264157 | Caspase Modulator I, 1541 - Calbiochem

264157
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₄H₁₇N₃O₄

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      264157-10MG
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          10 mg
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          Description
          OverviewA cell-permeable phenylimidazopyridinyl-methoxy coumarin compound that inhibits caspase-3 and caspase-6 activities (IC50 = 35 and 38 µM, respectively) by targeting both the large and small subunit active sites. Kinetic studies with 1541 and its 8-Hydroxy analog (Cat. No. 529663) indicate that at suboptimal inhibitor : proenzyme molar ratio (100:1 or less), the compound does not effectively occupies both active sites of and stabilizes the proenzyme in an “on-state” conformation that facilitates the subsequent autoproteolysis or autoactivation process via the unoccupied active site of procaspase-3 and -6 (EC50 = 2.4 and 2.8 µM, respectively). Shown to effectively induce apoptosis (up to 50 µM) in various cancer cell lines (IC50 ranges from 3.8 to 8.7 µM) in a caspase-3-dependent, but p53-, caspase-8-, and Bak-independent manner. Exhibits little inhibitory effect against active caspase-7 (30 nM) even at concentrations as high as 50 µM, nor does it activate procaspase-1 or -7 even after prolonged incubations upto 4 and 24 h, respectively.
          Catalogue Number264157
          Brand Family Calbiochem®
          SynonymsCaspase-6 Inhibitor XI, Procaspase-3 Activator II, Procaspase-6 Activator I, 8-Methoxy-2-oxo-2H-chromene-3-carboxylic acid-(3-imidazo[1,2-a]pyridin-2-yl-phenyl)-amide, Caspase-3 Inhibitor XV
          References
          ReferencesWolan, D.W., et al. 2009. Science 326, 853.
          Product Information
          FormYellow solid
          Hill FormulaC₂₄H₁₇N₃O₄
          Chemical formulaC₂₄H₁₇N₃O₄
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥95% by HPLC
          Physicochemical Information
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Standard Handling
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          264157

          References

          Reference overview
          Wolan, D.W., et al. 2009. Science 326, 853.
          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.

          Revision31-March-2011 RFH
          SynonymsCaspase-6 Inhibitor XI, Procaspase-3 Activator II, Procaspase-6 Activator I, 8-Methoxy-2-oxo-2H-chromene-3-carboxylic acid-(3-imidazo[1,2-a]pyridin-2-yl-phenyl)-amide, Caspase-3 Inhibitor XV
          DescriptionA cell-permeable phenylimidazopyridinyl-methoxy coumarin compound that inhibits caspase-3 and caspase-6 activities (IC50 = 35 and 38 µM, respectively) by targeting both the large and small subunit active sites. Kinetic studies with 1541 and its 8-Hydroxy analog (Cat. No. 529663) indicate that at suboptimal inhibitor : proenzyme molar ratio (100:1 or less), the compound does not effectively occupies both active sites of and stabilizes the proenzyme in an “on-state” conformation that facilitates the subsequent autoproteolysis or autoactivation process via the unoccupied active site of procaspase-3 and -6 (EC50 = 2.4 and 2.8 µM, respectively). Shown to effectively induce apoptosis (up to 50 µM) in various cancer cell lines (IC50 ranges from 3.8 to 8.7 µM) in a caspase-3-dependent, but p53-, caspase-8-, and Bak-independent manner. Exhibits little inhibitory effect against active caspase-7 (30 nM) even at concentrations as high as 50 µM, nor does it activate procaspase-1 or -7 even after prolonged incubations upto 4 and 24 h, respectively.
          FormYellow solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₄H₁₇N₃O₄
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (5 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesWolan, D.W., et al. 2009. Science 326, 853.