530993 PKCε Translocation Inhibitor II, PKCe141 - Calbiochem

530993
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₂H₁₇N₃O₄S

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.30993.0001
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          Glass bottle 20 mg
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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
          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.