XY1 |
| カタログ番号GC19388 |
XY1 は SGC707 (31 nM の IC50 を持つ強力で選択的な PRMT3 の非競合的阻害剤) の非常に近い類似体ですが、XY1 は完全に不活性です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1624117-53-8
Sample solution is provided at 25 µL, 10mM.
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XY1 is a very close analogue of SGC707 (a potent, selective, and non-competitive inhibitor of PRMT3 with IC50 of 31 nM), but XY1 is completely inactive.Target: PRMT3XY1 is a close analogue of SGC707, is completely inactive againstPRMT3 at concentrations as high as 100 uM. 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.
References:
[1]. Kaniskan H, et al. A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3). Angew Chem Int Ed Engl. 2015 Apr 20;54(17):5166-70.
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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