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).
- A4502 ChaetocinSummary: SUV39H1 Inhibitor
- A4504 UNC 0646Summary: G9a and GLP inhibitor
- A4503 UNC 0224Summary: G9a histone methyltransferase inhibitor
- A8221 EPZ-64385 CitationSummary: EZH2 inhibitor, potent and selective
- B1582 MM-1021 CitationSummary: MLL1 inhibitor,high-affinity peptidomimetic
- B1583 UNC19992 CitationTarget: EZH2|EZH1Summary: EZH2 inhibitor
- B1622 SGI-1027Summary: DNMT inhibitor
- B8210 (R)-PFI 2 hydrochloride
- B4875 PFI-21 CitationTarget: SETD7Summary: SETD7 methyltransferase inhibitor
- B4947 A 366Summary: G9a/GLP histone lysine methyltransferase inhibitor