PRMT1-2e is a potent, specific and cell permeable inhibitor of protein arginine methyltransferase 1 (PRMT1) with an IC₅₀ ~1.5 μM. It has no activity against CARM1 and Set7/9 methyltransferases. It inhibits growth of MCF7a breast cancer cells (IC₅₀ ~1.97 μM) and LNCaP prostate cancer cells (IC₅₀ ~4.49 μM). It can attenuate androgen-induced gene expression in LNCaP cells.

How to Use:

• In vitro: PRMT1-2e was used at 10 µM in vitro.
• In vivo: n/a

Reference:

1. 1. Bissinger EM, et al. Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methyltransferase hPRMT1. (2011) Bioorg Med Chem. 19(12):3717-31.

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