Chemical Name: N-(3-Chloro-4-(4-isobutyrylpiperazin-1-yl)phenyl)benzofuran-2-carboxamide
Dual Ras/ARF6 inhibitor
Molecular Weight:
425.91
Purity:
98% by TLC NMR (Conforms)
Form:
Yellow solid
CAS Number:
[674359-73-0]
Formula:
C23H24ClN3O3
Application Notes:
Dual inhibitor of Ras and ARF6 discovered by screening a library of over 115,000 small molecules employing an endosomal BRET-based assay with the prototypical GPCR angiotensin II type 1 receptor (AT1R) seeking to identify inhibitors of receptor trafficking. IC50=7 and 0.7 µM for ARF and Ras respectively with no inhibition of Rac/Cdc42 and Rho up to 100 µM. It blocks agonist-mediated internalization of AT1R and other GPCRs. It also potently inhibits agonist-induced ERK1/2 signaling by GPCRs and MAPK and AKT signaling by EGFR (IC50=4-5 µM) and prevents cancer cell proliferation. Rasarfins direct action on Ras was also verified using purified H-Ras in an in vitro GEF exchange assay.1
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