1. Signaling Pathways
  2. Epigenetics
  3. Histone Demethylase

Histone Demethylase

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 相关产品 (46):

Cat. No. Product Name Effect Purity
  • HY-104048
    QC6352 Inhibitor >98.0%
    QC6352 是一种有效的 KDM4C 抑制剂,其 IC50 值为 35 nM。
  • HY-15648B
    GSK-J4 Inhibitor >98.0%
    GSK-J4 是一种有效的 H3K27me3/me2 去甲基化酶 JMJD3/KDM6BUTX/KDM6A 双抑制剂,IC50 分别为 8.6 μM 和 6.6 μM。GSK-J4 抑制 LPS 诱导的人原代巨噬细胞产生 TNF-α,IC50 值为 9 μM。GSK-J4 是 GSK-J1 的细胞通透性前药。
  • HY-18632
    GSK2879552 Inhibitor 99.94%
    GSK2879552 是一种可口服的,不可逆的 LSD1 抑制剂,具有抗肿瘤活性。
  • HY-12635
    SP2509 Antagonist 99.81%
    SP2509 是有效,选择性的 LSD1 拮抗剂,IC50 值为 13 nM。
  • HY-100421
    CPI-455 Inhibitor >98.0%
    CPI-455 是一种特异性的泛 KDM5 抑制剂,对 KDM5A 的 IC50 为 10 nM,CPI-455 介导 KDM5 抑制,提高 H3K4me3 的整体水平,并减少用标准化疗或靶向药物治疗的多肿瘤细胞系模型中耐药的持久癌细胞的数量。
  • HY-102047B
    KDOAM-25 citrate Inhibitor 98.04%
    KDOAM-25 citrate 是有效,高选择性的 KDM5 抑制剂,对 KDM5A,KDM5B,KDM5C,KDM5D 的 IC50 分别为 71 nM,19 nM,69 nM,69 nM。KDOAM-25 citrate 可增加转录起始位点的整体 H3K4 甲基化,并损害多发性骨髓瘤 MM1S 细胞的增殖。
  • HY-100860
    LSD1-IN-6 Inhibitor
    LSD1-in-2 (Compound 4m) 是一种有效、可逆的赖氨酸特异性去甲基化酶 (LSD1) 抑制剂,IC50 值为 123 nM。LSD1-in-2 (4m) 能增加组蛋白 H3 Lys4 的二甲基化,但对 LSD1 的表达无作用。
  • HY-100764
    YUKA1 Inhibitor
    YUKA1 是一种有效、可透过细胞的赖氨酸脱甲基化酶 (KDM5A) 抑制剂,IC50 值为 2.66 μM,对 KDM5C 的作用较弱,IC50 值为 7.12 μM,对 KDM5B,KDM6A 或 KDM6B 无作用。YUKA1 可增加人细胞中 H3K4me3 的水平,具有抗肿瘤活性。
  • HY-12782T
    ORY-1001(trans) Inhibitor 99.14%
    ORY-1001 trans 是一种不可逆的选择性赖氨酸特异性脱甲基酶 1A (KDM1A/LSD1) 抑制剂。
  • HY-B1496
    Tranylcypromine hemisulfate Inhibitor 99.05%
    Tranylcypromine hemisulfate是一种用于治疗抑郁症的不可逆,非选择性 MAO 抑制剂。
  • HY-100546A
    GSK-LSD1 Dihydrochloride Inhibitor >98.0%
    GSK-LSD1 Dihydrochloride是有效,选择性,不可逆的赖氨酸特异性脱甲基酶 (LSD1) 抑制剂,IC50 值为16 nM。
  • HY-103713
    Seclidemstat Inhibitor 98.78%
    Seclidemstat (SP-2577) 是一种有效的 LSD1 抑制剂,平均 IC50 值为 127 nM。
  • HY-15648
    GSK-J1 Inhibitor 99.98%
    GSK-J1 是 H3K27me3/me2-demethylases JMJD3/KDM6BUTX/KDM6A 的抑制剂,对 KDM6B 的 IC50 值为 60 nM。
  • HY-101799
    NCGC00244536 Inhibitor 98.57%
    NCGC00244536是高效的 KDM4B 抑制剂,IC50 值为10 nM。
  • HY-13953
    JIB-04 Inhibitor 98.39%
    JIB-04 是 Jumonji 组蛋白去甲基酶 (Jumonji histone demethylase) 广谱抑制剂,能抑制 JARID1A,JMJD2E,JMJD3,JMJD2A,JMJD2B,JMJD2C 和 JMJD2D 的活性,其 IC50 值分别为 230,340,855,445,435,1100 和 290 nM。
  • HY-12304
    IOX1 Inhibitor
    IOX1,是 20G 氧合酶 (2OG oxygenases) 的有效广谱抑制剂,包括 JmjC 去甲基酶。IOX1 抑制 KDM4C,KDM4E,KDM2A,KDM3A 和 KDM6B 的 IC50 值分别为 0.6 μM,2.3 μM,1.8 μM,0.1 μM 和 1.4 μM。
  • HY-100422
    KDM5-IN-1 Inhibitor >98.0%
    KDM5-IN-1是高效选择,有口服活性的KDM5抑制剂,IC50值为15.1 nM。
  • HY-13643
    Daminozide Inhibitor >98.0%
    Daminozide(DMASA; DIMG; B 995)为植物生长调节剂,能选择性抑制KDM2/7 JmjC亚家族。
  • HY-100014
    KDM5A-IN-1 Inhibitor 98.65%
    KDM5A-IN-1 是一种有效的,口服可生物利用的泛组氨酸赖氨酸脱甲基酶 5 KDM5 抑制剂,对 KDM5AKDM5BKDM5CIC50 值分别为 45 nM,56 nM 和 55 nM,对 PC9 H3K4Me3 的 EC50 值为 960 nM。KDM5A-IN-1 对其他 KDM 酶 (1A,2B,3B,4C,6A,7B) 的效力明显较低。
  • HY-100744
    AS8351 Inhibitor 99.70%
    AS8351 是一种 KDM5B 抑制剂,可以诱导和维持有活性的染色质标记从而促进心肌细胞样细胞的产生。
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