Rasarfin

CAT: 0498-bs-83128C-01Size: 5 mgDry Ice: NoHazardous: No

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CAT#:0498-bs-83128C-01Size:5 mg

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24/48H Stock Items & 2 to 6 Weeks non Stock Items.

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Background

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

Conjugation

Unconjugated

Buffer

Yellow solid

Storage Conditions

-20°C

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Catalog	Name
MBS3617191-01	Rasarfin
A24571-10	Rasarfin 10mg
A24571-5	Rasarfin 5mg
A24571-50	Rasarfin 50mg
A24571-1	Rasarfin 1mg

Rasarfin

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