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616461 TGF-β RI Kinase Inhibitor VI, SB431542 - CAS 301836-41-9 - Calbiochem

TGF-β RI Kinase Inhibitor VI, SB431542, CAS 301836-41-9, is a cell-permeable inhibitor of SMAD2 phosphorylation. Inhibits the activity of ALK4 and ALK5 (IC₅₀ = 140 nM and 94 nM, respectively).

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Synonymes: 4-[4-(3,4-Methylenedioxyphenyl)-5-(2-pyridyl)-1H-imidazol-2-yl]benzamide, Dihydrate, 4-[4-(1,3-Benzodioxol-5-yl)-5-(2-pyridyl)-1H-imidazol-2-yl]benzamide, Dihydrate, SB-431542

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616461
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Tableau de caractéristiques principal

CAS #Empirical Formula
301836-41-9C₂₂H₁₆N₄O₃. 2H₂O

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616461-5MG
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      Description
      OverviewA cell-permeable triarylimidazole compound that is shown to effectively inhibit cellular Smad2 phosphorylation (>90% inhibition by 10 µM inhibitor) upon vector-mediated expression of constitutively active ALK4, ALK5, or ALK7 in NIH 3T3 cells, while exhibiting little effect against Smad1 phosphorylation by other members of type I receptors for TGF-β in NIH 3T3 cultures expressing active ALK1, 2, 3, or 6. When tested directly in cell-free kinase assays, SB431542 is demonstrated to potently inhibit the activity of ALK4 and ALK5 (IC50 = 140 nM and 94 nM, respectively) with no or much reduced potency toward a panel of 24 other kinases (IC50 ≥10 µM in the presence of 10 µM ATP), including ALK2 and ALK6. Reported to improve the efficiency of 4-TF-induced human iPSCs generation from fibroblast cultures by >200-fold when used together with PD0325901 (Cat. No. 444966) and Thiazovivin (Cat. No. 420220). Also available as a 100 mM solution in DMSO (Cat. No. 616464).
      Catalogue Number616461
      Brand Family Calbiochem®
      Synonyms4-[4-(3,4-Methylenedioxyphenyl)-5-(2-pyridyl)-1H-imidazol-2-yl]benzamide, Dihydrate, 4-[4-(1,3-Benzodioxol-5-yl)-5-(2-pyridyl)-1H-imidazol-2-yl]benzamide, Dihydrate, SB-431542
      References
      ReferencesIkushima, H., et al. 2009. Cell Stem Cell 5, 504.
      Lin, T., et al. 2009. Nat. Methods 6, 805.
      Maherali, N. and Hochedlinger, K., 2009. Curr. Biol. 19, 1718.
      Callahan, J.F., et al. 2002. J. Med. Chem. 45, 999.
      Inman, G.J., et al. 2002. Mol. Pharmacol. 62, 65.
      Laping, N.J., et al. 2002. Mol. Pharmacol. 62, 58.
      Product Information
      CAS number301836-41-9
      FormOff-white solid
      Hill FormulaC₂₂H₁₆N₄O₃. 2H₂O
      Chemical formulaC₂₂H₁₆N₄O₃. 2H₂O
      Structure formula ImageStructure formula Image
      Quality LevelMQ300
      Applications
      Biological Information
      Purity≥97% 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 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
      Global Trade Item Number
      Référence GTIN
      616461-5MG 04055977185928

      Documentation

      TGF-β RI Kinase Inhibitor VI, SB431542 - CAS 301836-41-9 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      616461

      Références bibliographiques

      Aperçu de la référence bibliographique
      Ikushima, H., et al. 2009. Cell Stem Cell 5, 504.
      Lin, T., et al. 2009. Nat. Methods 6, 805.
      Maherali, N. and Hochedlinger, K., 2009. Curr. Biol. 19, 1718.
      Callahan, J.F., et al. 2002. J. Med. Chem. 45, 999.
      Inman, G.J., et al. 2002. Mol. Pharmacol. 62, 65.
      Laping, N.J., et al. 2002. Mol. Pharmacol. 62, 58.
      Fiche technique

      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.

      Revision30-August-2010 RFH
      Synonyms4-[4-(3,4-Methylenedioxyphenyl)-5-(2-pyridyl)-1H-imidazol-2-yl]benzamide, Dihydrate, 4-[4-(1,3-Benzodioxol-5-yl)-5-(2-pyridyl)-1H-imidazol-2-yl]benzamide, Dihydrate, SB-431542
      DescriptionA cell-permeable triarylimidazole compound that is shown to effectively inhibit cellular Smad2 phosphorylation (>90% inhibition by 10 µM inhibitor) upon vector-mediated expression of constitutively active ALK4, ALK5, or ALK7 in NIH 3T3 cells, while exhibiting little effect against Smad1 phosphorylation by other members of type I receptors for TGF-β in NIH 3T3 cultures expressing active ALK1, 2, 3, or 6. When tested directly in cell-free kinase assays, SB431542 is demonstrated to potently inhibit the activity of ALK4 and ALK5 (IC50 = 140 nM and 94 nM, respectively) with no or much reduced potency toward a panel of 24 other kinases (IC50 ≥10 µM in the presence of 10 µM ATP), including ALK2 and ALK6. Reported to improve the efficiency of 4-TF-induced human iPSCs generation from fibroblast cultures by >200-fold when used together with PD0325901 (Cat. No. 444966) and Thiazovivin (Cat. No. 420220).
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number301836-41-9
      Chemical formulaC₂₂H₁₆N₄O₃. 2H₂O
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml) or Ethanol (10 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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
      ReferencesIkushima, H., et al. 2009. Cell Stem Cell 5, 504.
      Lin, T., et al. 2009. Nat. Methods 6, 805.
      Maherali, N. and Hochedlinger, K., 2009. Curr. Biol. 19, 1718.
      Callahan, J.F., et al. 2002. J. Med. Chem. 45, 999.
      Inman, G.J., et al. 2002. Mol. Pharmacol. 62, 65.
      Laping, N.J., et al. 2002. Mol. Pharmacol. 62, 58.