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-155526
    FY-21
    		Inhibitor
    FY-21 is a selective inhibitor of LSD1 (IC50=340 nM), with anti-proliferation and anti-colony formation activities. FY-21 enhances p53 expression, down-regulates HOXA9 and MEIS1 expression. FY-21 also induces leukemia cell differentiation to exhibts antitumor activity.
    FY-21
  • HY-150619
    KDM4-IN-4
    		Inhibitor
    KDM4-IN-4 (compound 47) is a potent histone lysine demethylase 4 (KDM4) inhibitor with a modest affinity binding to ~80 μM for KDM4A-Tudor domain. KDM4-IN-4 can inhibit H3K4Me3 binding to the Tudor domain in cells with an EC50 value of 105 μM. KDM4-IN-4 can be used for researching anticancer.
    KDM4-IN-4
  • HY-161849
    LSD1-IN-31
    		Inhibitor
    LSD1-IN-31 (compound 11e) can directly bind to LSD1/CoREST complex to reduce LSD1 demethylation enzymatic activity. LSD1-IN-31 inhibits LSD1 demethylation activity and influences its downstream IκB/NF-κB signaling pathway. LSD1-IN-31 inhibits osteoclastic bone loss in vitro and in vivo. LSD1-IN-31 can be used for osteoporosis research.
    LSD1-IN-31
  • HY-144758
    LSD1-IN-17
    		Inhibitor
    LSD1-IN-17 (compound 5b) is a potent LSD1 inhibitor. LSD1-IN-17 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC50 values of 0.005, 0.028, and 0.820 μM, respectively. LSD1-IN-17 displays cell growth arrest in prostate cancer LNCaP cells, with an IC50 of 17.2 μM.
    LSD1-IN-17
  • HY-W015114R
    L-2-Hydroxyglutaric acid (disodium) (Standard)
    		Inhibitor
    L-2-Hydroxyglutaric acid (disodium) (Standard) is the analytical standard of L-2-Hydroxyglutaric acid (disodium). This product is intended for research and analytical applications. L-2-Hydroxyglutaric acid disodium is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid disodium can inhibit histone demethylases and hence promote histone methylation. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki of 2.52 mM and 11.13 mM, respectively.
    L-2-Hydroxyglutaric acid (disodium) (Standard)
  • HY-156094
    JMJD3/HDAC-IN-1
    		Inhibitor
    JMJD3/HDAC-IN-1 (compound A5b) is a dual inhibitor targeting Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylase (HDAC1, IC50=16 nM). JMJD3/HDAC-IN-1 promotes hypermethylation of histone H3K27 and hyperacetylation of H3K9, and also cleaves caspase-7 and PARP to induce apoptosis. JMJD3/HDAC-IN-1 effectively inhibits cancer cell cloning, migration, and invasion.
    JMJD3/HDAC-IN-1
  • HY-155115
    LSD1-IN-27
    		Inhibitor 98.88%
    LSD1-IN-27 (Compound 5ac) is a LSD1 inhibitor (IC50: 13 nM). LSD1-IN-27 inhibits the stemness and migration of gastric cancer cells. LSD1-IN-27 also reduces the expression of PD-L1 in BGC-823 and MFC cells. LSD1-IN-27 can enhance T cell immune response in gastric cancer.
    LSD1-IN-27
  • HY-169098
    HSP90/LSD1-IN-1
    		Inhibitor
    HSP90/LSD1-IN-1 (compound 6) is a HSP90/LSD1 dual inhibitor. HSP90/LSD1-IN-1 inhibits the proliferation of prostate cancer cell lines PC-3 and DU145, with GI50 values ​​of 0.24 and 0.30 μM, respectively.
    HSP90/LSD1-IN-1
  • HY-144756
    LSD1-IN-15
    		Inhibitor
    LSD1-IN-15 (compound 1b) is a potent LSD1 inhibitor. LSD1-IN-15 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC50 values of 0.149, 0.028, and 0.327 μM, respectively. LSD1-IN-15 displays cell growth arrest in prostate cancer LNCaP cells, with an IC50 of 9.9 μM.
    LSD1-IN-15
  • HY-149595
    LSD1-UM-109
    		Inhibitor
    LSD1-UM-109 is a ighly potent and reversible LSD1 inhibitor with an IC50 of 3.1 nM. LSD1-UM-109 inhibits cell growth with IC50 values of 0.6 nM in the MV4;11 acute leukemia cell line and 1.1 nM in the H1417 small-cell lung cancer cell line.
