Rasarfin is a dual Ras and ARF6 inhibitor[1].
Rasarfin also potently inhibits agonist-induced ERK1/2 signaling by GPCRs, and MAPK and Akt signaling by EGFR, as well as prevents cancer cell proliferation[1].Rasarfin blocks GPCR internalization through inhibition of ARF6[1].Rasarfin treatment results in a dose-dependent reduction in MDA-MB-231 cells[1]. Rasarfin inhibits the recruitment of the clathrin adaptor AP-2 to β-arrestin2 and receptor internalization, both processes that require active ARF6[1].
[1]. Jenna Giubilaro, et al. Discovery of a dual Ras and ARF6 inhibitor from a GPCR endocytosis screen. Nat Commun. 2021 Aug 3;12(1):4688.