1. Signaling Pathways
  2. Epigenetics
  3. Histone Demethylase

Histone Demethylase

Demethylase

There are two classes of enzymes involved in histone methylation: methyltransferases and demethylases. While methyltransferases are responsible for establishing methylation patterns, demethylases are capable of removing methyl groups not only from histones but other proteins as well. Histone demethylases not only target methylated sites on histone tails but also interact with methylated sites on non-histone proteins, such as p53.

Histone lysine demethylases (KDMs) are of interest as drug targets due to their regulatory roles in chromatin organization and their tight associations with diseases including cancer and mental disorders.

JMJD1A (also named KDM3A) is a demethylasethat removes methyl from histone lysine H3K9. It plays important roles in various cellular processes, including spermatogenesis, energy metabolism, regulation of stem cell and gender display.

Jumonji domain-containing 3 (Jmjd3) has been identified as a histone demethylase, which specifically catalyzes the removal of methylation from H3K27me3.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B0660
    Eicosapentaenoic Acid
    Activator 98.70%
    Eicosapentaenoic Acid (EPA) is an orally active Omega-3 long-chain polyunsaturated fatty acid (ω-3 LC-PUFA). Eicosapentaenoic Acid exhibits a DNA demethylating action that promotes the re-expression of the tumor suppressor gene CCAAT/enhancer-binding protein δ (C/EBPδ). Eicosapentaenoic Acid activates RAS/ERK/C/EBPβ pathway through H-Ras intron 1 CpG island demethylation in U937 leukemia cells. Eicosapentaenoic Acid can promote relaxation of vascular smooth muscle cells and vasodilation.
    Eicosapentaenoic Acid
  • HY-15648B
    GSK-J4
    Inhibitor 99.64%
    GSK-J4 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 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1. GSK-J4 induces endoplasmic reticulum stress-related apoptosis.
    GSK-J4
  • HY-12304
    IOX1
    Inhibitor 99.72%
    IOX1, 5-Carboxy-8-hydroxyquinoline, is a potent broad‐spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 inhibits KDM4C, KDM4E, KDM2A, KDM3A and KDM6B with IC50 values of 0.6 μM, 2.3 μM, 1.8 μM, 0.1 μM and 1.4 μM, respectively. IOX1 also inhibits ALKBH5.
    IOX1
  • HY-18632
    GSK2879552
    Inhibitor 99.90%
    GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity.
    GSK2879552
  • HY-100421
    CPI-455
    Inhibitor 98.95%
    CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents.
    CPI-455
  • HY-168593
    PROTAC KDM3 degrader-1
    Degrader 99.07%
    PROTAC KDM3 degrader-1 (Compound 4) is a CRBN-recruiting PROTAC designed based on the IOX1 (HY-12304) scaffold. PROTAC KDM3 degrader-1 selectively degrades the KDM3A and KDM3B proteins, thereby inhibiting the Wnt/β-catenin signaling pathway. PROTAC KDM3 degrader-1 significantly suppresses the self-renewal capacity of colorectal cancer stem cells and inhibits the growth of colorectal cancer tumors. PROTAC KDM3 degrader-1 is suitable for research on colorectal cancer (Target protein ligand (Pink): HY-12304; linker (Black): HY-22335; Conjugate of E3 ligase ligand and linker: HY-112599; E3 ligase (Blue): HY-41547).
    PROTAC KDM3 degrader-1
  • HY-148807B
    (S)-Zavondemstat
    Control
    (S)-Zavondemstat is the S-enantiomer of Zavondemstat (HY-148807). Zavondemstat is an inhibitor of histone lysine demethylase 4D (KDM4D) with antineoplastic activity[1].
    (S)-Zavondemstat
  • HY-168433
    LSD1/EGFR-IN-1
    Inhibitor
    LSD1/EGFR-IN-1 (compound L-1) is a potent inhibitor of LSD1, EGFRT790M/L858R and EGFRL858R/T790M/C797S, with IC50s of 6.24 and 2.06 and 5.01 μM, respectively. LSD1/EGFR-IN-1 plays an important role in cancer research.
    LSD1/EGFR-IN-1
  • HY-12782T
    Iadademstat dihydrochloride
    Inhibitor 99.98%
    Iadademstat (ORY-1001) dihydrochloride is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.
    Iadademstat dihydrochloride
  • HY-13953
    JIB-04
    Inhibitor 98.29%
    JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50s of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.
    JIB-04
  • HY-15648
    GSK-J1
    Inhibitor 99.94%
    GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
    GSK-J1
  • HY-103641
    (2R)-Octyl-α-hydroxyglutarate
    Control 99.91%
    (2R)-Octyl-α-hydroxyglutarate ((2R)-Octyl-2-HG) is a modified form of D-isomer 2-Hydroxyglutarate.
    (2R)-Octyl-α-hydroxyglutarate
  • HY-120400
    KDM5-C70
    Inhibitor
    KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels.
    KDM5-C70
  • HY-104048
    QC6352
    Inhibitor 99.48%
    QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC50s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC50 of 750 nM (KDM5B).
    QC6352
  • HY-B1496
    Tranylcypromine hemisulfate
    Inhibitor 99.94%
    Tranylcypromine (SKF 385) hemisulfate is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. Tranylcypromine hemisulfate is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis. Tranylcypromine has antidepressant effects.
    Tranylcypromine hemisulfate
  • HY-15648F
    GSK-J4 hydrochloride
    Inhibitor 99.01%
    GSK-J4 hydrochloride 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 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable proagent of GSK-J1.
    GSK-J4 hydrochloride
  • HY-12635
    SP2509
    Antagonist 99.90%
    SP2509 is a potent and selective antagonist of lysine specific demethylase 1 (LSD1) with an IC50 of 13 nM.
    SP2509
  • HY-103713
    Seclidemstat
    Inhibitor 99.77%
    Seclidemstat is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat 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 can be used for the research of Ewing Sarcoma.
    Seclidemstat
  • HY-100546A
    GSK-LSD1 dihydrochloride
    Inhibitor ≥98.0%
    GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC50 of 16 nM.
    GSK-LSD1 dihydrochloride
  • HY-116761
    GSK467
    Inhibitor 99.55%
    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.
    GSK467
Cat. No. Product Name / Synonyms Application Reactivity

