XY1

Description	XY1 is a close analogue of SGC707, is completely inactive againstPRMT3 at concentrations as high as 100 μM. XY1 contains a naphthyl group replacing the isoquinoline group, lacks the key hydrogen bond with T466. The naphthyl ring of XY1 could act as a weak hydrogen-bond acceptor, but this should come with a substantial enthalpic penalty. The more than 1000-fold potency loss of XY1 compared with SGC707 supports this analysis. It is unclear whether other factors such as electronic effects also contributed to the potency loss of XY1 compared with SGC707. SGC707 and XY1 are a pair of excellent tools for the biomedical community to further elucidate biological functions and disease associations of PRMT3.
Pathways	Epigenetics
Targets	Histone Methyltransferase

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