5.38092

K-Ras Inhibitor, SAH-SOS1A

• Sinonimo/i: K-Ras Inhibitor, SAH-SOS1A, K-Ras Inhibitor, SAH-SOS1 _A, K-Ras Inhibitor, SAH-SOS1_A
• Formula empirica (notazione di Hill): C₁₀₀H₁₅₉N₂₇O₂₈
• Peso molecolare: 2187.50
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Saggio: ≥95% (HPLC)
• Livello qualitativo: 100
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; desiccated (hygroscopic); protect from light
• Colore: off-white
• Solubilità: DMSO: 5 mg/mL; water: 5 mg/mL
• Temperatura di conservazione: −20°C

Descrizione

Descrizione generale

A cell-permeable hydrocarbon-stapled, α-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.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
K-Ras

Reversible: yes

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Sequenza

Ac-RRFFGIXLTNXLKTEEGN (X=(S)-2-(4′-pentenyl)Ala, stapled)

Stato fisico

Supplied as a trifluoroacetate salt.

Ricostituzione

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Altre note

Leshchiner, E. S. et al. 2015. Proc. Natl. Acad. Sci. USA.112, 1761.

Note legali

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable