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530993 PKCε Translocation Inhibitor II, PKCe141 - Calbiochem

530993
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₂H₁₇N₃O₄S

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      Description
      OverviewA cell-permeable, non-toxic thienoquinoline compound that dose-dependently inhibits PKCε-RACK2 interaction (IC50 = 5.9 µM). Shown to occupy PKCε to RACK2 binding site in a reversible manner and block cellular phosphorylation of MARCKS and Elk-1 (IC50 = 11.2 µM in HeLa cells). Prevents TPA-induced PKCε translocation to the plasma membrane, and reduces PKCε-induced cell migration, invasion and suppresses angiogenesis. Displays desireable selectivity in a 109-kinase panel, and at higher concentrations affects PKCα, βI and ζ (~80% at 50 µM) and ERK1, RSK2, NUAK1, PIM3 & BTK (> 50% at 25 µM) activities.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number530993
      Brand Family Calbiochem®
      SynonymsN-(3-Acetylphenyl)-9-amino-2,3-dihydro-[1,4]dioxino[2,3-g]thieno[2,3-b]quinoline-8-carboxamide, PKCε-RACK2 Interaction Inhibitor II, Protein Kinase Cε Translocation Inhibitor II
      References
      ReferencesRechfeld, F., et al. 2014. J. Med. Chem. 57, 3235.
      Product Information
      FormBrown powder
      Hill FormulaC₂₂H₁₇N₃O₄S
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPKCε
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      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

      PKCε Translocation Inhibitor II, PKCe141 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Rechfeld, F., et al. 2014. J. Med. Chem. 57, 3235.
      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-July-2014 JSW
      SynonymsN-(3-Acetylphenyl)-9-amino-2,3-dihydro-[1,4]dioxino[2,3-g]thieno[2,3-b]quinoline-8-carboxamide, PKCε-RACK2 Interaction Inhibitor II, Protein Kinase Cε Translocation Inhibitor II
      DescriptionA cell-permeable non-peptidic thienoquinoline modeled after pharmacophore feature derived from the non-permeant EAVSLKPT (Cat. no. 539522) and found to selectively inhibit PKCε-RACK2, but not PKCβII-RACK1, interaction (IC50 = 5.9 µM; [RACK2-MBP] = 500 ng/50 µL or 62.5 nM) and suppress PKCε, but not PKCδ membrane translocation induced by PMA/TPA (Cat. nos. 500582 & 524400) in serum-starved PC-3 cultures (20 or 50 µM PKCe141 added 30 min prior to 50 or 100 nM TPA stimulation for 5 min). Likewise, PKCe141 is demonstrated to inhibit Elk-1 activation domain (aa 307-427) phosphorylation-dependent HeLa luciferase reporter (HLR) transcription (IC50 = 11.2 µM) as well as MARCKS S152/S156 phosphorylation in serum-starved HeLa cells (50 µM) upon TPA stimulation without cytotoxicity (up to 50 µM for 72 h by SRB assay). PKCe141 does not inhibit cellular PKCε phosphorylation and exhibits little potency against PKC kinase activity (% inhibition at 50 µM/150 ng PKC = 23/η, 18/βI, 17/α, 12/ε, 11/γ, 9/ι, 6/δ & θ, 1/βII, 0/ζ; [ATP] = 40 µM; substrate [PKCα 19-31] = 50 µM), while more significant inhibition is seen against 5 other kinases among a panel of 109, the observed potency (% inhibition at 50 µM = 73/RSK2, 58/BTK, 54/PIM3, 51/NUAK1, 45/ERK1) is less than that toward PKCε-RACK2 interaction. Also reported to suppress active PKCε-dependent HeLa migration (25 µM for 24 h) and inhibit VEGF-induced angiogenesis in chicken eggs (10 ng VEGF & 10 ng PKCe141).
      FormBrown powder
      Intert gas (Yes/No) Packaged under inert gas
      Purity≥95% by HPLC
      SolubilityDMSO (10 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
      ReferencesRechfeld, F., et al. 2014. J. Med. Chem. 57, 3235.