mep50

LLY-283 is a potent, selective, and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, exhibiting an IC50 of 22 nM and a Kd of 6 nM for the PRMT5:MEP50 complex, and demonstrates antitumor activity.

PRMT5:MEP50 PPI, a pioneering inhibitor of the PRMT5:MEP50 protein-protein interaction (PRMT5:MEP50 PPI), demonstrates anti-tumor and anti-proliferative effects in lung and prostate cancer cells.

PRMT5-IN-1 is a covalent inhibitor of protein arginine methyltransferase 5 (PRMT5)(IC50 of 11 nM for PRMT5/MEP50).

PRMT5-IN-11 demonstrates potent structure-dependent inhibition against the protein methyltransferase PRMT5:MEP50 complex at submicromolar concentrations.

PRMT5-IN-10 exhibits promising structure-dependent inhibitory effect on the protein methyltransferase PRMT5:MEP50 complex.

PRMT5 IN-1 hydrochloride (compound 9) is a hemiacetalamine and a potent inhibitor of selective protein arginine methyltransferase 5 (PRMT5), exhibiting an inhibitory effect on PRMT5/MEP50 with an IC50 of 11 nM. Under physiological conditions, it can be converted to an aldehyde and reacts with C449 to form a covalent adduct.

PRT543 is a potent selective inhibitor of the protein arginine methyltransferase 5 (PRMT5), showing a wide range of antitumor activities in vitro and in vivo. The compound also showed an inhibitory effect on methyltransferase activity of the PRMT5/MEP50 complex with an IC50 value of 10.8 nM.