virology, 2015, 482:244-59
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.
  • Virology, 2015, 482:244-259
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.
S7234 IOX1 IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases.
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.
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.
S7296 ML324 ML324 is a selective inhibitor of jumonji histone demethylase (JMJD2) with IC50 of 920 nM.
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).
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.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
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
S7234 IOX1 <1 mg/mL 37 mg/mL <1 mg/mL
S7680 SP2509 <1 mg/mL 38 mg/mL <1 mg/mL
S7795 ORY-1001 (RG-6016) 61 mg/mL 5 mg/mL 4 mg/mL
S7296 ML324 <1 mg/mL 43 mg/mL 3 mg/mL
S7574 GSK-LSD1 2HCl 57 mg/mL 57 mg/mL
S7581 GSK J1 <1 mg/mL 77 mg/mL <1 mg/mL
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