Temuterkib (LY3214996)

Description: LY3214996 is a novel, highly potent, selective and orally bioavailable inhibitor of the ERK1 (extracellular signal-regulated kinase) and ERK2, with IC50 value of 5 nM for both enzymes (ERK1/2) in biochemical assays. LY3214996 inhibits both ERK 1 and 2, thereby preventing the activation of the MAPK (mitogen-activated protein kinase)/ERK-mediated signal pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines. Therefore, LY-3214996 has the potential to be developed as an antineoplastic drug. LY3214996 also significantly inhibited the growth and migration of the AGO1 cells.

References: Cancer Research 77(13 Supplement):3231-3231; Cell Death Dis. 2018 Feb 27; 9(3):324.