半岛bd体育手机客户端 说明
一般描述
A cell-permeable, stabilized hydrocarbon-stapled α-helical peptide that targets a critical protein-protein interface and prevents assembly in the NOTCH1 trans-activation complex. Soluble FITC-SAHM1 was found to bind the pre-formed RAMANK-CSL complex (Kd= 0.12 ?M) competitively with MAML1, whereas the unmodified FITC-MAML1 (21-36) peptide bound the complex with markedly diminished affinity in anin vitropull down assay. Treatment of KOPT-K1 cell lines with 20 ?M of compound results in the suppression of NOTCH1 target genes,HES4, DTX1,andHES1. A consistent repressive effect on NOTCH1-activated gene expression by this compound was observed across a panel of human T-ALL cell lines, containing diverse mutantNOTCH1alleles. In HeLa cells, this peptide also inhibited the expression of ICN1 (IC50= 6.56 ?M) dose-dependently in a luciferase reporter-gene assay, as well as that of β-lactamase (IC50<2.5 ?M) in a second reporter-gene assay. Furthermore, treatment with this peptide inhibits NOTCH-mediated proliferation in cultured cells at 15 ?M, and in a mouse model of T-ALL cells at 30 mg/kg twice daily.
包装
1 mg in Glass bottle
警告
Toxicity: Standard Handling (A)
序列
Acetyl-βAla-ERLRRRI*LCR*HHST
* = Two S5 molecules (a non-natural alkenyl amino acid) stapled together with a double bond
重悬
Following reconstitution, aliquot and freeze (-20℃). Stock solutions are stable for up to 3 months at -20℃.
其他说明
Moellering, R.E., et al. 2009.Nature462,182.
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 | C94H162N36O23S · 7C2HF3O2· 13H2O |
| 分子量 | 3228.95 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥93% (HPLC) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem? |
| 储存条件 | OK to freeze |
| 颜色 | off-white |
| 溶解性 | DMSO: 50 mg/mL |
| 运输 | wet ice |
| 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 |
Sigma-Aldrich
m.cnreagent.com
