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KDM Inhibitors

" in MedChemExpress (MCE) Product Catalog:

103

Inhibitors & Agonists

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Targets Recommended:
Cat. No. 상품명 Target 연구분야 Chemical Structure
  • HY-15648B
    GSK-J4
    Maximum Cited Publications
    55 Publications Verification

    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 proagent of GSK-J1 . GSK-J4 induces endoplasmic reticulum stress-related apoptosis .
    GSK-J4
  • HY-B0568
    Deferiprone
    45+ Cited Publications

    Ferroptosis HCV Apoptosis COX Histone Demethylase Cardiovascular Disease Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Deferiprone is a potent, orally active, brain-penetrant, cell-penetrant, skin-permeable, free iron chelating agent. Deferiprone inhibits the proliferation and migration, and stimulates apoptosis in tumor cell. Deferiprone can inhibit KDM. Deferiprone has antianemic, neuroprotective, anti-inflammatory, antioxidant, and antidotal activity. Deferiprone can be used in cancer, cardiovascular disease, infection, inflammation, and neurological disease study .
    Deferiprone
  • HY-12304
    IOX1
    10+ Cited Publications

    Histone Demethylase Cancer
    IOX1, a chemical probe, 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 .
    IOX1
  • HY-13643
    Daminozide
    3 Publications Verification

    Environmental Pollutants 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 .
    Daminozide
  • HY-100421
    CPI-455
    10+ Cited Publications

    Histone Demethylase Cancer
    CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .
    CPI-455
  • HY-120400
    KDM5-C70
    5+ Cited Publications

    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 .
    KDM5-C70
  • HY-15648F
    GSK-J4 hydrochloride
    Maximum Cited Publications
    55 Publications Verification

    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 proagent of GSK-J1 .
    GSK-J4 hydrochloride
  • HY-104048
    QC6352
    10+ Cited Publications

    Histone Demethylase Cancer
    QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC50s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC50 of 750 nM (KDM5B) .
    QC6352
  • HY-15648
    GSK-J1
    15+ Cited Publications

    Histone Demethylase Cancer
    GSK-J1, a chemical probe, is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
    GSK-J1
  • HY-12782T
    Iadademstat dihydrochloride
    5+ Cited Publications

    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.
    Iadademstat dihydrochloride
  • HY-148807

    QC8222 free base; TACH 101 free base

    Histone Demethylase Apoptosis Cancer
    Zavondemstat (QC8222 free base; TACH 101 free base) is an orally active pan-KDM4 inhibitor, with a IC50 ≤ 0.08 μM against human KDM4A-D and a Kᵢ of 0.52 μM against human KDM4C. Zavondemstat induces cell apoptosis, causes S-phase cell cycle arrest, reduces the population of tumor-initiating cells and inhibits cancer cell proliferation. Zavondemstat suppresses tumor growth and induces tumor regression in mouse xenograft models. Zavondemstat can be used for the research of various cancers including colorectal cancer, esophageal squamous cell carcinoma and triple-negative breast cancer .
    Zavondemstat
  • HY-18632
    GSK2879552
    15+ Cited Publications

    Histone Demethylase Cancer
    GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity .
    GSK2879552
  • HY-107573
    KDM2/7-IN-1
    1 Publications Verification

    Histone Demethylase Cancer
    KDM2/7-IN-1 (TC-E 5002) is a selective histone demethylase KDM2/7 subfamily inhibitor (IC50 values are 0.2, 1.2, 6.8, 55, 83, >100 and >120 μM for KDM7A, KDM7B, KDM2A, KDM5A, KDM4C, KDM6A and KDM4A respectively). KDM2/7-IN-1 inhibits growth of HeLa and KYSE-150 cancer cells in vitro .
    KDM2/7-IN-1
  • HY-116761
    GSK467
    5 Publications Verification

    Histone Demethylase Cancer
    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-100760
    Toxoflavin
    5+ Cited Publications

    Xanthothricin; Toxoflavine; PKF-118-310

    β-catenin Bacterial Antibiotic Histone Demethylase Infection Cancer
    Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex, also acts as an inhibitor of KDM4A, with antitumor and antibiotic activity .
    Toxoflavin
  • HY-109117
    Iadademstat
    5+ Cited Publications

    ORY-1001

    Histone Demethylase Apoptosis Cancer
    Iadademstat (ORY-1001) is a highly potent, orally active and selective LSD1 (KDM1A) inhibitor with antileukemic activity. Iadademstat can be used for relapsed or refractory acute myeloid leukemia research .
    Iadademstat
  • HY-12725
    ML324
    5+ Cited Publications

