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K-Ras Inhibitor, SAH-SOS1A，5MG，5380920001，Sigma

销售价： ¥ 2291.92 / 件

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订货号： 0BV9925

品牌型号： Sigma 5380920001

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最小订货量： 1件

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商品介绍
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产品介绍 Product Description

General description

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.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
K-Ras
Reversible: yes

Packaging

Packaged under inert gas

Physical form

Supplied as a trifluoroacetate salt.

Preparation Note

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

Other Notes

Ac-RRFFGIXLTNXLKTEEGN (X=(S)-2-(4′-pentenyl)Ala, stapled)
Leshchiner, E. S. et al. 2015. Proc. Natl. Acad. Sci. USA.112, 1761.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

技术参数 Specifications

assay	≥95% (HPLC)
Quality Segment	100
form	solid
manufacturer/tradename	Calbiochem^®
storage condition	OK to freeze,desiccated (hygroscopic),protect from light
color	off-white
solubility	DMSO: 5 mg/mL,water: 5 mg/mL
storage temp.	−20°C

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