KDM1/LSD1

KDM2

KDM3

KDM4

KDM5

KDM6

KDM7

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.

Histone Demethylase Inhibitors & Antagonists
Product NameKDM1/LSD1KDM2KDM3KDM4KDM5KDM6KDM7Purity    
GSK-J4     
KDM6
 99.64%
IOX1 
KDM2
KDM3
KDM4
 
KDM6
 99.72%
GSK2879552
KDM1/LSD1
      99.90%
CPI-455    
KDM5
  98.95%
Iadademstat dihydrochloride
KDM1/LSD1
      99.98%
JIB-04   
KDM4
KDM5
KDM6
 98.29%
GSK-J1     
KDM6
 99.94%
KDM5-C70    
KDM5
  
QC6352   
KDM4A, IC50: 104 nM
KDM4B, IC50: 56 nM
KDM4C, IC50: 35 nM
KDM4D, IC50: 104 nM
KDM5B, IC50: 750 nM
  99.48%
Tranylcypromine hemisulfate
KDM1/LSD1
      99.94%
GSK-J4 hydrochloride     
KDM6
 99.01%
SP2509
KDM1/LSD1
      99.90%
Seclidemstat
KDM1/LSD1
      99.77%
GSK467    
KDM5, Ki: 10 nM
KDM5, IC50: 26 nM
  99.55%
Daminozide 
KDM2
     99.79%
AS8351    
KDM5
  99.19%
KDOAM-25 citrate    
KDM5
  98.11%
Pulrodemstat benzenesulfonate
KDM1/LSD1
      99.64%
NCGC00244536   
KDM4
   99.58%
ML324   
KDM4
   98.46%
KDM5A-IN-1    
KDM5
  99.80%
Bomedemstat ditosylate
KDM1/LSD1
      99.17%
Bomedemstat hydrochloride
KDM1/LSD1
      99.94%
PFI-90  
KDM3
    99.86%
TK-129    
KDM5, IC50: 44 nM
  ≥98.0%
Bomedemstat dihydrochloride
KDM1/LSD1
      99.55%
KDM2A/7A-IN-1 
KDM2
     99.94%
KDM5-IN-1    
KDM5
  99.52%
Iadademstat
LSD1
      99.61%
TAK-418
KDM1/LSD1
      99.81%
PBIT    
KDM5
  99.46%
KDM2/7-IN-1 
KDM2
 
