538092 Sigma-AldrichK-Ras Inhibitor, SAH-SOS1A - Calbiochem
Empfohlene Produkte
Übersicht
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Key Spec Table
| Empirical Formula |
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| C₁₀₀H₁₅₉N₂₇O₂₈ |
Preis & Verfügbarkeit
| Bestellnummer | Verfügbarkeit | Verpackung | St./Pkg. | Preis | Menge | |
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| 5380920001 |
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Glasflasche | 5 mg |
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| Description | |
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| Overview | 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. |
| Catalogue Number | 538092 |
| Brand Family | Calbiochem® |
| Synonyms | K-Ras Inhibitor, SAH-SOS1A |
| References | |
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| References | Leshchiner, E. S. et al. 2015. Proc. Natl. Acad. Sci. USA. 112, 1761. |
| Product Information | |
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| Form | Off-white solid |
| Formulation | Supplied as a trifluoroacetate salt. |
| Hill Formula | C₁₀₀H₁₅₉N₂₇O₂₈ |
| Chemical formula | C₁₀₀H₁₅₉N₂₇O₂₈ |
| Hygroscopic | Hygroscopic |
| Reversible | Y |
| Quality Level | MQ100 |
| Applications |
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| Biological Information | |
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| Primary Target | K-Ras |
| Purity | ≥95% by HPLC |
| Physicochemical Information | |
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| Cell permeable | Y |
| Peptide Sequence | Ac-RRFFGIXLTNXLKTEEGN (X=(S)-2-(4'-pentenyl)Ala, stapled) |
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| Toxicological Information |
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| Safety Information according to GHS |
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| Safety Information |
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| Product Usage Statements |
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| Packaging Information | |
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| Packaged under inert gas | Packaged under inert gas |
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| Specifications |
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| Global Trade Item Number | |
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| Bestellnummer | GTIN |
| 5380920001 | 04054839119422 |
Documentation
K-Ras Inhibitor, SAH-SOS1A - Calbiochem SDB
| Titel |
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Literatur
| Übersicht |
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| Leshchiner, E. S. et al. 2015. Proc. Natl. Acad. Sci. USA. 112, 1761. |
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Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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