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Histone Demethylase

Isoform-selective Products

KDM1 KDM2 KDM3 KDM4 KDM5 KDM6

Signaling Pathway

Histone Demethylase Products

All (25)
Histone Demethylase Inhibitors (25)
New Histone Demethylase Products

Catalog No.	Product Name	Information	Product Use Citations
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 Cell Biol, 2024, 26(7):1165-1175 J Clin Invest, 2024, 134(1)e163964 Clin Epigenetics, 2024, 16(1):51
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.	Nat Commun, 2024, 15(1):5631 bioRxiv, 2024, 2024.05.19.594897 MedComm (2020), 2023, 4(3):e269
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
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 Commun, 2024, 15(1):7366 Nat Commun, 2024, 15(1):5631 MedComm (2020), 2023, 4(3):e269
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 Commun, 2024, 15(1):5631 Cell Death Discov, 2024, 10(1):166 Nat Cell Biol, 2023, 10.1038/s41556-023-01281-y
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).	Nat Commun, 2024, 15(1):5631 Cell Death Dis, 2023, 10.1038/s41419-023-06238-5 Front Immunol, 2023,
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.	Cancer Cell, 2023, 41(6):1118-1133.e12 mBio, 2022, 13(1):e0337721 iScience, 2022, 25(9):104978
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.	Cell Death Discov, 2024, 10(1):166 bioRxiv, 2024, 2024.05.19.594897 Viruses, 2023, 15(1)163
S7296	ML324	ML324 is a selective inhibitor of jumonji histone demethylase (JMJD2) with IC50 of 920 nM.	Cancer Cell, 2023, 41(6):1118-1133.e12 EBioMedicine, 2023, 92:104602 Viruses, 2023, 15(1)163
S7234	IOX1	IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 is an inhibitor of ALKBH5.	Front Immunol, 2024, 15:1308978 Nat Commun, 2023, 14(1):1161 Nat Commun, 2022, 13(1):1172
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.	Cell Rep Med, 2023, 4(5):101026 Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 J Biol Chem, 2022, S0021-9258(22)00457-4
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.	Oxid Med Cell Longev, 2022, 2022:2405943 Front Cell Dev Biol, 2021, 9:697614 Exp Cell Res, 2021, S0014-4827(21)00315-3
S6389	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.	NPJ Precis Oncol, 2024, 8(1):59 EBioMedicine, 2023, 92:104602 Biomed Pharmacother, 2023, 157:114033
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.	Cell Metab, 2024, S1550-4131(24)00415-7 Cell Rep Med, 2023, 4(5):101026
E0132	NCGC00244536	NCGC00244536 is a novel KDM4 Inhibitor with an IC50 of ∼10 nM.
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.
E1819^New	Zavondemstat	Zavondemstat(QC8222, TACH 101) is a small-molecule pan-inhibitor of histone lysine demethylase 4D (KDM4D) that selectively targets KDM4A-D with no effect on other KDM families. It exhibits potent antiproliferative activity in various cancer cell lines and organoid models. It displays antineoplastic activity and acts as a potential anticancer agent.
S9882	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.
E1793^New	TC-E5002(KDM2/7-IN-1)	TC-E5002(KDM2/7-IN-1) is a selective inhibitor of histone demethylase KDM2/7 subfamily with IC50s of 6.8, 0.2, and 1.2 µM for KDM2A, KDM7A, and KDM7B, respectively. It is selective for the KDM2/7 subfamily over KDM4A, KDM4C, KDM5A, and KDM6A/UTX with IC50s of >120, 83, 55, and 100 µM, respectively. It exhibits antiproliferative activity, indicating its potential as an anticancer agent.
S5772	AS-8351	AS-8351 is a histone demethylase inhibitor that could induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.
S1059	KDM4D-IN-1	KDM4D-IN-1 is a potent inhibitor of KDM4D with an IC50 of 0.41 μM.	Cell Rep Med, 2024, 5(2):101416
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.	Nat Commun, 2024, 15(1):7366
E1733	PBIT	PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. It inhibits JARID1B (KDM5B/PLU1), JARID1Aand JARID1C with an IC50 of 3 μM, 6 μM and 4.9 μM respectively. It is capable of inhibiting the multiplication of breast cancer cell lines expressing high levels of JARIDB1.
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.
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.	Cell Death Discov, 2024, 10(1):166
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 Cell Biol, 2024, 26(7):1165-1175 J Clin Invest, 2024, 134(1)e163964 Clin Epigenetics, 2024, 16(1):51
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.	Nat Commun, 2024, 15(1):5631 bioRxiv, 2024, 2024.05.19.594897 MedComm (2020), 2023, 4(3):e269
