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
基本信息
| 经验(实验)分子式 | C75H108FN25O13 |
| 分子量 | 1586.82 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem® |
| 储存条件 | OK to freeze desiccated (hygroscopic) protect from light |
| 颜色 | off-white |
| 溶解性 | water: 100 mg/mL |
| 储存温度 | −20℃ |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 1 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
