EUB0000271b_PRMT6

Screened at 1 µM and 10 µM, clean against a panel of 8 PRMTs, 21 protein lysine methyltransferases, 3 DNA methyltransferases, and one RNA methyltransferase, targets as % of activity in the screen at 1 µM: PRMT6 (17%), PRMT1 (>90%), PRMT3 (>90%), PRMT4 (>90%), PRMT5 (>90%), PRMT7 (>90%), PRMT8 (>90%), PRMT9 (>90%), G9a (>90%), GLP (>90%), SETDB1 (>90%), SUV39H1 (>90%), SUV39H2 (>90%), SUV420H1 (>90%), SUV420H2 (>90%), SETD7 (>90%), SETD8 (>90%), MLL1 (>90%), MLL3 (>90%), PRDM9 (>90%), PRC2 (>90%), SETD2 (>90%), SMYD2 (>90%), SMYD3 (>90%), BCDN3D (>90%), DNMT1 (>90%), DNMT3A/3L (>90%), DNMT3B/3L (>90%), DOT1L (>90%), ASH1L (>90%), NSD1 (>90%), NSD2(>90%),NSD3(>90%); Targets as % of activity in the screen at 10 µM: PRMT6 (8%), PRMT1 (>90%), PRMT3 (>90%), PRMT4 (>90%), PRMT5 (>90%), PRMT7 (>90%), PRMT8 (>90%), PRMT9 (>90%), G9a (>90%), GLP (>90%), SETDB1 (>90%), SUV39H1 (>90%), SUV39H2 (>90%), SUV420H1 (>90%), SUV420H2 (>90%), SETD7 (>90%), SETD8 (>90%), MLL1 (>90%), MLL3 (>90%), PRDM9 (>90%), PRC2 (>90%), SETD2 (>90%), SMYD2 (>90%), SMYD3 (>90%), BCDN3D (>90%), DNMT1 (>90%), DNMT3A/3L (>90%), DNMT3B/3L (>90%), DOT1L (>90%), ASH1L (>90%), NSD1 (>90%), NSD2(>90%),NSD3(>90%); Screened against 44 non-epigenetic targets by Eurofins (kinases, GPCRs, ion channels and transporters) at 1 μM, closest target as % of inhibition: KOP (20%), COX1 (17%), GR (15%), 5-HT2A (12%), M3 (12%), MAOA (12%), D1 (9%), acetylcholinesterase (7%), https://pubmed.ncbi.nlm.nih.gov/33591753/;