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Histone Demethylase

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Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S7070 GSK-J4 Hydrochloride 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.
Mol Cell, 2025, 85(15):2973-2987.e6
Nat Cell Biol, 2024, 26(7):1165-1175
J Clin Invest, 2024, 134(24)e173403
Verified customer review of GSK-J4 Hydrochloride
S7680 SP2509 SP2509 (HCI-2509) 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. This compound induces apoptosis and promotes autophagy.
Cell Death Discov, 2025, 11(1):380
Cancer Res Commun, 2025, 5(9):1584-1598
bioRxiv, 2025, 2025.06.20.660795
Verified customer review of SP2509
S8287 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.
Nature, 2023, 622(7983):619-626
Nature, 2023, 622(7983):619-626
Cancer Cell, 2023, 41(6):1118-1133.e12
S7795 Ladademstat (ORY-1001) Dihydrochloride 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.
EMBO Rep, 2025, 10.1038/s44319-025-00385-w
Nat Commun, 2024, 15(1):5631
Cell Death Discov, 2024, 10(1):166
Verified customer review of Ladademstat (ORY-1001) Dihydrochloride
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).
Nature, 2025, 10.1038/s41586-025-08915-1
Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z
Front Cell Dev Biol, 2025, 13:1566567
S7281 JIB-04 JIB-04 (NSC 693627) 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. This compound also induces cell apoptosis.
Mol Cell, 2025, 85(15):2973-2987.e6
J Immunother Cancer, 2025, 13(10)e013269
Front Cell Dev Biol, 2025, 13:1566567
Verified customer review of JIB-04
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.
Cancer Res Commun, 2025, 5(9):1584-1598
bioRxiv, 2025, 2025.06.20.660795
Cell Death Discov, 2024, 10(1):166
Verified customer review of OG-L002
S7296 ML324 ML324 is a selective inhibitor of jumonji histone demethylase (JMJD2) with IC50 of 920 nM.
Mol Cell, 2025, 85(15):2973-2987.e6
Cancer Cell, 2023, 41(6):1118-1133.e12
EBioMedicine, 2023, 92:104602
S7234 IOX1 IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. This compound is an inhibitor of ALKBH5.
Mol Cell, 2025, 85(15):2973-2987.e6
Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z
Front Immunol, 2024, 15:1308978
S7581 GSK J1 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.
Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z
Commun Biol, 2025, 8(1):269
Chem Biol Interact, 2025, 418:111576

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