Histone Demethylases

Histone Demethylases(组蛋白去甲基化酶)

Histone demethylases are a diverse group of enzymes catalyzing a process to reverse histone methylation, in which methyl (CH3-) groups are removed from instead of being transferred to histone.  So far, two evolutionarily conserved histone demethylase families have been identified, including LSD demethylases and JMJC demethylases. LSD1 and LSD2 are two well-established members of LSD demethylase family, which catalyze demethylation through a flavin adenine dinucleotide (FAD)-dependent amine oxidation reaction. LSD1 has been found to demethylate H3K4mel, H3K4me2, H3K9me1, H3K9me2 and a few non-histone targets; while LSD2 has been found to demethylate only H3K4me1 and H3K4me2. Members of JMJC demethylase family is characterized by containing the catalytic JMJC domain, which demethylate substrates, including H3K4, H3K9, H3K27, H3K36 and H4K20, through a Fe(II)- and α-ketogutarate-dependent dioxygenase reaction.

Histone Demethylases 相关产品(103)

  • GC12961 structure
    GC12961Apicidin
    CAS: 183506-66-3
    纯度: >98.00% / >90.00%

    A cell-permeable HDAC inhibitor

  • GC15497 structure
    GC15497GSK J4 HCl
    CAS: 1797983-09-5
    纯度: >98.00%

    GSK-J4 HCl 是一种小分子抑制剂,具有高效的细胞渗透性和药理学选择性抑制剂,可通过抑制 KDM6B 来保持 H3K27 甲基化。

  • GC18159 structure
    GC18159BAY-598
    CAS: 1906919-67-2
    纯度: >99.50%

    BAY-598是一种氨基吡唑啉基的选择性小分子抑制剂,靶点为含有SET和MYND结构域的蛋白2(SMYD2),半抑制浓度(IC 50 )为27nM。

  • GC10148 structure
    GC10148RN 1 dihydrochloride
    CAS: 1781835-13-9
    纯度: >98.00%

    An irreversible LSD1 inhibitor

  • GC10319 structure
    GC10319TC-E 5002
    CAS: 1453071-47-0
    纯度: >98.00%

    A KDM2/7 inhibitor

  • GC10774 structure
    GC10774CPI-455
    CAS: 1628208-23-0
    纯度: >98.50% / >98.00%

    CPI-455是一种KDM5抑制剂,KDM5(Kissinger Demethylase 5)是一种赖氨酸特异性脱甲基酶,在染色质修饰中起着至关重要的作用,并参与各种生物学过程,包括肿瘤发展和免疫反应。

  • GC11578 structure
    GC11578GSK2879552
    CAS: 1401966-69-5
    纯度: >99.50%

    An LSD1 inhibitor

  • GC11792 structure
    GC11792OG-L002 HCl
    CAS: 1357298-75-9

    An LSD1 inhibitor

  • GC11873 structure
    GC118732,4-Pyridinedicarboxylic Acid
    CAS: 499-80-9
    纯度: >99.00%

    An inhibitor of 2-oxoglutarate-dependent enzymes

  • GC12288 structure
    GC12288GSK-J1 sodium salt
    CAS: 1797832-71-3

    A dual inhibitor of JMJD3 and UTX

  • GC12458 structure
    GC12458N-Oxalylglycine
    CAS: 5262-39-5

    An inhibitor of JMJD2 histone demethylases

  • GC12557 structure
    GC12557ML324
    CAS: 1222800-79-4
    纯度: >98.50%

    A cell-permeable inhibitor of JMJD2 demethylases

  • GC12997 structure
    GC12997GSK J4 free base
    CAS: 1373423-53-0
    纯度: >99.50% / >98.00%

    GSK J4 free base 是 H3K27me3/me2-去甲基化酶 JMJD3/KDM6B 和 UTX/KDM6A 的有效双重抑制剂,IC50 分别为 8.6 和 6.6 μM。 GSK J4 游离碱抑制 LPS 诱导的 TNF-α;在人原代巨噬细胞中产生,IC50 为 9 μM. GSK J4 是 GSK-J1 的细胞渗透性前药。 GSK J4 free base 诱导内质网应激相关的细胞凋亡。

  • GC13086 structure
    GC13086GSK J2
    CAS: 1394854-52-4
    纯度: >99.50%

    A negative control compound for GSK-J1

  • GC13534 structure
    GC13534Lysine-specific Demethylase Inhibitor (1C)
    CAS: 927019-63-4

    lysine-specific demethylase Inhibitor

  • GC13919 structure
    GC13919Tranylcypromine hydrochloride
    CAS: 1986-47-6

    An irreversible, mechanism-based inhibitor of LSD1

  • GC14066 structure
    GC14066Procaine
    CAS: 59-46-1
    纯度: >99.00%

    An Analytical Reference Standard

  • GC14631 structure
    GC14631SP2509
    CAS: 1423715-09-6
    纯度: >99.50%

    A reversible inhibitor of LSD1

  • GC15301 structure
    GC15301PBIT
    CAS: 2514-30-9
    纯度: >98.00% / >99.50%

    An inhibitor of JARID1 family demethylases

  • GC15368 structure
    GC15368GSK-LSD1 2HCl
    CAS: 1431368-48-7

    不可逆的、选择性的 LSD1 抑制剂

  • GC15603 structure
    GC15603JIB-04
    CAS: 199596-05-9
    纯度: >98.00%

    JIB-04是一种泛选择性Jumonji组蛋白去甲基化酶抑制剂,对JARID1A、JMJD2E、JMJD3、JMJD2A、JMJD2B、JMJD2C和JMJD2D的IC 50 值分别为230nM、340nM、855nM、445nM、435nM、1100nM和290nM。

  • GC15830 structure
    GC15830Daminozide
    CAS: 1596-84-5
    纯度: >98.00%

    Selective inhibitor of KDM2/7 histone demethylases

  • GC16114 structure
    GC16114Bizine
    CAS: 1591932-50-1
    纯度: >95.00%

    An LSD1 inhibitor

  • GC17118 structure
    GC17118GSK J5
    CAS: 1394854-51-3
    纯度: >95.00%

    A negative control compound for GSK-J4