616451 TGF-β RI Kinase Inhibitor - CAS 396129-53-6 - Calbiochem

616451
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Overview

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Key Specifications Table

Empirical FormulaCAS #
C₁₇H₁₂N₄ 396129-53-6

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616451-5MG
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      Plastic ampoule 5 mg
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      Description
      OverviewA cell-permeable diheteroaryl-substituted pyrazole compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of TGF-β Receptor I kinase (IC50 = 51 nM). Displays ~15-fold greater selectivity over p38α MAP kinase (IC50 = 740 nM). Shown to inhibit TGF-β-dependent cellular growth (IC50 = 89 nM in NIH 3T3 mouse fibroblasts) and transcription activation (IC50 = 47 nM in mink lung cells).
      Catalogue Number616451
      Brand Family Calbiochem®
      SynonymsALK5 Inhibitor I, [3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole, TβR-I Inhibitor, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor, LY-364947, HTS-466284
      References
      ReferencesSawyer, J.S., et al. 2003. J. Med. Chem. 46, 3953.
      Singh, J., et al. 2003. Bioorg. Med. Chem. Lett. 13, 4355.
      Product Information
      CAS number396129-53-6
      ATP CompetitiveY
      FormBrown solid
      Hill FormulaC₁₇H₁₂N₄
      Chemical formulaC₁₇H₁₂N₄
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ200
      Applications
      Biological Information
      Primary TargetTGF-β receptor I kinase
      Primary Target IC<sub>50</sub>51 nM against TGF-β Receptor I kinase; 89 nM against TGF-β-dependent cellular growth in NIH 3T3 mouse fibroblasts; 47 nM against TGF-β-dependent transcription activation in mink lung cells
      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 Carcinogenic / Teratogenic
      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

      TGF-β RI Kinase Inhibitor - CAS 396129-53-6 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      TGF-β RI Kinase Inhibitor - CAS 396129-53-6 - Calbiochem Certificates of Analysis

      TitleLot Number
      616451

      References

      Reference overview
      Sawyer, J.S., et al. 2003. J. Med. Chem. 46, 3953.
      Singh, J., et al. 2003. Bioorg. Med. Chem. Lett. 13, 4355.

      Citations

      Title
    • Anush Oganesian, et al. (2006) The NH2-terminal propeptide of type I procollagen acts intracellularly to modulate cell function. Journal of Biological Chemistry 281, 38507-38518.
    • 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.

      Revision13-January-2010 RFH
      SynonymsALK5 Inhibitor I, [3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole, TβR-I Inhibitor, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor, LY-364947, HTS-466284
      DescriptionA cell-permeable, a potent, selective, reversible, and ATP-competitive inhibitor of TGF-b RI serine/threonine kinase (IC50 = 51 nM). Displays ~15-fold greater selectivity over p38α MAP kinase (IC50 = 740 nM). Reported to inhibit TGF-b-dependent cellular growth (IC50 = 89 nM in mouse NIH3T3 fibroblasts) and transcription activation (IC50 = 47 nM in mink lung cells).
      FormBrown solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number396129-53-6
      Chemical formulaC₁₇H₁₂N₄
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (5 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 Carcinogenic / Teratogenic
      ReferencesSawyer, J.S., et al. 2003. J. Med. Chem. 46, 3953.
      Singh, J., et al. 2003. Bioorg. Med. Chem. Lett. 13, 4355.
      Citation
    • Anush Oganesian, et al. (2006) The NH2-terminal propeptide of type I procollagen acts intracellularly to modulate cell function. Journal of Biological Chemistry 281, 38507-38518.