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).

MS115 is a selective PRMT5/MEP50 PROTAC degrader with DC50 values of 17.4 nM for PRMT5 and 11.3 nM for PRMT5 in MDAMB468 cells after 24 hours. MS115 also inhibits the proliferation of breast cancer cells.

PRMT5-IN-53 is an orally active, gut-restricted PRMT5 inhibitor, exhibiting pIC50 values of ≥ 9.7 against both hPRMT5 and mPRMT5. It binds to the PRMT5:MEP50 complex with a KD of 11.3 pM. In mice, PRMT5-IN-53 effectively inhibits intestinal PRMT5, significantly reducing both the number and size of polyps while avoiding systemic hematologic toxicity such as anemia and neutropenia. This compound is applicable in colorectal cancer research, particularly for familial adenomatous polyposis (FAP).

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.