Histone Demethylases
Histone demethylases are a diverse group of enzymes catalyzing a process to reverse histone methylation, in which methyl (CH3-) groups are removed from instead of being transferred to histone. So far, two evolutionarily conserved histone demethylase families have been identified, including LSD demethylases and JMJC demethylases. LSD1 and LSD2 are two well-established members of LSD demethylase family, which catalyze demethylation through a flavin adenine dinucleotide (FAD)-dependent amine oxidation reaction. LSD1 has been found to demethylate H3K4mel, H3K4me2, H3K9me1, H3K9me2 and a few non-histone targets; while LSD2 has been found to demethylate only H3K4me1 and H3K4me2. Members of JMJC demethylase family is characterized by containing the catalytic JMJC domain, which demethylate substrates, including H3K4, H3K9, H3K27, H3K36 and H4K20, through a Fe(II)- and α-ketogutarate-dependent dioxygenase reaction.
Products for Histone Demethylases
- Cat.No. Product Name Information
- GC60004 (rel)-Tranylcypromine D5 hydrochloride Tranylcypromine-d5 (SKF 385-d5) hydrochloride is a deuterium labeled (rel)-Tranylcypromine hydrochloride.
- GC11873 2,4-Pyridinedicarboxylic Acid 2,4-Pyridinedicarboxylic Acid (2,4 pyridine dicarboxylic acid) is a broad-spectrum inhibitor of 2OG oxygenase, including JmjC domain-containing family of histone demethylases (JHDMs). 2,4-Pyridinedicarboxylic Acid is a target chemical in the field of bio-based plastics.
- GC42075 2,4-Pyridinedicarboxylic Acid (hydrate) 2,4-Pyridinedicarboxylic Acid (2,4-PDCA) is a compound that structurally mimics 2-oxoglutarate (2-OG, also known as α-ketoglutarate) and chelates zinc, thus affecting a range of enzymes.
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GC12961
Apicidin
A cell-permeable HDAC inhibitor
- GC17820 AS8351 histone demethylase inhibitor
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GC18159
BAY-598
A potent and selective SMYD2 inhibitor
- GC16114 Bizine LSD1 inhibitor
- GC64865 Bomedemstat Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.
- GC67921 Bomedemstat ditosylate
- GC65879 Bomedemstat hydrochloride Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.
- GC35621 CBB1003 CBB1003 is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
- GC35622 CBB1003 hydrochloride CBB1003 Hcl is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
- GC14151 CBB1007 LSD1 inhibitor,potent and selective
- GC35623 CBB1007 hydrochloride CBB1007 Hcl is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
- GC35624 CBB1007 trihydrochloride CBB1007 trihydrochloride is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
- GC34165 Corin Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histone deacetylase (HDAC), with a Ki(inact) of 110 nM for LSD1 and an IC50 of 147 nM for HDAC1.
- GC25304 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.
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GC10774
CPI-455
KDM5 inhibitor
- GC25305 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.This product has poor solubility, animal experiments are available, cell experiments please choose carefully!
- GC15830 Daminozide Selective inhibitor of KDM2/7 histone demethylases
- GC33013 DDP-38003 dihydrochloride DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
- GC34296 DDP-38003 trihydrochloride DDP-38003 trihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
- GC34314 GSK 690 Hydrochloride GSK 690 (Hydrochloride) is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a Kd value of 9 nM and a biochemical IC50 of 37 nM.
- GC10617 GSK J1 A dual inhibitor of JMJD3 and UTX
- GC13086 GSK J2 inactive control of GSK J1, JMJD3 (KDM6B) and UTX (KDM6A) inhibitor
- GC12997 GSK J4 free base GSK J4 free base is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK J4 free base inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable prodrug of GSK-J1. GSK J4 free base induces endoplasmic reticulum stress-related apoptosis.
- GC15497 GSK J4 HCl Prodrug of a selective H3K27 histone demethylase inhibitor
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GC17118
GSK J5
inactive isomer of GSK J4, KDM inhibitor
- GC36195 GSK-J1 lithium salt GSK-J1 lithium salt is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
- GC43792 GSK-J2 (sodium salt) The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.
- GC43794 GSK-J5 (hydrochloride) The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.
- GC18012 GSK-LSD1 (hydrochloride) LSD1 inhibitor
- GC15368 GSK-LSD1 2HCl irreversible, and selective LSD1 inhibitor
- GC32764 GSK-LSD1 Dihydrochloride An LSD1 inhibitor
- GC11578 GSK2879552 Novel and irreversible LSD1 inhibitor
- GC62719 GSK2879552 dihydrochloride GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.
- GC34604 GSK467 GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a Ki of 10 nM and an IC50 of 26 nM. GSK467 shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members.
- GC17754 IOX 1 histone demethylase JMJD inhibitor
- GC15603 JIB-04 Jumonji histone demethylase inihibitor
- GC64841 JQKD82 trihydrochloride JQKD82 (JADA82) trihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 trihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma.
- GC36388 KDM2A/7A-IN-1 KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16?μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases.
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GC69327
KDM2B-IN-4
KDM2B-IN-4 is a histone demethylase KDM2B inhibitor. It can be used for cancer research. For more information, please refer to compound 182b in patent document WO2016112284A1.
- GC36389 KDM4-IN-2 KDM4-IN-2 (Compound 19a) is a potent and selective KDM4/KDM5 dual inhibitor with Kis of 4 and 7?nM for KDM4A and KDM5B, respectively.
- GC31887 KDM4D-IN-1 KDM4D-IN-1 is a new histone lysine demethylase 4D (KDM4D) inhibitor with an IC50 value of 0.41±0.03 μM.
