Histone Demethylase

Choose Selective Histone Demethylase Inhibitors

Histone Demethylase Signaling Pathway Map

Histone Demethylase Signaling Pathways

Histone Demethylase Products

  • All (23)
  • Histone Demethylase Inhibitors (23)
  • New Histone Demethylase Products
Catalog No. Product Name Information Product Use Citations Product Validations
E0132New NCGC00244536

NCGC00244536 is a novel KDM4 Inhibitor with an IC50 of ∼10 nM.

S0201 Z-JIB-04 (NSC 693627) Z-JIB-04 (NSC 693627, JIB-04 Z-isomer) is an isomer of JIB-04. JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50 of 230 nM, 340 nM, 855 nM, 445 nM, 435 nM, 1100 nM and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.
S0269 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.
S0356 CC-90011 besylate CC-90011 besylate (LSD1-IN-7 benzenesulfonate) is a potent and orally active lysine specific demethylase-1 (LSD1) inhibitor that is found to be effective in various tumors.
S1059 KDM4D-IN-1 KDM4D-IN-1 is a potent inhibitor of KDM4D with an IC50 of 0.41 μM.
S1325 L-2-Hydroxyglutaric acid disodium

L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium, L-2-Hydroxyglutarate disodium, LGA, L-2HG) is an epigenetic modifier and a putative oncometabolite in kidney cancer that inhibits histone demethylases and hence promotes histone methylation. L-2-Hydroxyglutaric acid disodium is also an inhibitor of mitochondrial creatine kinase (Mi-CK) with Km and Ki of 2.52 mM and 11.13 mM, respectively.

S4800 Daminozide Daminozide (Aminozide, DMASA, DIMG, B 995, Alar, Kylar, B-NINE, SADH), 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.
S5772 AS-8351 AS-8351 is a histone demethylase inhibitor that could induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.
S6389New CPI-455

CPI-455 is a specific KDM5 inhibitor with an IC50 of 10 nM for full-length KDM5A in enzymatic assays. CPI-455 shows over 200-fold selectivity for KDM5 relative to KDM2, 3, 4, 6, and 7 enzymes.

S7070 GSK J4 HCl (GSKJ4 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.
Mol Cell, 2021, 81(10):2183-2200.e13
Nat Commun, 2021, 12(1):7216
Nat Commun, 2021, 12(1):7204
S7234 IOX1 IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases.
Sci Rep, 2021, 11(1):2942
Mol Cell, 2019, 76(6):885-895
J Biol Chem, 2019, 294(23):9186-9197
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.
Sci Rep, 2021, 11(1):10285
Nat Genet, 2020, 52(10):1011-1017
Sci Rep, 2020, 10(1):377
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. JIB‑04 also induces cell apoptosis.
Mol Ther Oncolytics, 2021, 20:583-595
Sci Rep, 2021, 11(1):2942
Research Square, 2021, 10.21203/rs.3.rs-620216/v1
S7296 ML324 ML324 is a selective inhibitor of jumonji histone demethylase (JMJD2) with IC50 of 920 nM.
Chem Biol Interact, 2022, 353:109806
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
ACS Infect Dis, 2020, 8;6(5):1058-1075
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).
Cell Res, 2021, 1-13
Pharmacol Res, 2021, S1043-6618(21)00348-0
Int Immunopharmacol, 2021, 91:107324
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.
Front Cell Dev Biol, 2021, 9:702462
Leukemia, 2021, 10.1038/s41375-021-01121-8
Cell Death Dis, 2020, 11(10):927
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. SP2509 induces apoptosis and promotes autophagy.
Cell Death Dis, 2021, 12(11):993
Front Cell Dev Biol, 2021, 9:694071
Acta Biochim Biophys Sin (Shanghai), 2021, gmab083
S7795 Iadademstat (ORY-1001) 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.
FASEB J, 2022, 36(1):e22122
Theranostics, 2021, 11(14):6983-7004
Cell Death Dis, 2021, 12(11):993
S7796 GSK2879552 2HCl GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1.
Mol Cell, 2021, S1097-2765(21)01037-6
J Neurosci, 2021, JN-RM-3102-20
Front Cell Dev Biol, 2021, 9:694071
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.
Nat Cell Biol, 2021, 23(7):771-781
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
S8438 T-3775440 HCl 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.
S8601 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.
Front Cell Dev Biol, 2021, 9:697614
Exp Cell Res, 2021, S0014-4827(21)00315-3
Int Immunopharmacol, 2020, 1;83:106438
S9882New 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.
E0132New NCGC00244536

NCGC00244536 is a novel KDM4 Inhibitor with an IC50 of ∼10 nM.

