GlpBio

Histone Methyltransferase

Histone Methyltransferase(组蛋白甲基转移酶)

Histone methyltransferases are a group of enzymes that catalyze the methylation of histone lysine and arginine by adding methyl groups to specific histone arginine or lysine residues. Histone methyltransferaes can be classified into 3 classes, including SET domain lysine methyltransferases, non-SET domain lysine methyltransferases and arginine methyltransferases (PRMTs), all of which use S-adenosylmethionine as a cosubstrate for the transfer of the methyl group. Aberrant histone methylation has been associated with a wide range of human cancers (such as hematological malignancies), which leads to the development of novel cancer chemotherapies targeting cancer-associated histone methyltransferases (more than 20 lysine methyltransferases and 9 arginine methyltransferases in humans).

Histone Methyltransferase 相关产品(238)

  • GC73957 structure
    GC73957NSD2 ligand 1
    纯度: >99.00%

    NSD2 ligand 1是NSD2配体。

  • GC73966 structure
    GC73966DCPT1061
    CAS: 2289726-31-2
    纯度: >99.00%

    DCPT1061在体外有效抑制PRMT1、PRMT6和PRMT8，对PRMT3、PRMT4和PRMT5或其他表观遗传酶的抑制作用较小。

  • GC73967 structure
    GC73967DCPT1061 hydrochloride
    纯度: >99.00%

    DCPT1061 hydrochloride在体外对PRMT1、PRMT6、PRMT8有较强的抑制作用，对PRMT3、PRMT4、PRMT5等表观遗传酶的抑制作用较小。

  • GC73982 structure
    GC73982NSD-IN-3
    CAS: 744260-15-9
    纯度: >98.00%

    NSD-IN-3（化合物3）是一种强效的核受体结合SET结构域（NSD）抑制剂。

  • GC73993 structure
    GC73993EPIC-0628
    纯度: >98.00%

    EPIC-0628是HOTAIR-EZH2相互作用的抑制剂，促进ATF3表达。

  • GC74088 structure
    GC74088EPZ011989 hydrochloride
    CAS: 2095432-26-9
    纯度: >99.00%

    EPZ011989 hydrochloride是一种有效的口服活性Zeste Homolog 2 （EZH2）抑制剂，Ki值<3 nM。

  • GC74631 structure
    GC74631PRMT5-IN-30
    CAS: 330951-01-4
    纯度: >99.00%

    PRMT5-IN-30（化合物17）是一种有效的选择性蛋白精氨酸甲基转移酶5 （PRMT5）抑制剂，IC50为0.33 μM， Kd为0.987 μM。

  • GC91025 structure
    GC91025PTD2 (trifluoroacetate salt)
    纯度: >98.00%

    一种抑制WHSC1的肽类抑制剂

  • GC91061 structure
    GC91061UNC8153 (trifluoroacetate salt)
    CAS: 2929304-61-8
    纯度: >95.00%

    NSD2的降解剂

  • GC15610 structure
    GC15610UNC0638
    CAS: 1255580-76-7
    纯度: >99.00%

    A G9a and GLP histone methyltransferase inhibitor

  • GC17907 structure
    GC179073-Deazaneplanocin A (DZNep) hydrochloride
    CAS: 120964-45-6
    纯度: >99.50%

    3-Deazaneplanocin A (DZNep) hydrochloride 是一种腺苷类似物，是一种竞争性 S-腺苷高半胱氨酸水解酶抑制剂，在无细胞试验中的 Ki 为 50 pM。

  • GC14936 structure
    GC14936Chaetocin
    CAS: 28097-03-2
    纯度: >98.00%

    据报道毛壳素是组蛋白甲基转移酶 (HMT)（例如 SUV39H1）的非特异性抑制剂，从而影响基因表达。

  • GC12548 structure
    GC12548UNC 0631
    CAS: 1320288-19-4
    纯度: >99.00%

    An inhibitor of G9a/GLP methyltransferases

  • GC13103 structure
    GC13103AZ505 ditrifluoroacetate
    CAS: 1035227-44-1
    纯度: >99.50%

    An inhibitor of SMYD2

  • GC13744 structure
    GC13744AZ505
    CAS: 1035227-43-0
    纯度: >99.50%

    An inhibitor of SMYD2

  • GC14364 structure
    GC14364SGI-1027
    CAS: 1020149-73-8
    纯度: >99.00%

    A DNA methyltransferase inhibitor

  • GC16518 structure
    GC16518UNC 0646
    CAS: 1320288-17-2
    纯度: >99.50%

    An inhibitor of G9a/GLP methyltransferases

  • GC11491 structure
    GC11491SGC 0946
    CAS: 1561178-17-3
    纯度: >99.50%

    A potent inhibitor of DOT1L

  • GC13383 structure
    GC13383EPZ004777
    CAS: 1338466-77-5
    纯度: >98.00%

    EPZ004777 作为一种有效的表观遗传调节剂，可以逆转 TGF-β1 诱导的 T 调节细胞，可用于治疗多种免疫疾病。

  • GC15259 structure
    GC15259EPZ004777 HCl
    CAS: 1380316-03-9
    纯度: >98.00%

    EPZ004777 HCl 是一种有效的选择性 DOT1L 抑制剂，IC50 为 0.4 nM。

  • GC11375 structure
    GC11375UNC1999
    CAS: 1431612-23-5
    纯度: >99.50%

    UNC1999是一种口服活性的EZH2（IC 50 =2nM）和EZH1（IC 50 =45nM）抑制剂。

  • GC14652 structure
    GC14652MM-102
    CAS: 1417329-24-8
    纯度: >98.00%

    MM-102是一种高亲和性、细胞通透性的肽模拟物，作为MLL1-WDR5蛋白相互作用的有效抑制剂，IC₅₀为2.4nM，K i <1nM。