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].
Kinase Assay
Cell Assay
Animal Administration
References
[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.
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