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491002 Notch Transcription Factor Inhibitor, SAHM1 - Calbiochem

491002
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₉₄H₁₆₂N₃₆O₂₃S• 7CF₃CO₂H•13H₂O

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491002-1MG
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      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

      Documentation

      Notch Transcription Factor Inhibitor, SAHM1 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Notch Transcription Factor Inhibitor, SAHM1 - Calbiochem Certificates of Analysis

      TitleLot Number
      491002

      References

      Reference overview
      Moellering, R.E., et al. 2009. Nature 462, 182.

      Technical Info

      Title
      Chemical Structure for 491002 Notch Transcription Factor Inhibitor, SAHM1
      Data Sheet

      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.