    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 .
    ML324
  • HY-18632A
    GSK2879552 dihydrochloride
    15+ Cited Publications

    Histone Demethylase Cancer
    GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity .
    GSK2879552 dihydrochloride
  • HY-100744
    AS8351
    1 Publications Verification

    NSC51355

    Histone Demethylase Cardiovascular Disease
    AS8351 (NSC51355) is a KDM5B inhibitor, which can induce and sustain active chromatin marks to facilitate the induction of cardiomyocyte-like cells .
    AS8351
  • HY-103713
    Seclidemstat
    10+ Cited Publications

    SP-2577

    Histone Demethylase Cancer
    Seclidemstat is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat can be used for the research of Ewing Sarcoma .
    Seclidemstat
  • HY-102047B
    KDOAM-25 citrate
    5+ Cited Publications

    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 .
    KDOAM-25 citrate
  • HY-19612A
    DDP-38003 dihydrochloride
    1 Publications Verification

    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 .
    DDP-38003 dihydrochloride
  • HY-100421A
    CPI-455 hydrochloride
    10+ Cited Publications

    Histone Demethylase Cancer
    CPI-455 hydrochloride is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents .
    CPI-455 hydrochloride
  • HY-139348
    PFI-90
    1 Publications Verification

    Histone Demethylase Apoptosis 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).
    PFI-90
  • HY-132896

    Histone Demethylase Cancer
    KDM4-IN-3 (Compound 15) is a KDM4 inhibitor (IC50 = 871 nM) that exhibits improved potency in biochemical assays. KDM4-IN-3 is cell-permeable and kills prostate cancer cells at low micro molar concentrations. KDM4-IN-3 inhibits growth of prostate cancer cell lines and increases the H3K9me3 abundance. KDM4-IN-3 can be studied in research for prostate cancer .
    KDM4-IN-3
  • HY-100422
    KDM5-IN-1
    2 Publications Verification

    Histone Demethylase Cancer
    KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.
    KDM5-IN-1
  • HY-100014
    KDM5A-IN-1
    4 Publications Verification

    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) .
    KDM5A-IN-1
  • HY-101799
    NCGC00244536
    2 Publications Verification

    KDM4B Inhibitor B3

    Histone Demethylase Cancer
    NCGC00244536 is a potent KDM4B inhibitor with an IC50 of 10 nM.
    NCGC00244536
  • HY-15648A
    GSK-J2
    4 Publications Verification

    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.
    GSK-J2
  • HY-101451
    PBIT
    3 Publications Verification

    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 .
    PBIT
  • HY-100624

    CDK DNA/RNA Synthesis Histone Demethylase Histone Methyltransferase Inflammation/Immunology Cancer
    Ryuvidine is a potent inhibitor of SET domain-containing protein 8(SETD8) with an IC50 of 0.5 µM and suppresses monomethylation of H4K20. Ryuvidine also inhibits CDK4 with an IC50 of 6.0 μM. Ryuvidine also inhibits KDM5A and blocks DNA synthesis. Ryuvidine has anticancer activity against tumors such as breast cancer. Ryuvidine improves arthritis .
    Ryuvidine
  • HY-119397A
    KDM5-C49 hydrochloride
    1 Publications Verification

    KDOAM-20 hydrochloride

    Histone Demethylase Cancer
    KDM5-C49 (KDOAM-20) hydrochloride is a potent and selective inhibitor of KDM5 demethylases, with IC50s of 40 nM, 160 nM, and 100 nM for KDM5A, KDM5B, and KDM5C enzymes, respectively. KDM5-C49 hydrochloride can be used for the research of cancer .
    KDM5-C49 hydrochloride
  • HY-139561

    Histone Demethylase Inflammation/Immunology Cancer
    KDM2B-IN-2, a potent histone demethylase (kdm2b) inhibitor with an IC50 of 0.021 μM in a KDM2B TR-FRET assay. KDM2B-IN-2 can be used for hyperproliferative diseases research .
    KDM2B-IN-2
  • HY-110154

    Histone Demethylase Cancer
    NSC636819 is a competitive and selective inhibitor of KDM4A/KDM4B. KDM4A/KDM4B are potential progression factors for prostate cancer. NSC636819 has the potential for the research of cancer diseases, especially prostate cancer .
    NSC636819
  • HY-139601

    Histone Demethylase Cancer
    KDM2B-IN-4 (Compound 182b) is a histone demethylase KDM2B inhibitor with an IC50 of 1.12 nM. KDM2B-IN-4 can be used for the research of hyperproliferative diseases such as cancers .
    KDM2B-IN-4
  • HY-146148
    KDM4C-IN-1
    2 Publications Verification