    LSD1-UM-109
  • HY-153608
    JHDM-IN-1
    		Inhibitor
    JHDM-IN-1 (Compound 1) is a Jumonji C domain-containing HDMs (JHDM) inhibitor with IC50s of 3.4, 4.3, 5.9, 10 and 43 μM against JMJD2C, JMJD2A, JMJD2E, PHF8 and JMJD3, respectively.
    JHDM-IN-1
  • HY-170403
    LSD1-IN-38
    		Inhibitor
    LSD1-IN-38 (Compound 23e) is a reversible, orally active inhibitor for lysine specific demethylase 1 (LSD1) with an IC50 of 1.2 nM. LSD1-IN-38 inhibits the proliferation of cancer cells MV4-11, Kasumi-1 and NCI-H526, with IC50 of 5, 4 and 11 nM, respectively. LSD1-IN-38 activates CD86 expression with an EC50 of 0.034 μM, and induces differentiation in MV4−11 cell. LSD1-IN-38 exhibits antitumor efficacy in mouse models.
    LSD1-IN-38
  • HY-P10819
    S9-CMC1 TFA
    		Inhibitor
    S9-CMC1 TFA is a covalent peptide lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 value of 2.53 μM. S9-CMC1 TFA specifically recognizes Cys360 in the enzyme-active region. S9-CMC1 TFA inhibits LSD1 activity, increasing H3K4me1 and H3K4me2 levels, leading to G1 cell cycle arrest and apoptosis and inhibiting cell proliferation. S9-CMC1 TFA significantly inhibits tumor growth in A549 xenograft animal models.
    S9-CMC1 TFA
  • HY-141677B
    INCB059872 tosylate
    		Inhibitor
    INCB059872 tosylate is a potent, selective and orally active lysine-specific demethylase 1 inhibitor. INCB059872 binds to and inhibits LSD1, enhancing H3K4 methylation, thereby increasing the expression of tumor suppressor genes. INCB059872 inhibition also promotes H3K9 methylation, thereby reducing the transcription of tumor-promoting genes.
    INCB059872 tosylate
  • HY-112304A
    (1R,2S)-NCD38 TFA
    		Inhibitor
    (1R,2S)-NCD38 TFA is an enantiomer of NCD38 TFA. NCD38 TFA is a LSD1-selective inhibitor.
    (1R,2S)-NCD38 TFA
  • HY-146380
    S1427
    		Inhibitor
    S1427 is a tranylcypromine-derived LSD1 inhibitor with the IC50 of 390 nM and Ki of 80 nM. S1427 exhibits desirable hERG channel inhibition and microsomal stability profiles. Inhibition of LSD1 partially reduces the proliferation of cancer cells.
    S1427
  • HY-117226
    GSK 690
    		Inhibitor
    GSK 690 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
  • HY-156202
    Geranylgeranoic acid
    		Inhibitor
    Geranylgeranoic acid (Compound 5) is inhibits lysine-specific demethylase 1 (LSD1) with an IC50 value of 46.97 µM. Geranylgeranoic acid induces apoptosis via loss of the mitochondrial membrane potential and activation of interleukin-1β-converting enzyme (ICE) and cysteine protease precursor 32 (CPP32) in Huh7 and PLC/PRF/5 human hepatoma cells and MLE-10 transformed mouse hepatocytes. Geranylgeranoic acid an isoprenoid with anticancer activity, which is found in S. chinensis.
    Geranylgeranoic acid
  • HY-152032
    LSD1-IN-23
    		Inhibitor
    LSD1-IN-23 is a competitive/non-competitive mixed inhibitor of lysine specific demethylase 1 (LSD1). LSD1-IN-23 has LSD1 inhibitory activity with an IC50 value of 0.58 μM. LSD1-IN-23 can be used for the research of neuroblastoma (NB).
    LSD1-IN-23
  • HY-151194
    LSD1/2-IN-4
    		Inhibitor
    LSD1/2-IN-4, a PCPA derivative, is an inhibitor of lysine-specific demethylase 1 (LSD1) and lysine-specific demethylase 2 (LSD2). LSD1/2-IN-4 inhibits LSD1 and LSD2 with Ki values of 0.11 μM and 130 μM, respectively. LSD1/2-IN-4 can be used for the research of several cancers including T-cell acute lymphoblastic leukemia (TALL).
    LSD1/2-IN-4
Cat. No. Product Name / Synonyms Application Reactivity
Histone Demethylase Isoform Comparison

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