345885 | GGTI-2147 - CAS 191102-87-1 - Calbiochem

345885
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₈H₃₀N₄O₃ 191102-87-1

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      345885-250UG
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          Plastic ampoule 250 μg
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          Description
          OverviewA cell-permeable non-thiol peptidomimetic that acts as a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I). Blocks the geranyl-geranylation of Rap1A with an IC50 value that is over 60-fold lower than that required to disrupt the farnesylation of H-Ras (IC50 = 500 nM for Rap1A versus IC50 > 30 µM for H-Ras).
          Catalogue Number345885
          Brand Family Calbiochem®
          Synonyms4-[[N-(Imidazol-4-yl)methyleneamino]-2-(1-naphthyl)benzoyl]leucine methyl ester
          References
          ReferencesBernot, D., et al. 2003. J. Cardiovasc. Pharmacol. 41, 316.
          Vasudevan, A., et al. 1999. J. Med. Chem. 42, 1333.
          Product Information
          CAS number191102-87-1
          ATP CompetitiveN
          FormOff-white solid
          Hill FormulaC₂₈H₃₀N₄O₃
          Chemical formulaC₂₈H₃₀N₄O₃
          Hygroscopic Hygroscopic
          ReversibleN
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetGGTase-I
          Primary Target IC<sub>50</sub>500 nM in blocking the geranyl-geranylation of Rap1A
          Purity≥95% 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 Standard Handling
          Storage -20°C
          Hygroscopic Hygroscopic
          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
          345885

          References

          Reference overview
          Bernot, D., et al. 2003. J. Cardiovasc. Pharmacol. 41, 316.
          Vasudevan, A., et al. 1999. J. Med. Chem. 42, 1333.
          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.

          Revision31-March-2011 RFH
          Synonyms4-[[N-(Imidazol-4-yl)methyleneamino]-2-(1-naphthyl)benzoyl]leucine methyl ester
          DescriptionMethyl ester derivative of GGTI-2133 (Cat. No. 345884). A potent and selective non-thiol inhibitor of geranylgeranyltransferase I (GGTase I) over farnesyltransferase (FTase) in whole cells. Blocks the geranylgeranylation of Rap1A with an IC50 value greater than 60-fold lower than that required to disrupt the farnesylation of H-Ras (IC50 = 500 nM for Rap1A versus IC50 <30 µM for H-Ras).
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number191102-87-1
          Chemical formulaC₂₈H₃₀N₄O₃
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (200 mg/ml)
          Storage -20°C
          Hygroscopic
          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 Standard Handling
          ReferencesBernot, D., et al. 2003. J. Cardiovasc. Pharmacol. 41, 316.
          Vasudevan, A., et al. 1999. J. Med. Chem. 42, 1333.

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          Categories

          Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Other Inhibitors of Biological Interest > Farnesyltransferase (FTase), Geranylgeranyltransferase (GGTase), & Methyltransferase Inhibitors