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)

  • 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。

  • GC18161 structure
    GC18161BCI-121
    CAS: 432529-82-3
    纯度: >99.00%

    An inhibitor of SMYD3

  • GC18428 structure
    GC18428SGC2085 (hydrochloride)
    CAS: 1821908-49-9

    A PRMT4/CARM1 inhibitor

  • GC18577 structure
    GC18577CID-2818500
    CAS: 1215-07-2

    An inhibitor of PRMT1

  • GC18642 structure
    GC18642SW155246
    CAS: 420092-79-1

    A DNA methyltransferase 1 inhibitor

  • GC18650 structure
    GC18650S-(5'-Adenosyl)-L-methionine (tosylate)
    CAS: 52248-03-0
    纯度: >98.00%

    S-Adenosyl-L-methioninetosylate(S-Adenosylmethioninetosylate)是通过蛋氨酸腺苷转移酶的作用由蛋氨酸和ATP内源性生产的，是一种重要的具有口服活性的甲基供体。

  • GC18949 structure
    GC18949CAY10677
    CAS: 1443253-20-0

    An inhibitor of protein prenylation

  • GC19130 structure
    GC19130EED226
    CAS: 2083627-02-3
    纯度: >98.50%

    EED226是一种强效的多梳抑制复合物2（PRC2）抑制剂，IC 50 值为22.3nM。

  • GC19141 structure
    GC19141EPZ011989
    CAS: 1598383-40-4
    纯度: >99.50%

    An orally bioavailable EZH2 inhibitor

  • GC19149 structure
    GC19149EZM 2302
    CAS: 1628830-21-6
    纯度: >99.00%

    EZM 2302是一种对CARM1有效的且具有选择性的抑制剂，其IC 50 值为6nM。

  • GC19181 structure
    GC19181GSK2807 Trifluoroacetate
    CAS: 2245255-66-5

    GSK2807 Trifluoroacetate 是一种有效的、选择性的、SAM 竞争性的 SMYD3 抑制剂，Ki 为 14 nM，IC50 为 130 nM。

  • GC19211 structure
    GC19211JQEZ5
    CAS: 1913252-04-6
    纯度: >98.00%

    An EZH2 inhibitor

  • GC19329 structure
    GC19329SGC2085
    CAS: 1821908-48-8
    纯度: >99.50%

    A PRMT4/CARM1 inhibitor

  • GC19388 structure
    GC19388XY1
    CAS: 1624117-53-8
    纯度: >99.00%

    A negative control for SGC707

  • GC19465 structure
    GC19465JNJ-64619178
    CAS: 2086772-26-9
    纯度: >99.50%

    A PRMT5 inhibitor

  • GC19849 structure
    GC19849SGC3027
    CAS: 2624313-13-7
    纯度: >98.50% / >98.00%

    A prodrug form of SGC8158

  • GC25159 structure
    GC25159BMF-219
    CAS: 2448172-22-1
    纯度: >98.00%

    BMF-219是一种高选择性和不可逆的menin抑制剂,在小鼠模型中具有良好的抑制效果 。

  • GC30503 structure
    GC30503A-893
    CAS: 1868232-32-9

    A-893是一个有细胞活性的，SMYD2的抑制剂，其IC50值为2.8nM。

  • GC30530 structure
    GC30530Dot1L-IN-2
    CAS: 1940206-71-2

    Dot1L-IN-2是一种有效的，选择性的，可口服的Dot1L(一种histonemethyltransferase)，IC50值和Ki值分别为0.4nM和0.08nM。

  • GC32693 structure
    GC32693GSK3326595 (EPZ015938)
    CAS: 1616392-22-3
    纯度: >99.50% / >99.00%

    GSK3326595 (EPZ015938) 是一种具有口服活性的、有效的、选择性protein arginine methyltransferase 5（PRMT5）抑制剂。

  • GC32861 structure
    GC32861A-196
    CAS: 1982372-88-2
    纯度: >98.00%

    A selective inhibitor of SUV420H1 and SUV420H2

  • GC32977 structure
    GC32977PF-06726304
    CAS: 1616287-82-1
    纯度: >99.50%

    PF-06726304是有效，选择性的EZH2抑制剂，Ki值为0.7nM。

  • GC32988 structure
    GC32988BRD9539
    CAS: 1374601-41-8
    纯度: >99.00%

    An inhibitor of EHMT2/G9a and PRC2 in enzyme assays

  • GC33184 structure
    GC33184LLY-283
    CAS: 2040291-27-6
    纯度: >99.00%

    A PRMT5 inhibitor