420350 ICMT Inhibitor - Calbiochem

420350
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      Replacement Information

      Prix & Disponibilité

      Référence DisponibilitéConditionnement Qté Prix Quantité
      420350-10MG
      Récupération des données relatives à la disponibilité...
      Disponibilité limitéeDisponibilité limitée
      En stock 
      Interrompu(e)
      Disponible en quantités limitées
      Disponibilité à confirmer
        Pour le restant : Nous vous tiendrons informé
          Pour le restant : Nous vous tiendrons informé
          Nous vous tiendrons informé
          Contacter le Service Clients
          Contact Customer Service

          Flacon en verre 10 mg
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          Description
          OverviewA cell-permeable indole acetamide that acts as a substrate-competitive and AdoMet-noncompetitive Icmt (isoprenylcysteine carboxyl methyltransferase) inhibitor (Ki = 0.02 µM; IC50 = 0.29 µM; Substrate = S-farnesyl-L-cysteine), exhibiting no activity against FTase, gernaylgeranyltransferase type I, CaaX protease Rce1, AdoMet-dependent DNA methyltransferase, SssI DNA methyltransferase, or PCMT1 protein methyltransferase. Cysmethynil (25 µM) induces G1 cell cycle-arrest and autophagy-mediated, but not apoptotic, cell death in prostate cancer PC3 cells with concomitant PI 3-K/Akt and mTOR signaling blockage, consistent with inhibition of Icmt-mediated activation of Ras and Rheb GTPases. Murine PC3 xenograft studies reveal limited in vivo efficacy.
          Catalogue Number420350
          Brand Family Calbiochem®
          Synonyms2-(5-(3-Methylphenyl)-1-octyl-1H-indol-3-yl)acetamide, 2-(1-Octyl-5-m-tolyl-1H-indol-3-yl) acetamide, Cysmethynil, Cysmethynil, Isoprenylcysteine Carboxyl Methyltransferase Inhibitor
          References
          ReferencesGo, M.L., et al. 2010. J. Med. Chem. 53, 6838; Wang, M., et al. 2008. J. Biol. Chem. 283, 18678; Baron, R.A., et al. 2007. Biochemistry 46, 554; Winter-Vann, A.M., et al. 2005. Proc. Natl. Acad. Sci. USA 102, 4336.
          Product Information
          FormPale yellow semi-solid
          Hill FormulaC₂₅H₃₂N₂0
          Chemical formulaC₂₅H₃₂N₂0
          Structure formula ImageStructure formula Image
          Quality LevelMQ100
          Applications
          Biological Information
          Purity≥95% 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 with Blue Ice or with Dry Ice
          Toxicity Regulatory Review
          Storage -20°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

          Documentation

          ICMT Inhibitor - Calbiochem FDS

          Titre

          Fiche de données de sécurité des matériaux (FDS) 

          Références bibliographiques

          Aperçu de la référence bibliographique
          Go, M.L., et al. 2010. J. Med. Chem. 53, 6838; Wang, M., et al. 2008. J. Biol. Chem. 283, 18678; Baron, R.A., et al. 2007. Biochemistry 46, 554; Winter-Vann, A.M., et al. 2005. Proc. Natl. Acad. Sci. USA 102, 4336.
          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.

          Revision04-June-2012 JSW
          Synonyms2-(5-(3-Methylphenyl)-1-octyl-1H-indol-3-yl)acetamide, 2-(1-Octyl-5-m-tolyl-1H-indol-3-yl) acetamide, Cysmethynil, Cysmethynil, Isoprenylcysteine Carboxyl Methyltransferase Inhibitor
          DescriptionA cell-permeable indole acetamide compound that inhibits Icmt (isoprenylcysteine carboxyl methyltransferase) activity in an acceptor substrate isoprenylated cysteine-competitive (Ki = 0.02 µM; IC50 = 0.29 and 2.1 µM, respectively, with or without inhibitor preincubation; Substrate = S-farnesyl-L-cysteine) and donor substrate AdoMet-noncompetitive manner, exhibiting no activity against FTase, gernaylgeranyltransferase type I, CaaX protease Rce1, AdoMet-dependent DNA methyltransferase, SssI DNA methyltransferase, or PCMT1 protein methyltransferase. Shown to inhibit the proliferation of non-cancer MEF cells (by 100% at 30 µM) and prevent anchorage-independent growth of colon cancer DKOB8 (by >90% at 20 µM) in a dose- and Icmt-dependent manner. Cysmethynil (25 µM) induces G1 cell cycle-arrest and autophagy-mediated, but not apoptotic, cell death in prostate cancer PC3 cells with concomitant PI 3-K/Akt and mTOR signaling blockage, consistent with inhibition of Icmt-mediated activation of Ras and Rheb GTPases. Murine PC3 xenograft studies reveal limited in vivo efficacy (tumor volume on day 28 = 9- and 22-fold of day 0, respectively, with or without 200 mg/kg/i.p. q.o.d.).
          FormPale yellow semi-solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₅H₃₂N₂0
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage -20°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 6 months at -20°C).
          Toxicity Regulatory Review
          ReferencesGo, M.L., et al. 2010. J. Med. Chem. 53, 6838; Wang, M., et al. 2008. J. Biol. Chem. 283, 18678; Baron, R.A., et al. 2007. Biochemistry 46, 554; Winter-Vann, A.M., et al. 2005. Proc. Natl. Acad. Sci. USA 102, 4336.