N,N'-[Sulfonylbis(1,4-phenylene)]bis(chloroacetamide)

Description

TC-E 5003 is an inhibitor of protein arginine methyltransferase 1 (PRMT1; IC₅₀ = 1.5 μM for human PRMT1 in a methylation assay). It is selective for PRMT1 over PRMT4/CARM1 and SET7/9 methyltransferases, with less than 5% inhibition at a concentration of 50 μM for SET7/9. TC-E 5003 inhibits growth of MCF-7a breast cancer and LNCaP prostate cancer cells (GI₅₀s = 1.97 and 4.49 μM, respectively) and decreases androgen-dependent gene transcription in vitro. TC-E 5003 (80 mg/kg) also has antimalarial properties and eradicates P. berghei in mice.

Uses

NSC 30176 is a inhibitor of human PRMT1, it is selective for PRMT1 over the arginine methyltransferase CARM1 and the lysine methyltransferase Set7/9.

References

1) Bissinger?et al. (2011),?Acyl derivatives of p-aminosulfonamides and dapsone as new inhibitors of the arginine methytransferase hPRMT1; Bioorg. Med. Chem.,?19?3717