420350 | ICMT Inhibitor - Calbiochem

420350
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      Overview

      Replacement Information

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      420350-10MG
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          Glass bottle 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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          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.
          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.

          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.