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).
- B6120 AdoxSummary: indirect methyltransferase inhibitor
- B6168 OICR-9429Summary: Wdr5-MLL interaction antagonist
- B6182 GSK591Target: PRMTSummary: PRMT5 inhibitor
- B6183 MS0231 CitationSummary: type I PRMTs inhibitor
- B7806 HLCL-61Summary: PRMT5 inhibitor
- B7819 CPI-1205Summary: EZH2 inhibitor
- C3503 MS023 (hydrochloride)Summary: type I PRMTs inhibitor
- C3776 MS049 (hydrochloride)Summary: PRMT4 and PRMT6 inhibitor
- C4834 (S)-PFI-2 (hydrochloride)Summary: Negative control of (R)-PFI 2 hydrochloride
- B1127 UNC 0631Summary: G9a inhibitor