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Histone Demethylase

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Histone Demethylase Signaling Pathway Map

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All (22)
Histone Demethylase Inhibitors (22)
New Histone Demethylase Products

Catalog No.	Product Name	Information	Product Use Citations
E0132^New	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	Pulrodemstat (CC-90011) besylate	Pulrodemstat (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.
S5772	AS-8351	AS-8351 is a histone demethylase inhibitor that could induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.
S6389^New	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.	Cancers (Basel), 2022, 14(6)1537
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.	Nat Immunol, 2022, 23(3):431-445 Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Cell Death Dis, 2022, 13(2):174
S7234	IOX1	IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases.	Nat Commun, 2022, 13(1):1172 Chem Biol Drug Des, 2022, 10.1111/cbdd.14051 Sci Rep, 2021, 11(1):2942
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.	mBio, 2022, 13(1):e0337721 Cancer Biol Ther, 2022, 23(1):65-75 Mol Ther Oncolytics, 2021, 20:583-595
S7296	ML324	ML324 is a selective inhibitor of jumonji histone demethylase (JMJD2) with IC50 of 920 nM.	Cancer Biol Ther, 2022, 23(1):65-75 Cancer Chemother Pharmacol, 2022, 89(5):643-653 Chem Biol Interact, 2022, 353:109806
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 Death Differ, 2022, 10.1038/s41418-022-00983-4 Theranostics, 2022, 12(4):1500-1517 Cancer Chemother Pharmacol, 2022, 89(5):643-653
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.	Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 J Biol Chem, 2022, S0021-9258(22)00457-4 Front Cell Dev Biol, 2021, 9:702462
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.	Biomedicines, 2022, 10(3)638 Invest Ophthalmol Vis Sci, 2022, 63(3):20 Cell Death Dis, 2021, 12(11):993
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.	Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Mol Psychiatry, 2022, 10.1038/s41380-022-01508-8 Cell Rep, 2022, 39(5):110790
S7796	GSK2879552 2HCl	GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with K_i_app of 1.7 μM. Phase 1.	Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Mol Cell, 2021, S1097-2765(21)01037-6 J Neurosci, 2021, JN-RM-3102-20
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 Chem Biol, 2022, 10.1038/s41589-022-00996-7 Oncogene, 2022, 10.1038/s41388-022-02185-1 Cancers (Basel), 2022, 14(6)1537
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
S9882^New	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.
E0132^New	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	Pulrodemstat (CC-90011) besylate	Pulrodemstat (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.
S5772	AS-8351	AS-8351 is a histone demethylase inhibitor that could induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.
S6389^New	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.	Cancers (Basel), 2022, 14(6)1537
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.	Nat Immunol, 2022, 23(3):431-445 Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Cell Death Dis, 2022, 13(2):174
S7234	IOX1	IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases.	Nat Commun, 2022, 13(1):1172 Chem Biol Drug Des, 2022, 10.1111/cbdd.14051 Sci Rep, 2021, 11(1):2942
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.	mBio, 2022, 13(1):e0337721 Cancer Biol Ther, 2022, 23(1):65-75 Mol Ther Oncolytics, 2021, 20:583-595
S7296	ML324	ML324 is a selective inhibitor of jumonji histone demethylase (JMJD2) with IC50 of 920 nM.	Cancer Biol Ther, 2022, 23(1):65-75 Cancer Chemother Pharmacol, 2022, 89(5):643-653 Chem Biol Interact, 2022, 353:109806
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 Death Differ, 2022, 10.1038/s41418-022-00983-4 Theranostics, 2022, 12(4):1500-1517 Cancer Chemother Pharmacol, 2022, 89(5):643-653
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.	Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 J Biol Chem, 2022, S0021-9258(22)00457-4 Front Cell Dev Biol, 2021, 9:702462
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.	Biomedicines, 2022, 10(3)638 Invest Ophthalmol Vis Sci, 2022, 63(3):20 Cell Death Dis, 2021, 12(11):993
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.	Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Mol Psychiatry, 2022, 10.1038/s41380-022-01508-8 Cell Rep, 2022, 39(5):110790
S7796	GSK2879552 2HCl	GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with K_i_app of 1.7 μM. Phase 1.	Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Mol Cell, 2021, S1097-2765(21)01037-6 J Neurosci, 2021, JN-RM-3102-20
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 Chem Biol, 2022, 10.1038/s41589-022-00996-7 Oncogene, 2022, 10.1038/s41388-022-02185-1 Cancers (Basel), 2022, 14(6)1537
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
S9882^New	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.
E0132^New	NCGC00244536	NCGC00244536 is a novel KDM4 Inhibitor with an IC50 of ∼10 nM.
S6389^New	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.	Cancers (Basel), 2022, 14(6)1537
S9882^New	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.