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Histone Methyltransferase

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).

  1. Cat.No. Product Name Information
  2. GC45908 (R)-BAY-598
  3. GC11340 (R)-PFI 2 hydrochloride SETD7 histone lysine methyltransferase inhibitor
  4. GC13634 (S)-PFI-2 (hydrochloride) Negative control of (R)-PFI 2 hydrochloride
  5. GC17907 3-Deazaneplanocin A (DZNep) hydrochloride A SAHH and ENZ2 inhibitor
  6. GC13145 3-Deazaneplanocin,DZNep

    S-adenosylhomocysteine and EZH2 inhibitor

  7. GC16015 A 366 G9a/GLP histone lysine methyltransferase inhibitor
  8. GC32861 A-196 A-196是有效的选择性SUV420H1和SUV420H2化学抑制剂,在多种细胞系中抑制H4K20me二甲基化和三甲基化。
  9. GC33187 A-395 (A395) A-395是一种新型的Polycomb抑制复合物2(Polycombrepressivecomplex2(PRC2))蛋白质-蛋白质相互作用的拮抗剂,抑制三聚体PRC2复合物(EZH2-EED-SUZ12)的IC50值为18nM。
  10. GC30503 A-893 A-893是一个有细胞活性的,SMYD2的抑制剂,其IC50值为2.8nM。
  11. GC16509 Adox

    indirect methyltransferase inhibitor

  12. GC17275 AMI-1 PRMT1 inhibitor
  13. GC39840 AMI-1 free acid AMI-1 free acid 是一种有效的,细胞渗透性的,可逆的蛋白精氨酸 N-甲基转移酶 (PRMTs) 抑制剂,对人 PRMT1 和酵母 Hmt1p 作用的 IC50 值分别为 8.8 μM 和 3.0 μM。AMI-1 free acid 通过阻断肽-底物结合对 PRMTs 发挥抑制作用。
  14. GC17546 AMI5 protein methyltransferase inhibitor
  15. GC42790 Amodiaquine Amodiaquine is an aminoquinoline antimalarial compound.
  16. GC60579 Amodiaquine dihydrochloride Amodiaquinedihydrochloride(Amodiaquindihydrochloride)是一种4-氨基喹啉类抗疟剂,是一种有效的具有口服活性的组胺N-甲基转移酶(histamineN-methyltransferase)抑制剂,Ki值为18.6nM。Amodiaquinedihydrochloride也是一种Nurr1激动剂,可特异性结合Nurr1的配体结合域,EC50为~20μM。抗炎作用。
  17. GC10905 Amodiaquine dihydrochloride dihydrate histamine N-methyl transferase inhibitor
  18. GC62615 AS-99 AS-99 是首创的、有效的、选择性的 ASH1L 组蛋白甲基转移酶抑制剂 (IC50= 0.79 µM, Kd= 0.89 µM),具有抗白血病活性。AS-99 在体内阻断细胞增殖,诱导细胞凋亡 (apoptosis) 和分化,下调 MLL 融合靶基因,减轻白血病。
  19. GC13744 AZ505 SMYD2 inhibitor,potent and selective
  20. GC13103 AZ505 ditrifluoroacetate SMYD2 inhibitor
  21. GC18159 BAY-598 A potent and selective SMYD2 inhibitor

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