Target: Protein farnesyltransferase (FTase) enzyme activity and inhibitory kinetics.
Brand: ModifiSite
Development Stage: Research-Grade Protein-Based Assay Development
Short Description
Quantifies farnesyltransferase activity using a fluorescence method.
Brand
ModifiSite
Development Stage
Research-Grade Protein-Based Assay Development
Description
The ModifiSite™ Farnesyltransferase Inhibitor Screening Kit provides a safe, non-radioactive fluorimetric platform for high-throughput screening of FTase inhibitors. This homogeneous "mix-incubate-measure" system enables rapid evaluation of drug modulators that target protein farnesylation, a critical process in oncology research. With a robust Z' factor and automated compatibility, it streamlines the identification of potent therapeutic candidates in drug discovery.
Features
High Sensitivity & Precision: Employs a robust fluorescence-based format to detect subtle enzymatic shifts, ensuring reliable IC50 determination for potential inhibitors. Streamlined Homogeneous Protocol: Optimized for "mix-and-read" workflows, eliminating tedious wash steps and reducing experimental variability across diverse throughput scales. Validated Specificity: Precision-engineered components minimize interference from complex chemical libraries, providing high-fidelity results during primary and secondary screening phases.
Process Relevance
Accelerating lead identification by quantifying FTase inhibition to streamline the development of targeted anti-cancer small molecule therapies.
Application Stage
Lead discovery, preclinical drug candidate validation, and enzymatic activity profiling during early-stage pharmacological development.
Applications
Enabling high-throughput screening of chemical libraries, characterization of novel inhibitors, and kinetic analysis of protein farnesylation across various biological matrices.
Qualified With
Internal performance validation using reference standards under defined assay conditions.
Target
Protein farnesyltransferase (FTase) enzyme activity and inhibitory kinetics.
Detection Method
Fluorescence Detection (Ex 340 nm / Em 550 nm)
Sample Type
Chemical compounds
Research Areas
Oncology therapeutics, signal transduction, molecular pharmacology, cell cycle regulation, etc.
Size
400 tests
Data Output Type
Quantitative enzyme inhibition percentage and kinetic activity measurement via fluorescence intensity.
Assay Time
60 min
Species
All Species
Storage
Store at −20 °C; upon receipt to maintain reagent stability. Follow recommended handling procedures to ensure consistent assay performance.
Storage Comment
Avoid repeated freeze-thaw cycles. During use, minimize the time components are exposed to room temperature and return them promptly to −20 ℃ storage after handling. Do not store at elevated temperatures for extended periods.
Expiry Date
6 months under recommended storage conditions to ensure optimal performance.
Note
For bulk pricing or custom reagent inquiries, please contact us by email or phone. Products are shipped on ice via FedEx.
Restrictions
For Research Use Only (RUO). Not intended for diagnostic or therapeutic use.
Shipping
Shipped on ice under temperature-controlled conditions.
Background
Farnesyltransferase (FTase) facilitates post-translational lipid modifications, crucial for anchoring proteins like Ras to cell membranes. Dysregulation of this prenylation process drives oncogenic transformation, making FTase a high-priority target for cancer therapeutics.
Pathways
FTase operates within the protein prenylation pathway, adding a 15-carbon farnesyl group to the C-terminal CaaX motif. This modification is essential for the activation of Ras-MAPK and PI3K/Akt signaling cascades governing cell proliferation.