2. Signaling Pathways
  3. Epigenetics
  4. Histone Demethylase

Histone Demethylase

Histone Demethylase

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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.

Histone Demethylase Isoform Specific Products:

Histone Demethylase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P5275
    Tripeptide-41
    		Inhibitor 99.30%
    Tripeptide-41 (CG-Lipoxyn) is a signal peptide. Tripeptide-41 activates the NF-kB signaling pathway, inhibits the expression of C/EBP and increases cAMP. Tripeptide-41 is an important intracellular signaling factor that causes lipolysis by promoting the hydrolysis of lipids into triglycerides. Tripeptide-41 can be used in cosmetics that targets fat accumulation.
    Tripeptide-41
  • HY-N0857
    Deoxyandrographolide
    		98.0%
    Deoxyandrographolide is an orally active lactone found in the Andrographis paniculata Nees. Deoxyandrographolide shows a KD of 38.4 μM of HDAC1. Deoxyandrographolide enhances GLUT4 plasma membrane translocation, activates PI3K and AMPK-dependent signaling pathways, suppresses fasting blood glucose, serum insulin, triglycerides, and LDL-cholesterol levels. Deoxyandrographolide enhances HDAC1 expression via inhibited ubiquitination degradation, represses H3K4me3, improves chromosome stability, and restrains aging biomarkers p16, p21, γH2A.X, p53 and ROS production. Deoxyandrographolide interacts with Foot-and-Mouth Disease Virus 3Cpro active site, inhibits protease and IFN-antagonist activity, derepresses ISG expression, and inhibits viral replication. Deoxyandrographolide can be used for the researches of type 2 diabetes mellitus, vascular senescence and virus infection.
    Deoxyandrographolide
  • HY-B0546AR
    Procaine hydrochloride (Standard)
    Procaine (hydrochloride) (Standard) is the analytical standard of Procaine (hydrochloride). This product is intended for research and analytical applications. Procaine hydrochloride is a DNA-demethylating agent. Procaine hydrochloride acts through multiple targets and has a slow onset and a short duration of action.
    Procaine hydrochloride (Standard)
  • HY-149213
    LSD1/TLK1-IN-1
    		Inhibitor 99.20%
    LSD1/TLK1-IN-1 is an orally active LSD1, TLK1, TLK2, TTK inhibitor with an LSD1 IC50 of 0.247 μM. LSD1/TLK1-IN-1 suppresses phosphorylation of Nek1 at T141 and Rad9 at S328, abrogates the TLK1>Nek1>ATR>Chk1 axis, protects H3K4me1/2 from demethylation, and does not affect LSD2, MAO-A, or MAO-B. LSD1/TLK1-IN-1 induces apoptosis, bypasses cell-cycle arrest, suppresses tumor growth, downregulates PD-L1 expression, enhances T-cell killing response, inhibits gastric cancer cell proliferation. LSD1/TLK1-IN-1 can be used for the research of prostate cancer and gastric cancer.
    LSD1/TLK1-IN-1
  • HY-113038AS
    α-Hydroxyglutaric acid-13C5 disodium
    		99.80%
    α-Hydroxyglutaric acid-13C5 (sodium) is the 13C labeled α-Hydroxyglutaric acid sodium. α-Hydroxyglutaric acid (2-Hydroxyglutarate) sodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid sodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases.
    α-Hydroxyglutaric acid-<sup>13</sup>C<sub>5</sub> disodium
  • HY-132198
    JMJD7-IN-1
    		Inhibitor 98.57%
    JMJD7-IN-1 is a potent JMJD7 inhibitor, with an IC50 of 6.62 μM. JMJD7-IN-1 shows good inhibitory activity against cells expressing a high level of JMJD7.
    JMJD7-IN-1
  • HY-P2255
    H3K4(Me) (1-20)
    		99.87%
    H3K4(Me) (1-20), a histone peptide. H3K4me is an intricately regulated posttranslational modification, which is broadly associated with enhancers and promoters of actively transcribed genomic loci.
