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491002 Notch Transcription Factor Inhibitor, SAHM1 - Calbiochem

Notch Transcription Factor Inhibitor, SAHM1, is a cell-permeable inhibitor that prevents assembly in the NOTCH1 trans-activation complex.

Notch Transcription Factor Inhibitor, SAHM1 - Calbiochem: MSDS (material safety data sheet) o SDS, certificato d’analisi (CoA) e certificato di qualità (CoQ), dossier, brochure e altri documenti disponibili.

Sinonimi: AcβA1a-ERLRRRI*LCR*HHST (*=S5)

491002
Purchase on Sigma-Aldrich

Panoramica

Replacement Information

Tabella delle specifiche principali

Empirical Formula
C₉₄H₁₆₂N₃₆O₂₃S• 7CF₃CO₂H•13H₂O

Products

Numero di catalogoConfezionamento Qtà/conf
491002-1MG Bottiglia di vetro 1 mg
Description
OverviewA 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 µM) competitively with MAML1, whereas the unmodified FITC-MAML1 (21-36) peptide bound the complex with markedly diminished affinity in an in vitro pull down assay. Treatment of KOPT-K1 cell lines with 20 µM of compound results in the suppression of NOTCH1 target genes, HES4, DTX1, and HES1. 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 mutant NOTCH1 alleles. In HeLa cells, this peptide also inhibited the expression of ICN1 (IC50 = 6.56 µM) dose-dependently in a luciferase reporter-gene assay, as well as that of β-lactamase (IC50 < 2.5 µM) in a second reporter-gene assay. Furthermore, treatment with this peptide inhibits NOTCH-mediated proliferation in cultured cells at 15 µM, and in a mouse model of T-ALL cells at 30 mg/kg twice daily.
Catalogue Number491002
Brand Family Calbiochem®
SynonymsAcβA1a-ERLRRRI*LCR*HHST (*=S5)
References
ReferencesMoellering, R.E., et al. 2009. Nature 462, 182.
Product Information
FormOff-white solid
Hill FormulaC₉₄H₁₆₂N₃₆O₂₃S• 7CF₃CO₂H•13H₂O
Chemical formulaC₉₄H₁₆₂N₃₆O₂₃S• 7CF₃CO₂H•13H₂O
Quality LevelMQ100
Applications
Biological Information
Purity≥93% by HPLC
Physicochemical Information
Peptide SequenceAcetyl-βAla-ERLRRRI*LCR*HHST
* = Two S5 molecules (a non-natural alkenyl amino acid) stapled together with a double bond
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freze (20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Numero di catalogo GTIN
491002-1MG 04055977273427

Documentation

Notch Transcription Factor Inhibitor, SAHM1 - Calbiochem MSDS

Titolo

Scheda di sicurezza (MSDS) 

Notch Transcription Factor Inhibitor, SAHM1 - Calbiochem Certificati d'Analisi

TitoloNumero di lotto
491002

Riferimenti bibliografici

Panoramica delle referenze
Moellering, R.E., et al. 2009. Nature 462, 182.

Informazioni tecniche

Titolo
Chemical Structure for 491002 Notch Transcription Factor Inhibitor, SAHM1
Scheda tecnica

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.

Revision09-December-2010 RFH
SynonymsAcβA1a-ERLRRRI*LCR*HHST (*=S5)
DescriptionA 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 µM) competitively with MAML1, whereas the unmodified FITC-MAML1 (21-36) peptide bound the complex with markedly diminished affinity in an in vitro pull down assay. Treatment of KOPT-K1 cell lines with 20 µM of compound results in the suppression of NOTCH1 target genes, HES4, DTX1, and HES1. 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 mutant NOTCH1 alleles. In HeLa cells, this peptide also inhibited the expression of ICN1 (IC50 = 6.56 µM) dose-dependently in a luciferase reporter-gene assay, as well as that of β-lactamase (IC50 < 2.5 µM) in a second reporter-gene assay. Furthermore, treatment with this peptide inhibits NOTCH-mediated proliferation in cultured cells at 15 µM, and in a mouse model of T-ALL cells at 30 mg/kg twice daily.
FormOff-white solid
Chemical formulaC₉₄H₁₆₂N₃₆O₂₃S• 7CF₃CO₂H•13H₂O
Peptide SequenceAcetyl-βAla-ERLRRRI*LCR*HHST
* = Two S5 molecules (a non-natural alkenyl amino acid) stapled together with a double bond
Purity≥93% by HPLC
SolubilityDMSO (50 mg/ml)
Storage -20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freze (20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesMoellering, R.E., et al. 2009. Nature 462, 182.