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Product Sizes
5 mg
£168.00
10-5498-5MG
25 mg
£320.00
10-5498-25MG
About this Product
SKU:
10-5498
CAS Number:
674359-73-0
Extra Details:
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 uM for ARF and Ras respectively with no inhibition of Rac/Cdc42 and Rho up to 100 uM. 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 uM) 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
Immunogen:
GTPase
Molecular Weight:
425.91
Physical State:
Solid
Purity:
98%
Shipping Conditions:
Ambient
Storage Conditions:
-20[o]C
Supplier:
Focus Biomolecules
Type:
Proteins, Peptides, Small Molecules & Other Biomolecules: Inhibitors