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Targets Recommended: Histone Demethylase
Results for "

demethylases

" in MCE Product Catalog:

69

Inhibitors & Agonists

2

Screening Libraries

2

Peptides

1

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-137187
    FB23

    Others Cancer
    FB23 is a potent and selective FTO demethylase inhibitor with an IC50 of 60 nM. FB23 directly binds to FTO and selectively inhibits FTO's mRNA N 6-methyladenosine (m6A) demethylase activity.
  • HY-122746
    E67-2

    Histone Methyltransferase Cancer
    E67-2, as the E67 derivative, is a low-toxicity, selective KIAA1718 Jumonji domain inhibitor with an IC50 value of 3.4 µM. E67-2 selectively inhibits histone H3 lysine 9 (H3K9) Jumonji demethylase as well as histone H3 lysine 4 (H3K4) demethylase.
  • HY-141677
    INCB059872

    Histone Demethylase Cancer
    INCB059872 is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 can be used for the research of myeloid leukemia.
  • HY-13643
    Daminozide

    Histone Demethylase Cancer
    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.
  • HY-139348
    PFI-90

    Histone Demethylase Cancer
    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).
  • HY-113039
    L-2-Hydroxyglutaric acid

    (S)-2-Hydroxyglutaric acid

    Histone Demethylase Mitochondrial Metabolism Endogenous Metabolite Cancer
    L-2-Hydroxyglutaric acid is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid 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.
  • HY-127103
    FB23-2

    Apoptosis Cancer
    FB23-2 is a potent and selective inhibitor of mRNA N 6-methyladenosine (m 6A) demethylase FTO, with an IC50 of 2.6 μM. FB23-2 has anti-proliferation activity. FB23-2 can be used for the research of acute myeloid leukemia (AML).
  • HY-15648F
    GSK-J4 hydrochloride

    Histone Demethylase Cancer
    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 prodrug of GSK-J1.
  • HY-W015114
    L-2-Hydroxyglutaric acid disodium

    (S)-2-Hydroxyglutaric acid disodium

    Histone Demethylase Mitochondrial Metabolism Cancer
    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.
  • HY-15648B
    GSK-J4

    Histone Demethylase Apoptosis Cancer
    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 prodrug of GSK-J1. GSK-J4 induces endoplasmic reticulum stress-related apoptosis.
  • HY-131970
    LSD1/HDAC6-IN-1

    Histone Demethylase Cancer
    LSD1/HDAC6-IN-1 is an orally active dual inhibitor of lysine specific demethylase 1(LSD1)/Histone deacetylase 6 (HDAC6), with anti-tumor activity. LSD1/HDAC6-IN-1 can be used for the research of multiple myeloma (MM).
  • HY-112308
    NCGC00247743

    Histone Demethylase Cancer
    NCGC00247743 is a histone lysine demethylase KDM4 inhibitor.
  • HY-136522
    S2116

    Histone Demethylase Apoptosis Cancer
    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.
  • HY-122635A
    T-448

    Histone Demethylase Neurological Disease
    T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons.
  • HY-15774A
    CBB1003 hydrochloride

    Histone Demethylase Cancer
    CBB1003 Hcl is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
  • HY-15774
    CBB1003

    Histone Demethylase Cancer
    CBB1003 is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
  • HY-136523
    S2157

    Histone Demethylase Apoptosis Cancer
    S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells.
  • HY-122635
    T-448 free base

    Histone Demethylase Neurological Disease
    T-448 free base is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 free base enhances H3K4 methylation in primary cultured rat neurons.
  • HY-15648
    GSK-J1

    Histone Demethylase Cancer
    GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B. 
  • HY-117226A
    GSK 690 Hydrochloride

    Histone Demethylase Others
    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.
  • HY-103085
    T-3775440 hydrochloride

    Histone Demethylase Cancer
    T-3775440 (hydrochloride) is an irreversible lysine-specific histone demethylase (LSD1) inhibitor with an IC50 value of 2.1 nM.
  • HY-15648D
    GSK-J1 lithium salt

    Histone Demethylase Cancer
    GSK-J1 lithium salt is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
  • HY-100546A
    GSK-LSD1 dihydrochloride

    Histone Demethylase Monoamine Oxidase Cancer
    GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC50 of 16 nM.
  • HY-12635
    SP2509

    Histone Demethylase Apoptosis Cancer
    SP2509 is a potent and selective antagonist of lysine specific demethylase 1 (LSD1) with an IC50 of 13 nM.
  • HY-108706
    KDM2A/7A-IN-1

    Histone Demethylase Cancer
    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.
  • HY-129388A
    Pulrodemstat

