526527 | PIM Kinase Inhibitor VIII, R8-T198wt - Calbiochem

526527
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₁₁H₂₁₁N₅₉O₂₆S₁

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      526527-5MG
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          Glass bottle 5 mg
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          Description
          OverviewThe human p27Kip1 C-terminus PIM-1 phosphorylation site- (Thr198) containing sequence is synthesized with an N-terminal Arg octamer/R8-containing sequence to facilitate its use as a cell-permeable, substrate-competitive PIM-1 inhibitor. Reported to completely prevents human prostate carcinoma DU145-derived tumor expansion for up to 17 days (0.5 µmol/animal on days 0 & 5; intratumoral injection) in mice in vivo when combined with a single Taxol (Cat. No. 580555) dosage on day zero (60 mg/kg; i.p.). Studies using FITC-conjugated R8-T198wt demonstrate that R8-T198wt-induced cell cycle arrest and apoptosis in PIM-1-expressing DU145 cells are direct consequences of inhibition of PIM-1-mediated p27Kip1 Thr198 and Bad Ser112 phosphorylation, respectively.
          Catalogue Number526527
          Brand Family Calbiochem®
          SynonymsNH₂-GGGRRRRRRRRGC~KKPGLRRRQT-CO₂H, cpm-P27Kip1189-198
          References
          ReferencesMorishita, D., et al. 2011. J. Biol. Chem. 286, 2681.
          Morishita, D., et al. 2008. Cancer Res. 68, 5076.
          Product Information
          FormWhite solid
          FormulationSupplied as a trifluoroacetate salt
          Hill FormulaC₁₁₁H₂₁₁N₅₉O₂₆S₁
          Chemical formulaC₁₁₁H₂₁₁N₅₉O₂₆S₁
          Hygroscopic Hygroscopic
          Applications
          Biological Information
          Purity≥95% by HPLC
          Physicochemical Information
          Peptide SequenceH-Gly-Gly-Gly-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Gly-Cys-Lys-Lys-Pro-Gly-Leu-Arg-Arg-Arg-Gln-Thr-OH
          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 Regulatory Review
          Storage -20°C
          Protect from Light Protect from light
          Hygroscopic Hygroscopic
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month 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
          526527

          References

          Reference overview
          Morishita, D., et al. 2011. J. Biol. Chem. 286, 2681.
          Morishita, D., et al. 2008. Cancer Res. 68, 5076.
          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.

          Revision04-June-2012 JSW
          SynonymsNH₂-GGGRRRRRRRRGC~KKPGLRRRQT-CO₂H, cpm-P27Kip1189-198
          DescriptionThe human p27Kip1 C-terminus PIM-1 phosphorylation site- (Thr198) containing sequence is synthesized with an N-terminal Arg octamer/R8-containing sequence to facilitate its use as a cell-permeable, substrate-competitive PIM-1 inhibitor. Reported to retard human prostate carcinoma DU145-derived tumor growth in mice (100% vs 257% tumor growth on day 14 with or without 0.5 µmol/animal dosing on days 0 & 3; intratumoral injection) in vivo and completely prevents tumor expansion for up to 17 days (0.5 µmol/animal on days 0 & 5; intratumoral injection) when combined with a single Taxol (Cat. No. 580555) dosage (60 mg/kg; i.p.) on day zero. Studies using FITC-conjugated R8-T198wt confirms cellular delivery and PIM-1 interaction (KD = 323 nM), demonstrating also that R8-T198wt-induced cell cycle arrest and apoptosis in PIM-1-expressing DU145 cells are direct consequences of inhibition of PIM-1-mediated p27Kip1 Thr198 and Bad Ser112 phosphorylation, respectively.
          FormWhite solid
          FormulationSupplied as a trifluoroacetate salt
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₁₁H₂₁₁N₅₉O₂₆S₁
          Peptide SequenceH-Gly-Gly-Gly-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Gly-Cys-Lys-Lys-Pro-Gly-Leu-Arg-Arg-Arg-Gln-Thr-OH
          Purity≥95% by HPLC
          SolubilityDMSO (50 mg/ml; clear, colorless solution) or H₂O (50 mg/ml; clear, colorless solution). Use only fresh DMSO.
          Storage -20°C
          Hygroscopic
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
          Toxicity Regulatory Review
          ReferencesMorishita, D., et al. 2011. J. Biol. Chem. 286, 2681.
          Morishita, D., et al. 2008. Cancer Res. 68, 5076.