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

616451
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₇H₁₂N₄ 396129-53-6

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      616451-5MG
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          Glass bottle 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 Image
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.

          Brochure

          Title
          TGF-b Signaling: Dual Role in Tumor Suppression and Oncogenesis

          Technical Info

          Title
          TGF-β Signaling: Dual Role in Tumor Suppression and Oncogenesis

          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 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.