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).
- B8210 (R)-PFI 2 hydrochloride
- B4875 PFI-21 CitationTarget: SETD7Summary: SETD7 methyltransferase inhibitor
- B4947 A 366Summary: G9a/GLP histone lysine methyltransferase inhibitor
- B4948 UNC 2400Summary: negative control of UNC1999
- B4949 WDR5 0103Summary: WD repeat-containing protein 5 (WDR5) antagonist
- B4989 EPZ015666Target: Protein Arginine MethyltransferasesSummary: PRMT5 inhibitor
- B5913 C7280948Summary: Novel PRMT1 inhibitor
- B6048 SGC707Summary: PRMT3 inhibitor
- A1905 3-Deazaneplanocin,DZNep6 CitationTarget: HydrolaseSummary: S-adenosylhomocysteine and EZH2 inhibitor
- A1908 AMI-1Summary: PRMT1 inhibitor