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
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 Commun, 2024, 15(1):7366 Nat Commun, 2024, 15(1):5631 MedComm (2020), 2023, 4(3):e269
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 Commun, 2024, 15(1):5631 Cell Death Discov, 2024, 10(1):166 Nat Cell Biol, 2023, 10.1038/s41556-023-01281-y
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).	Nat Commun, 2024, 15(1):5631 Cell Death Dis, 2023, 10.1038/s41419-023-06238-5 Front Immunol, 2023,
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.	Cancer Cell, 2023, 41(6):1118-1133.e12 mBio, 2022, 13(1):e0337721 iScience, 2022, 25(9):104978
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.	Cell Death Discov, 2024, 10(1):166 bioRxiv, 2024, 2024.05.19.594897 Viruses, 2023, 15(1)163
S7296	ML324	ML324 is a selective inhibitor of jumonji histone demethylase (JMJD2) with IC50 of 920 nM.	Cancer Cell, 2023, 41(6):1118-1133.e12 EBioMedicine, 2023, 92:104602 Viruses, 2023, 15(1)163
S7234	IOX1	IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 is an inhibitor of ALKBH5.	Front Immunol, 2024, 15:1308978 Nat Commun, 2023, 14(1):1161 Nat Commun, 2022, 13(1):1172
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.	Cell Rep Med, 2023, 4(5):101026 Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 J Biol Chem, 2022, S0021-9258(22)00457-4
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.	Oxid Med Cell Longev, 2022, 2022:2405943 Front Cell Dev Biol, 2021, 9:697614 Exp Cell Res, 2021, S0014-4827(21)00315-3
S6389	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.	NPJ Precis Oncol, 2024, 8(1):59 EBioMedicine, 2023, 92:104602 Biomed Pharmacother, 2023, 157:114033
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.	Cell Metab, 2024, S1550-4131(24)00415-7 Cell Rep Med, 2023, 4(5):101026
E0132	NCGC00244536	NCGC00244536 is a novel KDM4 Inhibitor with an IC50 of ∼10 nM.
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.
E1819^New	Zavondemstat	Zavondemstat(QC8222, TACH 101) is a small-molecule pan-inhibitor of histone lysine demethylase 4D (KDM4D) that selectively targets KDM4A-D with no effect on other KDM families. It exhibits potent antiproliferative activity in various cancer cell lines and organoid models. It displays antineoplastic activity and acts as a potential anticancer agent.
S9882	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.
E1793^New	TC-E5002(KDM2/7-IN-1)	TC-E5002(KDM2/7-IN-1) is a selective inhibitor of histone demethylase KDM2/7 subfamily with IC50s of 6.8, 0.2, and 1.2 µM for KDM2A, KDM7A, and KDM7B, respectively. It is selective for the KDM2/7 subfamily over KDM4A, KDM4C, KDM5A, and KDM6A/UTX with IC50s of >120, 83, 55, and 100 µM, respectively. It exhibits antiproliferative activity, indicating its potential as an anticancer agent.
S5772	AS-8351	AS-8351 is a histone demethylase inhibitor that could induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.
S1059	KDM4D-IN-1	KDM4D-IN-1 is a potent inhibitor of KDM4D with an IC50 of 0.41 μM.	Cell Rep Med, 2024, 5(2):101416
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.	Nat Commun, 2024, 15(1):7366
E1733	PBIT	PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. It inhibits JARID1B (KDM5B/PLU1), JARID1Aand JARID1C with an IC50 of 3 μM, 6 μM and 4.9 μM respectively. It is capable of inhibiting the multiplication of breast cancer cell lines expressing high levels of JARIDB1.
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.
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.	Cell Death Discov, 2024, 10(1):166
E1819^New	Zavondemstat	Zavondemstat(QC8222, TACH 101) is a small-molecule pan-inhibitor of histone lysine demethylase 4D (KDM4D) that selectively targets KDM4A-D with no effect on other KDM families. It exhibits potent antiproliferative activity in various cancer cell lines and organoid models. It displays antineoplastic activity and acts as a potential anticancer agent.
E1793^New	TC-E5002(KDM2/7-IN-1)	TC-E5002(KDM2/7-IN-1) is a selective inhibitor of histone demethylase KDM2/7 subfamily with IC50s of 6.8, 0.2, and 1.2 µM for KDM2A, KDM7A, and KDM7B, respectively. It is selective for the KDM2/7 subfamily over KDM4A, KDM4C, KDM5A, and KDM6A/UTX with IC50s of >120, 83, 55, and 100 µM, respectively. It exhibits antiproliferative activity, indicating its potential as an anticancer agent.

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