533760 PDK1 Inhibitor VII, RS1 - Calbiochem

533760
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₅H₉ClN₂O₂S₃

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      Glass bottle 25 mg
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      Description
      OverviewA cell-permeable benzothiazolyl-benzothienylsulfonamide compound that selectively binds to the PDK1-interacting fragment pocket of PDK1 (Kd = 1.5 µM) and disrupts its signaling in cells. Displays high selectivity over 44 other kinases (<35% inhibition at 10 µM). Acts as an allosteric, substrate-selective inhibitor of PDK1 when used as a single agent, however, it suppresses the activation of downstream kinases when combined with an ATP-competitive inhibitor (GSK2334470). As a single agent, it partially blocks the phosphorylation of S6 at Ser235/236 by S6K1 (IC50 ~ 30 µM in serum starved HEK293 cells) and has only a trivial effect (10% inhibition at 30 µM) on the phosphorylation of Thr308 of AKT.

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number533760
      Brand Family Calbiochem®
      SynonymsN-(6-Chlorobenzo[d]thiazol-2-yl)benzo[b]thiophene-3-sulfonamide
      References
      ReferencesRettenmaier, T.J., et al. 2014. Proc. Natl. Acad. Sci. USA. 52, 18590.
      Product Information
      FormWhite solid
      Hill FormulaC₁₅H₉ClN₂O₂S₃
      Chemical formulaC₁₅H₉ClN₂O₂S₃
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPDK1
      Primary Target K<sub>i</sub>1.5 µ
      Purity≥97% 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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      PDK1 Inhibitor VII, RS1 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Rettenmaier, T.J., et al. 2014. Proc. Natl. Acad. Sci. USA. 52, 18590.
      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.

      Revision20-November-2015 JSW
      SynonymsN-(6-Chlorobenzo[d]thiazol-2-yl)benzo[b]thiophene-3-sulfonamide
      DescriptionA cell-permeable benzothiazolyl-benzothienylsulfonamide compound that selectively binds to the PDK1-interacting fragment pocket of PDK1 (Kd = 1.5 µM) and disrupts its signaling in cells. Displays high selectivity over 44 other kinases (<35% inhibition at 10 µM). Acts as an allosteric, substrate-selective inhibitor of PDK1 when used as a single agent, however, it suppresses the activation of downstream kinases when combined with an ATP-competitive inhibitor (GSK2334470). As a single agent, it partially blocks the phosphorylation of S6 at Ser235/236 by S6K1 (IC50 ~ 30 µM in serum starved HEK293 cells) and has only a trivial effect (10% inhibition at 30 µM) on the phosphorylation of Thr308 of AKT.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₅H₉ClN₂O₂S₃
      Purity≥97% by HPLC
      SolubilityDMSO (50 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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesRettenmaier, T.J., et al. 2014. Proc. Natl. Acad. Sci. USA. 52, 18590.