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526527 PIM Kinase Inhibitor VIII, R8-T198wt - Calbiochem

The PIM Kinase Inhibitor VIII, R8-T198wt controls the biological activity of PIM Kinase. This small molecule/inhibitor is primarily used for Cancer applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: NH₂-GGGRRRRRRRRGC~KKPGLRRRQT-CO₂H, cpm-P27Kip1189-198

526527
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₁₁H₂₁₁N₅₉O₂₆S₁

Pricing & Availability

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526527-5MG
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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
      Quality LevelMQ100
      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

      PIM Kinase Inhibitor VIII, R8-T198wt - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      PIM Kinase Inhibitor VIII, R8-T198wt - Calbiochem 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 Protect from light
      -20°C
      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.
      Toxicity Regulatory Review
      ReferencesMorishita, D., et al. 2011. J. Biol. Chem. 286, 2681.
      Morishita, D., et al. 2008. Cancer Res. 68, 5076.