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)

  • GC45908 structure
    GC45908(R)-BAY-598
    CAS: 1906920-28-2
    纯度: >98.00%

    An inhibitor of SMYD2

  • GC45927 structure
    GC45927DS-437
    CAS: 1674364-87-4
    纯度: >98.00%

    A dual inhibitor of PRMT5 and PRMT7

  • GC46213 structure
    GC46213Ro 41-0960
    CAS: 125628-97-9
    纯度: >98.00%

    A COMT inhibitor

  • GC47180 structure
    GC47180Decitabine-15N4
    纯度: >95.00%

    A neuropeptide with diverse biological activities

  • GC47294 structure
    GC47294Entacapone-d10
    CAS: 1185241-19-3
    纯度: >99.00%

    An internal standard for the quantification of entacapone

  • GC48463 structure
    GC48463Bisubstrate Inhibitor 78
    CAS: 2368247-39-4
    纯度: >98.00%

    An inhibitor of NNMT

  • GC48967 structure
    GC48967D-Homoserine lactone
    CAS: 51744-82-2
    纯度: >95.00%

    An enantiomer of L-homoserine lactone

  • GC48980 structure
    GC48980EPZ004777 (formate)
    纯度: >98.00%

    DOT1L 的有效抑制剂

  • GC49398 structure
    GC49398GSK3368715 (hydrochloride)
    CAS: 2227587-25-7
    纯度: >98.00%

    An inhibitor of type I PRMTs

  • GC50082 structure
    GC50082UNC 2399
    CAS: 2412791-72-9

    UNC 2399 是一种生物素化的 UNC1999，是一种选择性 EZH2 降解剂，对 EZH2 保持高效的体外效力，IC50 为 17 nM。

  • GC50367 structure
    GC50367PF 06726304 acetate
    CAS: 2080306-28-9

    Highly potent and SAM-competitive EZH2 inhibitor

  • GC50540 structure
    GC50540BI 9321
    CAS: 2387510-86-1

    Nuclear receptor-binding SET domain (NSD) 3 antagonist; selectively binds PWWP1 domain

  • GC50576 structure
    GC50576MRK 740
    CAS: 2387510-80-5
    纯度: >99.00%

    Potent PRDM9 inhibitor

  • GC50697 structure
    GC50697GSK 591 dihydrochloride
    CAS: 2320953-89-5
    纯度: >97.00%

    A chemical probe for PRMT5

  • GC50699 structure
    GC50699SGC 6870
    CAS: 2561471-27-8
    纯度: >98.00%

    Potent and selective protein arginine methyltransferase 6 (PRMT6) inhibitor (IC50 = 77 nM)

  • GC60579 structure
    GC60579Amodiaquine dihydrochloride
    CAS: 69-44-3
    纯度: >98.00%

    A prodrug form of N-desethyl amodiaquine

  • GC61058 structure
    GC61058Metoprine
    CAS: 7761-45-7
    纯度: >99.00%

    Metoprine(BW197U)是一种有效的组胺N-甲基转移酶(HMT)抑制剂。Metoprine是一种二氨基嘧啶衍生物，可以透过血脑屏障，并通过抑制HMT增加脑组胺水平。Metoprine是一种抗叶酸(antifolate)和抗肿瘤药。

  • GC61142 structure
    GC61142NSC745885
    CAS: 4219-52-7
    纯度: >98.00%

    NSC745885是一种有效的抗肿瘤(anti-tumor)试剂，对多种癌细胞株有选择性毒性，但对正常细胞没有毒性。NSC745885是一种有效的EZH2的下调因子通过蛋白酶体降解途径。NSC745885为晚期膀胱癌和口腔鳞癌的研究提供了可能性。

  • GC61468 structure
    GC61468MR837
    CAS: 1210906-48-1
    纯度: >99.00%

    MR837是一种NSD2-PWWP1的抑制剂。MR837可以与人核受体结合SET结构域蛋白(PWWP结构域)结合。

  • GC62187 structure
    GC62187PROTAC EED degrader-1
    CAS: 2639882-72-5
    纯度: >99.50%

    PROTAC EED degrader-1 是靶向 EED 的 PROTAC 分子，pKD 为 9.02。PROTAC EED degrader-1 是靶向 EED 亚基的多梳抑制复合物 2 (PRC2) 抑制剂 (pIC50=8.17)。

  • GC62390 structure
    GC62390SW2_110A
    纯度: >99.00%

    SW2_110A 是一种选择性 chromobox 8 chromodomain (CBX8 ChD) 抑制剂，Kd 为 800 nM。SW2_110A 在体外对 CBX8 ChD 的选择性比所有其他 CBX 旁系同源物低 5 倍。

  • GC62555 structure
    GC62555EZM0414 (SETD2-IN-1) TFA
    CAS: 2411759-92-5
    纯度: >99.00% / >96.00%

    EZM0414 (SETD2-IN-1) TFA是EZM0414的三氟乙酸盐（TFA）形式。EZM0414 是一种首创的、强效的、选择性的、口服生物活性的小分子SETD2抑制剂，其IC 50 值为18nM。

  • GC62558 structure
    GC62558WDR5-IN-1
    CAS: 2408842-51-1
    纯度: >98.50%

    WDR5-IN-1 是一种有效的选择性 WD 重复结构域 5 (WDR5) 抑制剂，Kd 为 <0.02 nM。WDR5-IN-1 抑制 MLL1 组蛋白甲基转移酶活性 (HMT)，IC50为 2.2 nM。WDR5-IN-1 减少 WDR5 移位基因的 MYC 募集，并在 CHP-134 (神经母细胞瘤) 和 Ramos (Burkitt淋巴瘤) 细胞系中显示出有效的抗增殖作用。

  • GC62613 structure
    GC62613Dot1L-IN-4
    CAS: 2565705-02-2
    纯度: >99.50%

    A DOT1L inhibitor