Cyclorasin 9A5-Calbiochem

产品说明

一般描述

A cell-permeable 11-mer cyclic peptide that displays high-affinity towards Ras-GTP (IC₅₀ = 120 nM for K-Ras G12V) and inhibits Ras signaling. Shown to readily localize into cytoplasm and directly bind to Ras-GTP near the effector-binding site in a reversible manner. Dose-dependently impairs Ras-B-Raf interaction and blocks EGF-stimulated activation of Akt, MEK & ERK (IC₅₀ = 3.1 µM in H1299 cells). Efficiently induces lung cancer cell growth arrest and triggers apoptosis (LD₅₀ = 3.0 µM in H1299). NOTE: ala = D-Alanine; nal = D-2-naphthylalanine; nle = D-norleucine; Fpa = L-4-Fluorophenylalanine
A cell-permeable 11-mer cyclic peptide that displays high-affinity towards Ras-GTP (IC₅₀ = 120 nM for K-Ras G12V) and inhibits Ras signaling. Shown to readily localize into cytoplasm and directly bind to Ras-GTP near the effector-binding site in a reversible manner. Dose-dependently impairs Ras-B-Raf interaction and blocks EGF-stimulated activation of Akt, MEK & ERK (IC₅₀ = 3.1 µM in H1299 cells). Efficiently induces lung cancer cell growth arrest and triggers apoptosis (LD₅₀ = 3.0 µM in H1299). NOTE: ala = D-Alanine; nal = D-2-naphthylalanine; nle = D-norleucine; Fpa = L-4-Fluorophenylalanine

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

生化/生理作用

Cell permeable: yes
Target IC₅₀: 120 nM for K-Ras G12V
Primary Target
Ras-GTP
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

序列

cyclo(-Trp-Thr-ala-Arg-Arg-Arg-nal-Arg-Fpa-nle-Gln)

外形

Supplied as a trifluoroacetate salt.

重悬

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

其他说明

Upadhyaya. P., et al. 2015. Angew. Chem. Int. Ed.54, 7602.

法律信息

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

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