10-5498
Rasarfin
Size
£168.00
- SKU:
- 10-5498
- Physical State:
- Solid
- Molecular Weight:
- 425.91
- Purity:
- 98%
- Storage Conditions:
- -20[o]C
- Supplier:
- Focus Biomolecules
- CAS Number:
- 674359-73-0
- Immunogen:
- GTPase
- 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
- Shipping Conditions:
- Ambient