K-Ras Inhibitor, SAH-SOS1A – Calbiochem

Descrição detalhada : A cell-permeable hydrocarbon-stapled, alpha-helical peptide that mimics the native son of sevenless 1 (SOS1) helical domain (amino acids 929-944) with additional Arg-Arg tag for better cell permeability. Binds to wild-type and mutant KRAS at the SOS1 binding pocket in a sequence-specific manner and disrupts SOS1/KRAS interaction (EC50 = 79, 61, 103, 129, 140, and 124 nM for wild-type, G12D, G12V, G12C, G12S, and Q61H mutants, respectively) and blocks their nucleotide association. Reported to engage both GDP-KRAS and GTP-KRAS. Shown to impair the viability of cancer cells bearing G12D, G12C, G12V, G12S, G13D, and Q61H mutations (IC50 = 5 - 15 µM). Also diminishes the viability of HeLa and Colo320-HSR cells expressing wild-type KRAS. Inhibits the activity of MEK1/2, ERK1/2, and Akt in Panc10.05 cells treated with epidermal growth factor. Also shown to completely suppress the phosphorylation of Akt and ERK1/2 in Drosophila melanogaster expressing V12 mutant form of RAS85D upon RU486 (Cat. No. 475838) treatment.
Sinónimos : K-Ras Inhibitor, SAH-SOS1A - Calbiochem; K-Ras Inhibitor, SAH-SOS1 A; K-Ras Inhibitor, SAH-SOS1A
Fórmula molecula r: C100H159N27O28
Armazenamento : -20C
Embalagem : 1X1EA