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-138794G
    XL177A (GMP)
    		Inhibitor
    XL177A GMP is XL177A (HY-138794) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. XL177A is a covalent USP7 inhibitor that blocks the deubiquitinase activity of USP7. XL177A destabilizes non-canonical PRC1 complexes or KDM6A and reduces chromatin deposition of H2AK119Ub, thereby relieving the repression of neuronal differentiation programs. Meanwhile, XL177A also regulates the ELOF1-UVSSA-USP7-nuclear β-catenin axis, decreasing the transcription levels of related proteins and the accumulation of nuclear β-catenin. XL177A exerts antiviral effects by reducing the expression levels of coronavirus receptors, and exhibits inhibitory activity against APC-mutated colorectal cancer cells, neuroblastoma, and coronaviruses including SARS-CoV-2 variants. XL177A is mainly used in studies related to colorectal cancer, neuroblastoma, and coronavirus infections.
    XL177A (GMP)
  • HY-155115
    LSD1-IN-27
    		Inhibitor 98.88%
    LSD1-IN-27 is an orally active 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-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-176254
    LSD1-IN-43
    		Inhibitor
    LSD1-IN-43 is a highly selective, reversible, orally active and brain-penetrant LSD1 inhibitor with an IC50 value of 0.8 μM. LSD1-IN-43 has low inhibitory activity against MAO-A and MAO-B, two homologs of LSD1. LSD1-IN-43 significantly inhibits Aβ aggregation and enhances Aβ-induced neuronal cell viability. LSD1-IN-43 can be used for the study of Alzheimer’s disease (AD).
    LSD1-IN-43
  • 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-173136
    KDM4 ligand-1
    		Ligand
    KDM4 ligand-1 is a ligand for target protein (histone lysine demethylase KDM4) for PROTACs. KDM4 ligand-1 can be used in the synthesis of PROTACs (HY-173135).
    KDM4 ligand-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-183202
    NCD38
    		Inhibitor
    NCD38 is a Lysine-specific demethylase 1 (LSD1) inhibitor with a target IC50 of 0.59 μM. NCD38 selectively disrupts LSD1-GFI1B interactions, dissociates LSD1 and CoREST from the ERG super-enhancer. NCD38 increases apoptosis-related protein levels, induces apoptosis and reduces SOX2 and Oct4 levels. NCD38 can be used for the research of acute myeloid leukemia.
    NCD38
  • HY-186116
    LSD1-IN-49
    		Inhibitor
    LSD1-IN-49 is a Lysine-specific demethylase 1 (LSD1/KDM1A) inhibitor with a human IC50 of 29 nM. LSD1-IN-49 irreversibly inhibits LSD1 enzyme activity by forming an adduct with the flavin adenine dinucleotide (FAD) cofactor of LSD1. LSD1-IN-49 can be used as a lead compound for the development of LSD1-targeted PET imaging agents for the brain.
    LSD1-IN-49
  • HY-179610
    YU185530
    		Inhibitor
    YU185530 is a JARID1 histone demethylase inhibitor.
    YU185530
  • HY-19612
    DDP-38003
    		Inhibitor
    DDP-38003 (Compound 15) is an orally active KDM1A/LSD1 inhibitor with an IC50 value of 84 nM. DDP-38003 exhibits anticancer activity against promyelocytic leukemia.
    DDP-38003
  • 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-172519
    LSD1-IN-41
    		Inhibitor
    LSD1-IN-41 (compound 7) is a potent and selective LSD1 inhibitor. LSD1-IN-41 can be used for diffuse intrinsic pontine glioma (DIPG) research when combined with HDAC inhibitors.
    LSD1-IN-41
  • 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-B0660S2
    Eicosapentaenoic acid-d10
    Eicosapentaenoic acid-d10 (EPA-d10) is the deuterium labeled Eicosapentaenoic acid (HY-B0660). 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-d<sub>10</sub>
  • HY-141677C
    INCB059872 TFA
    		Inhibitor
    INCB059872 TFA 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 TFA can inhibit cell proliferation and induce cell differentiation by upregulating the expression of myeloid differentiation markers CD86 and CD11b. INCB059872 TFA can be used for the research of myeloid leukemia.
    INCB059872 TFA
  • 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-116796
    KDM4C-IN-2
    		Inhibitor
    KDM4C-IN-2 is a histone lysine demethylase KDM4C (JMJD2C) inhibitor with an IC50 of 147 μM and a Ki of 51 μM. KDM4C-IN-2 can be used for the research of cancer, such as prostate and breast cancer.
    KDM4C-IN-2
  • HY-141677B
    INCB059872 tosylate
    		Inhibitor
    INCB059872 tosylate 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 tosylate can inhibit cell proliferation and induce cell differentiation by upregulating the expression of myeloid differentiation markers CD86 and CD11b. INCB059872 tosylate can be used for the research of myeloid leukemia.
    INCB059872 tosylate
Cat. No. Product Name / Synonyms Application Reactivity
Histone Demethylase Isoform Comparison

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