    CC-90011; LSD1-IN-7

    Histone Demethylase Cancer
    Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
  • HY-12725
    ML324

    Histone Demethylase HSV CMV Cancer
    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.
  • HY-15648A
    GSK-J2

    Histone Demethylase Cancer
    GSK-J2 is an isomer of GSK-J1 that does not have any specific activity. GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A.
  • HY-12782T
    Iadademstat dihydrochloride

    ORY-1001 dihydrochloride; RG6016 dihydrochloride; RO 7051790 dihydrochloride

    Histone Demethylase Cancer
    Iadademstat (ORY-1001) dihydrochloride is a selective irreversible lysine (K)-specific demethylase 1A (KDM1A/LSD1) inhibitor.
  • HY-16719
    Dapaconazole

    Cytochrome P450 Infection
    Dapaconazole, as an antifungal agent, inhibits sterol 14α-demethylase cytochrome P450 activity with an IC50 of 1.4 μM.
  • HY-129388B
    Pulrodemstat benzenesulfonate

    CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate

    Histone Demethylase Cancer
    CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
  • HY-139560
    KDM2B-IN-1

    Others Cancer Inflammation/Immunology
    KDM2B-IN-1 is a histone demethylase (kdm2b) inhibitor and can be used for hyperproliferative diseases research.
  • HY-129388
    Pulrodemstat Methylbenzenesulfonate

    CC-90011 Methylbenzenesulfonate; LSD1-IN-7 Methylbenzenesulfonate

    Histone Demethylase Cancer
    CC-90011 Methylbenzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 Methylbenzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 Methylbenzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
  • HY-111048
    Corin

    Histone Demethylase HDAC Cancer
    Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histone deacetylase (HDAC), with a Ki(inact) of 110 nM for LSD1 and an IC50 of 147 nM for HDAC1.
  • HY-112623
    Vafidemstat

    ORY-2001

    Histone Demethylase Monoamine Oxidase Neurological Disease
    Vafidemstat (ORY-2001) is an oral, brain penetrant, dual lysine-specific histone demethylase (LSD1)/MAO-B inhibitor.
  • HY-19612B
    DDP-38003 trihydrochloride

    Histone Demethylase Cancer
    DDP-38003 trihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
  • HY-19612A
    DDP-38003 dihydrochloride

    Histone Demethylase Cancer
    DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
  • HY-18632
    GSK2879552

    Histone Demethylase Cancer
    GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity.
  • HY-110277
    S2101

    Histone Demethylase Cancer
    S2101 is a lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s.
  • HY-101928
    KDM4D-IN-1

    Histone Demethylase Cancer
    KDM4D-IN-1 is a new histone lysine demethylase 4D (KDM4D) inhibitor with an IC50 value of 0.41±0.03 μM.
  • HY-18632A
    GSK2879552 dihydrochloride

    Histone Demethylase Cancer
    GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity.
  • HY-109040
    Quilseconazole

    VT-1129

    Fungal Cytochrome P450 Infection
    Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes.
  • HY-107842
    (Z)-JIB-04

    NSC693627

    Others Cancer
    (Z)-JIB-04 (NSC693627) is the Z isomer of JIB-04 that has two forms, E (HY-13953) and Z isomers. (Z)-JIB-04 is inactive in epigenetic analysis.
  • HY-113038B
    α-Hydroxyglutaric acid

    2-Hydroxyglutarate; 2-Hydroxyglutaric acid; 2-Hydroxypentanedioic acid

    Histone Demethylase Cancer
    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.
  • HY-139601
    KDM2B-IN-4

    Histone Demethylase Cancer
    KDM2B-IN-4 is a histone demethylase KDM2B inhibitor extracted from patent WO2016112284A1, compound 182b. KDM2B-IN-4 can be used for the research of cancer.
  • HY-139600
    KDM2B-IN-3

    Histone Demethylase Cancer
    KDM2B-IN-3 is a histone demethylase KDM2B inhibitor extracted from patent WO2016112284A1, compound 183c. KDM2B-IN-3 can be used for the research of cancer.
  • HY-123037
    Triadimefon

    Fungal Infection
    Triadimefon is a triazole fungicide used to control powdery mildew, rusts, and other fungal pests on grains, fruit and vegetable crops, turf, shrubs, and trees. Triadimefon inhibits lanosterol 14α-demethylase, interfering with oxidative demethylation reactions in the ergosterol biosynthesis pathway of fungi, and also blocks gibberellin biosynthesis.
  • HY-100859
    LSD1-IN-5

    Histone Demethylase Cancer
    LSD1-IN-5 (Compound 4e) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 121 nM. LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1.
  • HY-13953
    JIB-04

