半岛bd体育手机客户端 说明
一般描述
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 ?M). 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 inDrosophila melanogasterexpressing V12 mutant form of RAS85D upon RU486 (Cat. No. 475838) treatment.
生化/生理作用
Cell permeable: yes
Reversible: yes
Primary Target
K-Ras
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
序列
Ac-RRFFGIXLTNXLKTEEGN (X=(S)-2-(4′-pentenyl)Ala, stapled)
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
Leshchiner, E. S. et al. 2015.Proc. Natl. Acad. Sci. USA.112,1761.
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 | C100H159N27O28 |
| 分子量 | 2187.50 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥95% (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 | DMSO: 5 mg/mL water: 5 mg/mL |
| 储存温度 | ?20℃ |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
Sigma-Aldrich
m.cnreagent.com