    H3K4(Me) (1-20)
  • HY-117226A
    GSK 690 Hydrochloride
    		Inhibitor 98.58%
    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.
    GSK 690 Hydrochloride
  • HY-N6896
    Isoviolanthin
    		99.87%
    Isoviolanthin is a flavonoid glycoside. Isoviolanthin can be extracted from Dendrobium officinale. Isoviolanthin has a strong affinity for binding to KDM6B, CHAC2, ESCO2, and IPO4. Isoviolanthin decreases MMP-2 and MMP-9. Isoviolanthin inhibits TGF-β/Smad and PI3K/Akt/mTOR signaling pathways. Isoviolanthin increases Fhl3 expression. Isoviolanthin has cytoprotective effects. Isoviolanthin has anticancer activity against hepatocellular carcinoma.
    Isoviolanthin
  • HY-15648D
    GSK-J1 lithium salt
    		Inhibitor 98.33%
    GSK-J1 lithium salt is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
    GSK-J1 lithium salt
  • HY-136522
    S2116
    		Inhibitor 98.05%
    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.
    S2116
  • HY-141677A
    INCB059872 dihydrochloride
    		Inhibitor 99.64%
    INCB059872 dihydrochloride is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor that achieves inhibitory activity through the formation of covalent FAD-adducts. INCB059872 dihydrochloride can inhibit cell proliferation and induce cell differentiation by upregulating the expression of myeloid differentiation markers CD86 and CD11b. INCB059872 dihydrochloride can be used for the research of myeloid leukemia.
    INCB059872 dihydrochloride
  • HY-145259
    HDAC6-IN-3
    		Inhibitor 98.0%
    HDAC6-IN-3 (Compound 14), an antiprostate cancer agent, is a potent, orally active HDAC6 inhibitor with IC50s ranging from 0.02-1.54 μM for HDAC1/2/3/6/8/10. HDAC6-IN-3 is also an effective MAO-A (IC50=0.79 μM) and LSD1 inhibitor. HDAC6-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    HDAC6-IN-3
  • HY-15313C
    CBB1007 trihydrochloride
    		Inhibitor
    CBB1007 trihydrochloride is a reversible and selective LSD1 inhibitor with an IC50 of 5.27 µM for human LSD1. CBB1007 trihydrochloride significantly blocks the demethylase activity of LSD1 on H3K4Me2 and H3K4Me. CBB1007 trihydrochloride shows selectivity for LSD1 over LSD2 or JARID1A, and induces differentiation-related genes in pluripotent cells. CBB1007 trihydrochloride is studied in non-pluripotent cancer research, targeting teratocarcinoma, embryonic carcinoma, and seminoma.
    CBB1007 trihydrochloride
  • HY-121095
    Bizine
    		Inhibitor
    Bizine, a Phenelzine analogue, is a potent and selective LSD1 inhibitor, with a b>Ki of 59 nM. Bizine can modulate bulk histone methylation in cancer cells. Bizine shows neuroprotective effects.
    Bizine
  • HY-112308
    NCGC00247743
    		Inhibitor 99.38%
    NCGC00247743 is a histone lysine demethylase KDM4 inhibitor.
    NCGC00247743
  • HY-160191
    LSD1-IN-30
    		Inhibitor 99.03%
    LSD1-IN-30 (compound 3) is a potent inhibitor of lysine-specific demethylase 1 (LSD1), with the IC50 value of 0.291 μM.
    LSD1-IN-30
  • HY-19612B
    DDP-38003 trihydrochloride
    		Inhibitor
    DDP-38003 trihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
    DDP-38003 trihydrochloride
  • HY-128343
    KDM4-IN-2
    		Inhibitor 98.29%
    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.
    KDM4-IN-2
  • HY-102047
    KDOAM-25
    		Inhibitor
    KDOAM-25 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 increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.
    KDOAM-25
Cat. No. Product Name / Synonyms Application Reactivity
Histone Demethylase Isoform Comparison

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