Biological ActivitySelective protein arginine methyltransferase 1 (PRMT1) inhibitor (IC50 = 1.8 μM). Exhibits five-fold selectivity for PRMT1 over PRMT6 and >250-fold selectivity over PRMT3 and CARM1.
(Modifications: Ser-1 = N-terminal Ac, X = N5-(2-Chloro-1-iminoethyl)]-Orn)
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
A chloroacetamidine-based inactivator of protein arginine methyltransferase 1: design, synthesis, and in vitro and in vivo evaluation.
Obianyo et al.
Kinetic mechanism of protein arginine methyltransferase 6 (PRMT6).
Obianyo and Thompson
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