    Histone Demethylase Cancer
    KDM4C-IN-1 (Compound 4d) is a potent KDM4C inhibitor with an IC50 of 8 nM. KDM4C-IN-1 inhibits the growth of HepG2 and A549 cells with IC50s of 0.8 µM and 1.1 µM, respectively .
    KDM4C-IN-1
  • HY-101928
    KDM4D-IN-1
    2 Publications Verification

    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.
    KDM4D-IN-1
  • HY-108706

    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 .
    KDM2A/7A-IN-1
  • HY-100764
    YUKA1
    1 Publications Verification

    Histone Demethylase Cancer
    YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM. YUKA1 has less inhibitory active on KDM5C (IC50 = 7.12 μM) and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 can increase H3K4me3 levels and inhibit cell proliferation. YUKA1 can be used for the research of cancer, such as lung and breast cancers .
    YUKA1
  • HY-138830
    TAK-418
    2 Publications Verification

    Histone Demethylase Neurological Disease
    TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC50 of 2.9 nM. TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models .
    TAK-418
  • HY-103713A
    Seclidemstat mesylate
    10+ Cited Publications

    SP-2577 mesylate

    Histone Demethylase Cancer
    Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma .
    Seclidemstat mesylate
  • HY-129079
    TFMB-(R)-2-HG
    3 Publications Verification

    Estrogen Receptor/ERR Histone Demethylase Fat Mass and Obesity-associated Protein (FTO) Cancer
    TFMB-(R)-2-HG is a cell membrane-permeable (R)-2-HG and acute myeloid leukemia (AML) oncogenic factor. TFMB-(R)-2-HG competitively inhibits α-ketoglutarate-dependent dioxygenases such as KDM2B and FTO. TFMB-(R)-2-HG impairs cell differentiation in response to Estrogen withdrawal. TFMB-(R)-2-HG is used in acute myeloid leukemia and glioma research .
    TFMB-(R)-2-HG
  • HY-139560

    Histone Demethylase Inflammation/Immunology Cancer
    KDM2B-IN-1 (example 32) is a histone demethylase (kdm2b) inhibitor with an IC50 of 0.016 nM. KDM2B-IN-1 can be used for hyperproliferative diseases research .
    KDM2B-IN-1
  • HY-149091

    Histone Demethylase Cancer
    KDM5B-IN-4 (compound 11ad) is a lysine demethylase 5B (KDM5B) inhibitor with an IC50 of 0.025 μM KDM5B-IN-4 increases substrate H3K4me1/2/3 level by inhibiting KDM5B in PC-3 cells. KDM5B-IN-4 downregulates PI3K/AKT. KDM5B-IN-4 reduces tumor volume in mice and shows less toxic to organs .
    KDM5B-IN-4
  • HY-151483

    Wnt Histone Demethylase Cardiovascular Disease
    TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC50=44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. TK-129 reduces ang II-induced activation of cardiac fibroblasts in vitro and reduces isoprenaline-induced myocardial remodelling and fibrosis in vivo. TK-129 can be used in studies of cardiovascular disease .
    TK-129
  • HY-138691A

    JADA82 trihydrochloride; PCK82 trihydrochloride

    Histone Demethylase Cancer
    JQKD82 (JADA82) trihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 trihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma .
    JQKD82 trihydrochloride
  • HY-N6896
    Isoviolanthin
    1 Publications Verification

    TGF-beta/Smad PI3K Akt mTOR MMP Histone Demethylase Endocrinology Cancer
    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-102047

    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 .
    KDOAM-25
  • HY-15648D
    GSK-J1 lithium salt
    15+ Cited Publications

    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.
    GSK-J1 lithium salt
  • HY-168593

    β-catenin PROTACs Wnt Histone Demethylase Cancer
    PROTAC KDM3 degrader-1 (Compound 4) is a CRBN-recruiting PROTAC designed based on the IOX1 (HY-12304) scaffold. PROTAC KDM3 degrader-1 selectively degrades the KDM3A and KDM3B proteins, thereby inhibiting the Wnt/β-catenin signaling pathway. PROTAC KDM3 degrader-1 significantly suppresses the self-renewal capacity of colorectal cancer stem cells and inhibits the growth of colorectal cancer tumors. PROTAC KDM3 degrader-1 is suitable for research on colorectal cancer (Target protein ligand (Pink): HY-12304; linker (Black): HY-22335; Conjugate of E3 ligase ligand and linker: HY-112599; E3 ligase (Blue): HY-41547) .
    PROTAC KDM3 degrader-1

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