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)

  • GC36656 structure
    GC36656MS049
    CAS: 1502816-23-0
    纯度: >98.00%

    A selective, dual PRMT4/PRMT6 inhibitor

  • GC36969 structure
    GC36969PRMT5-IN-1
    CAS: 2366149-83-7

    PRMT5 IN-1 是一种半缩醛胺，共价的蛋白质精氨酸甲基转移酶5 (PRMT5) 抑制剂，对 PRMT5/MEP50 的 IC50 为 11 nM。PRMT5 IN-1在生理条件下可以转化为醛并与 C449 反应形成共价加合物。

  • GC37654 structure
    GC37654SMYD3-IN-1
    CAS: 2095160-79-3

    SMYD3-IN-1 (compound 29) 是一种不可逆的、选择性的SMYD3 的抑制剂，其IC50 值为 11.7 nM。

  • GC37856 structure
    GC37856UNC0321
    CAS: 1238673-32-9
    纯度: >98.00%

    A highly potent inhibitor of G9a histone methyltransferase

  • GC37881 structure
    GC37881Valemetostat tosylate
    CAS: 1809336-93-3
    纯度: >99.50%

    Valemetostat tosylate (DS-3201 tosylate) 是一种首创的 EZH1/2 抑制剂，用于复发/难治性周围 T 细胞淋巴瘤的研究。

  • GC38062 structure
    GC38062Gambogenic acid
    CAS: 173932-75-7
    纯度: >99.50% / >98.00%

    Gambogenic acid是藤黄的主要活性成分，能抑制Aurora A激酶，IC 50 值为1.425μM。

  • GC38163 structure
    GC38163Tazemetostat hydrobromide
    CAS: 1467052-75-0
    纯度: >99.00%

    Tazemetostat hydrobromide (EPZ-6438 hydrobromide) 是一种有效，选择性，口服的 EZH2 抑制剂。Tazemetostat hydrobromide 抑制含有 PRC2 复合体的野生型 EZH2 的活性， Ki 值为 2.5±0.5 nM。Tazemetostat hydrobromide 抑制 EZH2，在肽测定和核小体测定中 IC50 分别为 11 和 16 nM。Tazemetostat hydrobromide 抑制大鼠 EZH2，IC50 为 4 nM。Tazemetostat hydrobromide 还抑制 EZH1，IC50 为 392 nM。

  • GC39407 structure
    GC39407MS1943
    CAS: 2225938-17-8
    纯度: >98.00%

    A PROTAC that drives EZH2 degradation

  • GC39663 structure
    GC39663BI-9321 trihydrochloride
    CAS: 2387510-87-2
    纯度: >98.50%

    BI-9321 trihydrochloride 是一种有效的，选择性的，具有细胞活性的 NSD3-PWWP1 拮抗剂，Kd 值为 166 nM。BI-9321 对 NSD2-PWWP1 和 NSD3-PWWP2 无效。BI-9321 trihydrochloride 在 U2OS 细胞中特异性破坏 NSD3-PWWP1 与组蛋白相互作用，IC50 为 1.2 μM。

  • GC39665 structure
    GC39665CMP-5
    CAS: 880813-42-3
    纯度: >98.50%

    CMP-5 是一种有效的选择性 PRMT5 抑制剂，对 PRMT1，PRMT4 和 PRMT7 酶无活性。CMP-5 在组蛋白的准备过程中，通过抑制 PRMT5 甲基转移酶活性选择性地阻断 S2Me-H4R3。CMP-5 阻断 EBV 驱动的 B 淋巴细胞转化，但对正常 B 细胞没有影响。

  • GC39840 structure
    GC39840AMI-1 free acid
    CAS: 134-47-4
    纯度: >97.00%

    AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively.

  • GC41263 structure
    GC41263TP-064
    CAS: 2080306-20-1
    纯度: >98.00%

    A potent inhibitor of PRMT4

  • GC42784 structure
    GC42784AMI-1 (sodium salt)
    纯度: >99.00%

    A cell permeable inhibitor of PRMTs

  • GC42790 structure
    GC42790Amodiaquine
    CAS: 86-42-0
    纯度: >98.00%

    Amodiaquine是一种4-氨基喹啉类化合物，主要用于疟疾的治疗，还具有抗炎、抗病毒作用。Amodiaquine是一种核受体Nurr1激动剂，EC 50 值约为20μM。

  • GC42944 structure
    GC42944BIX01294 (hydrochloride hydrate)
    CAS: 1808255-64-2
    纯度: >98.00%

    An inhibitor of G9a histone methyltransferase

  • GC43354 structure
    GC43354Cysmethynil
    CAS: 851636-83-4
    纯度: >98.00%

    An inhibitor of protein prenylation

  • GC43715 structure
    GC43715Furamidine (hydrochloride)
    CAS: 55368-40-6
    纯度: >98.00%

    A selective PRMT1 inhibitor and antiprotozoal agent

  • GC43837 structure
    GC43837Histone H3 Peptide Substrate (1-21)
    纯度: >95.00%

    Target substrate for several histone modifying enzymes

  • GC44859 structure
    GC44859S-(5'-Adenosyl)-L-methionine chloride (hydrochloride)
    CAS: 86867-01-8
    纯度: >95.00%

    Ubiquitous methyl donor

  • GC44886 structure
    GC44886S-Farnesyl Thioacetic Acid
    CAS: 135784-48-4
    纯度: >97.00%

    A competitive inhibitor of SAM-dependent methyltransferase

  • GC45117 structure
    GC45117UNC2327
    CAS: 1426152-53-5
    纯度: >98.00%

    An allosteric inhibitor of PRMT3

  • GC45389 structure
    GC45389BAY-6035
    CAS: 2247890-13-5
    纯度: >95.00%

    An inhibitor of SMYD3

  • GC45609 structure
    GC45609ZLD1039
    CAS: 1826865-46-6
    纯度: >98.00%

    An inhibitor of EZH2

  • GC45763 structure
    GC45763Tolcapone-d4
    CAS: 1246816-93-2
    纯度: >99.00%

    An internal standard for the quantification of tolcapone