- GC32790 KDM5-IN-1 KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
- GC32842 KDM5A-IN-1 KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).
- GC38709 KDOAM-25 citrate KDOAM-25 citrate is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.
- GC36484 LSD1-IN-5 LSD1-IN-5 (Compound 4e) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 121 nM. LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1.
- GC36485 LSD1-IN-6 LSD1-IN-6 (Compound 4m) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 123 nM. LSD1-IN-6 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1.
- GC62434 LSD1/HDAC6-IN-1 LSD1/HDAC6-IN-1 is an orally active dual inhibitor of lysine specific demethylase 1(LSD1)/Histone deacetylase 6 (HDAC6), with anti-tumor activity. LSD1/HDAC6-IN-1 can be used for the research of multiple myeloma (MM).
- GC13534 Lysine-specific Demethylase Inhibitor (1C) lysine-specific demethylase Inhibitor
- GC47586 Lysine-specific Demethylase Inhibitor (1C) (hydrochloride) An LSD1 inhibitor
- GC65254 MC4355 MC4355 is a dual inhibitor of EZH2 and histone deacetylase (HDAC).
- GC44184 Methylstat (hydrate) Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability.
- GC12557 ML324 JMJD2 demethylase inhibitor, potent and cell-permeable
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GC12458
N-Oxalylglycine
cell permeable inhibitor of α-ketoglutarate-dependent enzymes, including JMJD2A, JMJD2C, and JMJD2E.
- GC65138 NCDM-32B NCDM-32B is a potent and selective KDM4 inhibitor that impaires viability and transforming phenotypes of breast cancer.
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GC19410
NCGC00244536
NCGC00244536 is a potent KDM4B inhibitor with an IC50 of 10 nM
- GC32896 NCGC00247743 NCGC00247743 is a histone lysine demethylase KDM4 inhibitor.
- GC50136 NSC 636819 KDM4A/KDM4B inhibitor
- GC17314 OG-L002 LSD1 inhibitor,potent and specific
- GC11792 OG-L002 HCl LSD1 inhibitor,potent and specific
- GC36818 ORY-1001(trans) Iadademstat (ORY-1001) dihydrochloride is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.
- GC15301 PBIT JARID1 family demethylases inhibitor
- GC62678 PFI-90 PFI-90 is a selective inhibitor of histone demethylase (KDM3B) that inhibits PAX3-FOXO1 action. PFI-90 induces apoptosis and myogenic differentiation, resulting in the cell death increased. PFI-90 has the potential for the antitumor activity. (patent WO2021101929A1).
- GC14066 Procaine Sodium channel inhibitor
- GC44685 Procaine (hydrochloride) Procaine (hydrochloride) is an analytical reference standard categorized as a local anesthetic that is used as an adulterant.
- GC49116 Prohexadione A plant growth regulator
- GC32699 QC6352 QC6352 is an orally available, selective and potent KDM4C inhibitor with an IC50 of 35 nM.
- GC10148 RN 1 dihydrochloride LSD1 inhibitor, potent and selective
- GC16743 RN-1 (hydrochloride) LSD1 inhibitor
- GC33339 S 2101 S 2101 is a lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s.
- GC64303 S2116 S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice.
- GC64902 S2157 S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells.
- GC32820 Seclidemstat (SP-2577) Seclidemstat (SP-2577) is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat (SP-2577) promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat (SP-2577) can be used for the research of Ewing Sarcoma.
- GC63456 Seclidemstat mesylate Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma.
- GC14631 SP2509 Demethylase 1 (LSD1) antagonist, novel Lysine-specific
- GC33038 T-3775440 hydrochloride T-3775440 (hydrochloride) is an irreversible lysine-specific histone demethylase (LSD1) inhibitor with an IC50 value of 2.1 nM.
- GC65456 T-448 T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM.
- GC63437 TAK-418 TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC50 of 2.9 nM.
- GC10319 TC-E 5002 TC-E 5002 (TC-E 5002) is a selective histone demethylase KDM2/7 subfamily inhibitor (IC50 values are 0.2, 1.2, 6.8, 55, 83, >100 and >120 μM for KDM7A, KDM7B, KDM2A, KDM5A, KDM4C, KDM6A and KDM4A respectively). TC-E 5002 inhibits growth of HeLa and KYSE-150 cancer cells in vitro.
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GC70033
TK-129
TK-129 is an orally effective, low-toxicity and potent KDM5B inhibitor (with high affinity; IC50=44 nM). TK-129 exerts a cardioprotective effect by inhibiting KDM5B and blocking the KDM5B-related Wnt pathway. In vitro, TK-129 reduces the activation of cardiac fibroblasts induced by Ang II, while in vivo it reduces myocardial remodeling and fibrosis induced by isoproterenol. TK-129 can be used for research on cardiovascular diseases.
- GC11576 Tranylcypromine (2-PCPA) HCl (1S,2R)-Tranylcypromine ((1S,2R)-SKF 385) hydrochloride is a potent antidepressant agent.
- GC30766 Tranylcypromine hemisulfate (dl-Tranylcypromine hemisulfate) Tranylcypromine (SKF 385) hemisulfate is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression.
- GC13919 Tranylcypromine hydrochloride LSD1/BHC110 and monoamine oxidase (MAO) inhibitor
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GC37956
YUKA1
YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM, less active on KDM5C (IC50, 7.12 μM), and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 increases H3K4me3 levels in human cells with anti-cancer activity.
- GC18623 α-Hydroxyglutaric Acid α-Hydroxyglutaric acid (2-HG) is an α-hydroxy acid.