533298 TNIK Inhibitor, KY-05009 - Calbiochem

533298
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₈H₁₆N₄O₂S

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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable, non-toxic, 2-phenylaminothiazole derivative that acts as a highly potent, ATP competitive inhibitor of Traf2- and Nck-interacting kinase (TNIK; Ki = 100 nM, IC50 = 9 nM). Also shown to inhibit the activity of MLK1 (IC50 = 18 nM). Blocks multiple effects of TGF-β1 in A549 human lung adenocarcinoma cells, including nuclear translocation of β-catenin, TNIK binding to TCF4, phosphorylation of TCF4, and phosphorylation and nuclear translocation of Smad2/3. Significantly reduces TGF-β1 induced epithelial-to-mesenchymal transition (EMT). Reduces TGF-β1-induced migration and invasion in A549 cells and inhibits gelatinase activity of MMP2 and 9. Shown to diminish TGF-β1-induced phosphorylation of focal adhesion kinase (at Tyr925), Src (at Tyr416), and paxillin (at Tyr118) and of ERK1/2 (at Thr202/Tyr204), JNK1 (Thr183/Tyr221), and JNK2 (at Thr185/Tyr223).

      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 Number533298
      Brand Family Calbiochem®
      SynonymsTraf2- and Nck-interacting Kinase Inhibitor, KY-05009, KY05009, 5-(4-Methylbenzamido)-2-(phenylamino)thiazole-4-carboxamide
      References
      ReferencesKim, J., et al. 2014. PLOS One. 9, e110180.
      Product Information
      FormYellow solid
      Hill FormulaC₁₈H₁₆N₄O₂S
      Chemical formulaC₁₈H₁₆N₄O₂S
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetTNIK
      Primary Target K<sub>i</sub>100 nM, IC₅₀
      Purity≥98% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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

      TNIK Inhibitor, KY-05009 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Kim, J., et al. 2014. PLOS One. 9, e110180.
      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
      SynonymsTraf2- and Nck-interacting Kinase Inhibitor, KY-05009, KY05009, 5-(4-Methylbenzamido)-2-(phenylamino)thiazole-4-carboxamide
      DescriptionA cell-permeable, non-toxic, 2-phenylaminothiazole derivative that acts as a highly potent, ATP competitive inhibitor of Traf2- and Nck-interacting kinase (TNIK; Ki = 100 nM, IC50 = 9 nM). Also shown to inhibit the activity of MLK1 (IC50 = 18 nM). Blocks multiple effects of TGF-β1 in A549 human lung adenocarcinoma cells, including nuclear translocation of β-catenin, TNIK binding to TCF4, phosphorylation of TCF4, and phosphorylation and nuclear translocation of Smad2/3. Significantly reduces TGF-β1 induced epithelial-to-mesenchymal transition (EMT). Reduces TGF-β1-induced migration and invasion in A549 cells and inhibits gelatinase activity of MMP2 and 9. Shown to diminish TGF-β1-induced phosphorylation of focal adhesion kinase (at Tyr925), Src (at Tyr416), and paxillin (at Tyr118) and of ERK1/2 (at Thr202/Tyr204), JNK1 (Thr183/Tyr221), and JNK2 (at Thr185/Tyr223).
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₈H₁₆N₄O₂S
      Purity≥98% 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
      ReferencesKim, J., et al. 2014. PLOS One. 9, e110180.