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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.

Ficha de datos de seguridad (MSDS o SDS), certificado de análisis y de calidad (CoA y CoQ), expedientes, folletos y otros documentos disponibles.

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

491002
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Descripción

Replacement Information

Tabla espec. clave

Empirical Formula
C₉₄H₁₆₂N₃₆O₂₃S• 7CF₃CO₂H•13H₂O

Products

Número de referenciaEmbalaje Cant./Env.
491002-1MG Frasco de vidrio 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
Número de referencia GTIN
491002-1MG 04055977273427

Documentation

Notch Transcription Factor Inhibitor, SAHM1 - Calbiochem Ficha datos de seguridad (MSDS)

Título

Ficha técnica de seguridad del material (MSDS) 

Notch Transcription Factor Inhibitor, SAHM1 - Calbiochem Certificados de análisis

CargoNúmero de lote
491002

Referencias bibliográficas

Visión general referencias
Moellering, R.E., et al. 2009. Nature 462, 182.

Licencias necesarias e Información técnica

Cargo
Chemical Structure for 491002 Notch Transcription Factor Inhibitor, SAHM1
Ficha técnica

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.