KDM4
  
KDM7
99.00%
KDM4D-IN-1   
KDM4
   98.82%
KDM4C-IN-1   
KDM4
   98.99%
NSC636819   
KDM4
   98.90%
GSK 690 Hydrochloride
KDM1/LSD1
      98.58%
S2101
KDM1/LSD1
      99.73%
YUKA1    
KDM5
  99.56%
T-3775440 hydrochloride
KDM1/LSD1
      99.13%
DDP-38003 dihydrochloride
KDM1/LSD1
      98.22%
INCB059872 dihydrochloride
KDM1/LSD1
      99.18%
JQKD82 trihydrochloride    
KDM5
  99.94%
KDM2B-IN-4 
KDM2
     99.59%
LSD1/HDAC6-IN-2
LSD1, IC50: 5 nM
      99.66%
DDP-38003 trihydrochloride
KDM1/LSD1
      
INCB059872
KDM1/LSD1
      98.06%
HDAC6-IN-3
KDM1/LSD1
      ≥98.0%
LSD1-IN-30
LSD1, IC50: 0.291 μM
      99.03%
Pulrodemstat
KDM1/LSD1
      
Bomedemstat
KDM1/LSD1
      99.55%
KDM4-IN-2   
KDM4
   98.29%
Arborinine
LSD1
      99.87%
NCGC00247743   
KDM4
   98.61%
CBB1007 hydrochloride
KDM1/LSD1
      ≥98.0%
CBB1007 trihydrochloride
KDM1/LSD1
      
GSK-J1 lithium salt     
KDM6
 98.26%
LSD1-IN-5
KDM1/LSD1
      
LSD1-IN-6
KDM1/LSD1
      
Pulrodemstat Methylbenzenesulfonate
KDM1/LSD1
      
CPI-455 hydrochloride    
KDM5
  
LSD1/HDAC6-IN-1
KDM1/LSD1
      
LSD1-IN-13 hydrochloride
KDM1/LSD1
      
MC2652
KDM1/LSD1
      
KDM4-IN-4   
KDM4A-Tudor domain, Ki: 80 μM
   
LSD1-IN-31
LSD1
      
LSD1-IN-34
LSD1, IC50: 4.51 nM
      
HSP90/LSD1-IN-1
LSD1
      
LSD1-UM-109
LSD1, IC50: 3.1 nM
      
LSD1-IN-38
LSD1, IC50: 1.2 nM
      
S1427
KDM1/LSD1
      
LSD1-IN-23
KDM1/LSD1, IC50: 0.58 μM
      
LSD1/2-IN-4
KDM1/LSD1
      
NCL1
LSD1, IC50: 2.5 ± 0.5 μM
      
cis-4-Br-2,5-F2-PCPA
KDM1/LSD1
      
KDM1/CDK1-IN-1
KDM1/LSD1
      
LSD1/HDAC-IN-2
KDM1/LSD1, IC50: 39.0 nM
      
LSD1-IN-26
LSD1, IC50: 25.3 ± 1.4 nM
      
LSD1-IN-21
LSD1, IC50: 0.956 μM
      
KDM5-C49    
KDM5
  
LSD1-IN-35
LSD1
      
LSD1-IN-18
KDM1/LSD1
      
LSD1-IN-25
LSD1, IC50: 46 nM
LSD1, Ki: 30.3 nM
      
(1S,2R)-Tranylcypromine hydrochloride
KDM1/LSD1
      
LSD1-IN-22
KDM1/LSD1
      
LSD1-IN-39
LSD1, IC50: 0.18 μM
      
LSD1-IN-19
KDM1/LSD1
      
LSD1-IN-42
LSD1, IC50: 0.08 μM
      
LSD1/2-IN-3
KDM1/LSD1
      
Tranylcypromine-d5 hydrochloride
KDM1/LSD1
      
LSD1/HDAC-IN-1
LSD1, IC50: 0.571 μM
      
JQKD82    
KDM5
  
LSD1/ER-IN-1
KDM1/LSD1
      
LSD1-IN-36
LSD1, IC50: 0.8 nM
      
CBB1003 hydrochloride
KDM1/LSD1