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344505 FTase Substrate, Fluorogenic

344505
  
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Overview

Replacement Information
Description
Overview

This product has been discontinued.





This product has been discontinued.

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A pentapeptide substrate based on the carboxyl terminus of H-Ras with a dansyl group attached to the amino terminus. Serves as a substrate for continuous fluorescent monitoring of protein-farnesyl transferase (FTase) activity (kcat = 0.5 s-1; Km = 1.4 µM) in the presence of farnesyl diphosphate. S-farnesylation of the cysteine moiety results in approximately 13-fold enhancement in fluorescence intensity (monitored at λ = 505 nm) accompanied by a shift in the emission maximum from 565 nm to 515 nm. Reported to be highly selective for FTase and is not recognized by geranylgeranyltransferase I. Useful for screening of potential FTase inhibitors.
ε340 = 4,250 M-1 cm-1 in 20 mM Tris-HCI, 10 mM EDTA, pH 7.5.
Catalogue Number344505
Brand Family Calbiochem®
SynonymsDansyl-GCVLS, Dns-GCVLS
References
ReferencesBohm, M., et al. 2001. J. Med. Chem. 44, 3117.
Schlitzer, M., et al. 1999. Bioorg. Med. Chem. 7, 2037.
Hightower, K.E., et al. 1998. Biochemistry 37, 15555.
Pickett, W.C., et al. 1995. Anal. Biochem. 225, 60.
Pompliano, D.L., et al. 1992. J. Am. Chem. Soc. 114, 7945.
Pompliano, D.L., et al. 1992. Biochemistry 31, 3800.
Product Information
CAS number143744-88-1
FormLyophilized
FormulationSupplied as a trifluoroacetate salt.
Hill FormulaC₃₁H₄₆N₆O₉S₂
Chemical formulaC₃₁H₄₆N₆O₉S₂
Hygroscopic Hygroscopic
Structure formula ImageStructure formula Image
Applications
Biological Information
Purity≥95% by HPLC
Physicochemical Information
Emission max.
Excitation max.
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Blue Ice Only
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
344505 0

Documentation

FTase Substrate, Fluorogenic Certificates of Analysis

TitleLot Number
344505

References

Reference overview
Bohm, M., et al. 2001. J. Med. Chem. 44, 3117.
Schlitzer, M., et al. 1999. Bioorg. Med. Chem. 7, 2037.
Hightower, K.E., et al. 1998. Biochemistry 37, 15555.
Pickett, W.C., et al. 1995. Anal. Biochem. 225, 60.
Pompliano, D.L., et al. 1992. J. Am. Chem. Soc. 114, 7945.
Pompliano, D.L., et al. 1992. Biochemistry 31, 3800.
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.

Revision27-June-2008 RFH
SynonymsDansyl-GCVLS, Dns-GCVLS
DescriptionA pentapeptide substrate based on the carboxyl terminus of H-Ras with a dansyl group attached to the amino terminus. Useful for continuous fluorescent monitoring of protein-farnesyl transferase (FTase) activity in the presence of farnesyl diphosphate (kcat = 0.5 s-1; Km = 1.4 µM). Following farnesylation of the cysteine thiol the dansyl residue is placed in a lipophilic environment, resulting in an approximately 13-fold enhancement of fluorescence intensity at a wavelength of 505 nm and a shift in the emission maximum wavelength from 565 nm to 515 nm. Reported to be highly specific to FTase and is not recognized by geranylgeranyl transferase type I (GGTase I). Useful for screening potential FTase inhibitors. Excitation maximum: ~340 nm; emission maximum: ~505 nm; ε340 = 4,250 M-1cm-1 in 20 mM Tris-HCl, pH 7.5, 10 mM EDTA.
FormLyophilized
FormulationSupplied as a trifluoroacetate salt.
Intert gas (Yes/No) Packaged under inert gas
Recommended reaction conditions10 µM farnesyl diphosphate, 0.5 nM FTase, in 50 mM Tris-HCl, pH 7.5, 5 mM DTT, 5 mM MgCl2, 10 µM ZnCl2, and 0.2% octyl-β-D-glucopyranoside, at 30°C.
CAS number143744-88-1
Chemical formulaC₃₁H₄₆N₆O₉S₂
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (10 mg/ml)
Storage Protect from light
-20°C
Hygroscopic
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Toxicity Standard Handling
ReferencesBohm, M., et al. 2001. J. Med. Chem. 44, 3117.
Schlitzer, M., et al. 1999. Bioorg. Med. Chem. 7, 2037.
Hightower, K.E., et al. 1998. Biochemistry 37, 15555.
Pickett, W.C., et al. 1995. Anal. Biochem. 225, 60.
Pompliano, D.L., et al. 1992. J. Am. Chem. Soc. 114, 7945.
Pompliano, D.L., et al. 1992. Biochemistry 31, 3800.