S0201 Z-JIB-04 (NSC 693627) Z-JIB-04 (NSC 693627, JIB-04 Z-isomer) is an isomer of JIB-04. JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50 of 230 nM, 340 nM, 855 nM, 445 nM, 435 nM, 1100 nM and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.
S0269 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.
S0356 CC-90011 besylate CC-90011 besylate (LSD1-IN-7 benzenesulfonate) is a potent and orally active lysine specific demethylase-1 (LSD1) inhibitor that is found to be effective in various tumors.
S1059 KDM4D-IN-1 KDM4D-IN-1 is a potent inhibitor of KDM4D with an IC50 of 0.41 μM.
S1325 L-2-Hydroxyglutaric acid disodium

L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium, L-2-Hydroxyglutarate disodium, LGA, L-2HG) is an epigenetic modifier and a putative oncometabolite in kidney cancer that inhibits histone demethylases and hence promotes histone methylation. L-2-Hydroxyglutaric acid disodium is also an inhibitor of mitochondrial creatine kinase (Mi-CK) with Km and Ki of 2.52 mM and 11.13 mM, respectively.

S4800 Daminozide Daminozide (Aminozide, DMASA, DIMG, B 995, Alar, Kylar, B-NINE, SADH), 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.
S5772 AS-8351 AS-8351 is a histone demethylase inhibitor that could induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.
S6389New CPI-455

CPI-455 is a specific KDM5 inhibitor with an IC50 of 10 nM for full-length KDM5A in enzymatic assays. CPI-455 shows over 200-fold selectivity for KDM5 relative to KDM2, 3, 4, 6, and 7 enzymes.

S7070 GSK J4 HCl (GSKJ4 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.
Mol Cell, 2021, 81(10):2183-2200.e13
Nat Commun, 2021, 12(1):7216
Nat Commun, 2021, 12(1):7204
S7234 IOX1 IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases.
Sci Rep, 2021, 11(1):2942
Mol Cell, 2019, 76(6):885-895
J Biol Chem, 2019, 294(23):9186-9197
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.
Sci Rep, 2021, 11(1):10285
Nat Genet, 2020, 52(10):1011-1017
Sci Rep, 2020, 10(1):377
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. JIB‑04 also induces cell apoptosis.
Mol Ther Oncolytics, 2021, 20:583-595
Sci Rep, 2021, 11(1):2942
Research Square, 2021, 10.21203/rs.3.rs-620216/v1
S7296 ML324 ML324 is a selective inhibitor of jumonji histone demethylase (JMJD2) with IC50 of 920 nM.
Chem Biol Interact, 2022, 353:109806
Br J Cancer, 2021, 10.1038/s41416-021-01441-7
ACS Infect Dis, 2020, 8;6(5):1058-1075
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).
Cell Res, 2021, 1-13
Pharmacol Res, 2021, S1043-6618(21)00348-0
Int Immunopharmacol, 2021, 91:107324
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.
Front Cell Dev Biol, 2021, 9:702462
Leukemia, 2021, 10.1038/s41375-021-01121-8
Cell Death Dis, 2020, 11(10):927
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. SP2509 induces apoptosis and promotes autophagy.
Cell Death Dis, 2021, 12(11):993
Front Cell Dev Biol, 2021, 9:694071
Acta Biochim Biophys Sin (Shanghai), 2021, gmab083
S7795 Iadademstat (ORY-1001) 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.
FASEB J, 2022, 36(1):e22122
Theranostics, 2021, 11(14):6983-7004
Cell Death Dis, 2021, 12(11):993
S7796 GSK2879552 2HCl GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1.
Mol Cell, 2021, S1097-2765(21)01037-6
J Neurosci, 2021, JN-RM-3102-20
Front Cell Dev Biol, 2021, 9:694071
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.
Nat Cell Biol, 2021, 23(7):771-781
Hepatology, 2021, 10.1002/hep.32245
Hepatology, 2021, 10.1002/hep.32245
S8438 T-3775440 HCl 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.
S8601 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.
Front Cell Dev Biol, 2021, 9:697614
Exp Cell Res, 2021, S0014-4827(21)00315-3
Int Immunopharmacol, 2020, 1;83:106438
S9882New 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.
E0132New NCGC00244536

NCGC00244536 is a novel KDM4 Inhibitor with an IC50 of ∼10 nM.

S6389New CPI-455

CPI-455 is a specific KDM5 inhibitor with an IC50 of 10 nM for full-length KDM5A in enzymatic assays. CPI-455 shows over 200-fold selectivity for KDM5 relative to KDM2, 3, 4, 6, and 7 enzymes.

S9882New 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.