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-101799
    NCGC00244536
    		Inhibitor 99.58%
    NCGC00244536 is a potent KDM4B inhibitor with an IC50 of 10 nM.
    NCGC00244536
  • HY-102047B
    KDOAM-25 citrate
    		Inhibitor 98.11%
    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.
    KDOAM-25 citrate
  • HY-100744
    AS8351
    		Inhibitor 99.19%
    AS8351 (NSC51355) is a KDM5B inhibitor, which can induce and sustain active chromatin marks to facilitate the induction of cardiomyocyte-like cells.
    AS8351
  • HY-18632A
    GSK2879552 dihydrochloride
    		Inhibitor 99.19%
    GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.
    GSK2879552 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
  • HY-13643
    Daminozide
    		Inhibitor 99.79%
    Daminozide, a plant growth regulator, is a selective inhibitor of the human KDM2/7 histone demethylases, with IC50s of 0.55, 1.5 and 2.1 μM for PHF8, KDM2A, and KIAA1718, respectively. Daminozide has >100-fold selectivity for KDM2/7 subfamily versus other demethylase subfamily members tested.
    Daminozide
  • HY-12725
    ML324
    		Inhibitor 98.54%
    ML324 is a potent JMJD2 demethylase inhibitor with antiviral activity. ML324 also exhibits inhibition for the histone demethylase KDM4B, with an IC50 of 4.9 μM. ML324 has potent anti-viral activity against both herpes simplex virus (HSV) and human cytomegalovirus (hCMV) infection via inhibition viral IE gene expression.
    ML324
  • HY-109169B
    Bomedemstat hydrochloride
    		Inhibitor 99.55%
    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.
    Bomedemstat hydrochloride
  • HY-139348
    PFI-90
    		Inhibitor 99.86%
    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).
    PFI-90
  • HY-100014
    KDM5A-IN-1
    		Inhibitor 99.80%
    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).
    KDM5A-IN-1
  • HY-139782
    SKLB325
    		Inhibitor 99.23%
    SKLB325 is a Jumonji domain-containing 6 (JMJD6) inhibitor with a binding affinity (KD) value of 0.755?μM, and the IC50 value of 0.7797?μM. SKLB325 exhibits antitumor effects on ovarian cancer in vivo and in vitro. SKLB325 induces apoptosis. SKLB325 exhibits remarkable antitumor efficacy in renal cell carcinoma (RCC) .
    SKLB325
  • HY-W015114
    L-2-Hydroxyglutaric acid disodium
    		Inhibitor 99.12%
    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
  • HY-B0546
    Procaine
    		99.96%
    Procaine is a DNA-demethylating agent. Procaine acts through multiple targets and has a slow onset and a short duration of action.
    Procaine
  • HY-113038A
    α-Hydroxyglutaric acid disodium
    		Inhibitor ≥98.0%
    α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium 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 disodium
  • HY-108706
    KDM2A/7A-IN-1
    		Inhibitor 99.94%
    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.
    KDM2A/7A-IN-1
  • HY-Q36392
    JNJ-9350
    		Inhibitor 99.21%
    JNJ-9350 is an inhibitor of spermine oxidase (SMOX) with an IC50 value of 0.01 μM. JNJ-9350 also inhibits polyamine oxidase (PAO) with an IC50 value of 0.79 μM. JNJ-9350 can be used for the research of cancer.
    JNJ-9350
  • HY-109169A
    Bomedemstat ditosylate
    		Inhibitor 99.17%
    Bomedemstat (IMG-7289) ditosylate is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat ditosylate can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat ditosylate shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.
    Bomedemstat ditosylate
  • HY-113038B
    α-Hydroxyglutaric acid
    		Inhibitor ≥99.0%
    α-Hydroxyglutaric acid (2-Hydroxyglutarate) is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid 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
  • HY-100422
    KDM5-IN-1
    		Inhibitor 99.87%
    KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
    KDM5-IN-1
  • HY-109169C
    Bomedemstat dihydrochloride
    		Inhibitor 99.55%
    Bomedemstat (IMG-7289) dihydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat dihydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat dihydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.
    Bomedemstat dihydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Histone Demethylase Isoform Comparison

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