bs-83128C

DATASHEET

Formulation Orange solid

Storage: -20°C

Product Information:

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. Rasarfin’s direct action on Ras was also verified using purified H-Ras in an in vitro GEF exchange assay.1

Description:

CAS Number: 674359-73-0 Chemical Name: N-(3-Chloro-4-(4-isobutyrylpiperazin-1-yl)phenyl)benzofuran-2-carboxamide Molecular weight: 425.91 Formula: C23H24ClN3O3 Solubility: DMSO (70 mg/ml) Physical Properties: Yellow solid Purity: 98% by TLC NMR (Conforms)