    Histone Demethylase Apoptosis Cancer
    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.
  • HY-100860
    LSD1-IN-6

    Histone Demethylase Cancer
    LSD1-IN-6 (Compound 4m) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 123 nM. LSD1-IN-6 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1.
  • HY-139561
    KDM2B-IN-2

    Others Cancer Inflammation/Immunology
    KDM2B-IN-1, a potent histone demethylase (kdm2b) inhibitor with an IC50 of 0.021 μM in a KDM2B TR-FRET assay. KDM2B-IN-1 can be used for hyperproliferative diseases research.
  • HY-16012
    Domatinostat tosylate

    4SC-202

    HDAC Apoptosis Cancer
    Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).
  • HY-110130
    RN-1 dihydrochloride

    Histone Demethylase Cancer Cardiovascular Disease
    RN-1 dihydrochloride is a potent, brain-penetrant, irreversible and selective lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 70 nM. RN-1 dihydrochloride exhibits selectivity for LSD1 over MAO-A and MAO-B with IC50 values of 0.51 μM and 2.785 μM respectively.
  • HY-16012A
    Domatinostat

    4SC-202 free base

    HDAC Apoptosis Cancer
    Domatinostat (4SC-202 free base) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).
  • HY-14282
    Lanoconazole

    Fungal Infection Inflammation/Immunology
    Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi in vitro and in vivo. Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis.
  • HY-B1496
    Tranylcypromine hemisulfate

    dl-Tranylcypromine hemisulfate; trans-2-Phenylcyclopropylamine hemisulfate salt

    Monoamine Oxidase Histone Demethylase Neurological Disease
    Tranylcypromine hemisulfate (dl-Tranylcypromine 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.
  • HY-14282A
    (Z)-Lanoconazole

    Fungal Infection Inflammation/Immunology
    (Z)-Lanoconazole is the Z configuration of Lanoconazole. Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi in vitro and in vivo. Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis.
  • HY-17447SA
    (rel)-Tranylcypromine D5 hydrochloride

    2-Phenylcyclopropylamine D5 hydrochloride

    Monoamine Oxidase Histone Demethylase Neurological Disease
    (rel)-Tranylcypromine D5 hydrochloride (2-Phenylcyclopropylamine D5 hydrochloride) is a deuterium labeled (rel)-Tranylcypromine hydrochloride. (rel)-Tranylcypromine hydrochloride is an irreversible, nonselective monoamine oxidase (MAO) inhibitor used in the treatment of depression. (rel)-Tranylcypromine hydrochloride is also a lysine-specific demethylase 1 (LSD1) inhibitor, suppresses lesion growth and improves generalized hyperalgesia in mouse with induced endometriosis.
  • HY-101451
    PBIT

    Histone Demethylase Cancer
    PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1) histone demethylase with an IC50 of about 3 μM . PBIT also inhibits JARID1A and JARID1C with IC50s of 6 μM and 4.9 μM, respectively.
  • HY-100764
    YUKA1

    Histone Demethylase Cancer
    YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM, less active on KDM5C (IC50, 7.12 μM), and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 increases H3K4me3 levels in human cells with anti-cancer activity.
  • HY-17514
    Itraconazole

    R51211

    Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Infection Cancer
    Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor.
  • HY-120400
    KDM5-C70

    Histone Demethylase Cancer
    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.
  • HY-117766
    PC945

    Fungal Cytochrome P450 Infection
    PC945, a potent, long-acting antifungal triazole, possesses activity against a broad range of both azole-susceptible and azole-resistant strains of Aspergillus fumigatus. PC945 is also a potent, tightly binding inhibitor of A. fumigatus sterol 14α-demethylase activity, CYP51A and CYP51B, with IC50s of 0.23 μM and 0.22 μM, respectively.
  • HY-102047
    KDOAM-25

    Histone Demethylase Cancer
    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.
  • HY-102047A
    KDOAM-25 trihydrochloride

    Histone Demethylase Cancer
    KDOAM-25 trihydrochloride 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 trihydrochloride increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells.
  • HY-17514S
    Itraconazole-d5

    Fungal Hedgehog Cytochrome P450 Autophagy Antibiotic Infection Cancer
    Itraconazole-d5 (R51211-d5) is the deuterium labeled Itraconazole. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects.
  • HY-102047B
    KDOAM-25 citrate

    Histone Demethylase Cancer
    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.
  • HY-12304
    IOX1

    Histone Demethylase Cancer
    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.
  • HY-100014
    KDM5A-IN-1

    Histone Demethylase Cancer
    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).