491002 | Notch Transcription Factor Inhibitor, SAHM1 - Calbiochem

491002
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₉₄H₁₆₂N₃₆O₂₃S• 7CF₃CO₂H•13H₂O

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      491002-1MG
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          Glass bottle 1 mg
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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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          491002

          References

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

          Brochure

          Title
          Ionic Liquids
          Ionic Liquids Product Range
          Let's start something new! Ionic Liquids Product Range for your innovations (EMD Version)

          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.