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About CDC42BPG
CDC42BPG (CDC42 Binding Protein Kinase Gamma), also known as MRCK-gamma, belongs to the DMPK (Dystrophia Myotonica Protein Kinase) family within the AGC kinase superfamily. Like its paralogs MRCK-alpha (CDC42BPA) and MRCK-beta (CDC42BPB), CDC42BPG is activated downstream of the Rho-family GTPase CDC42, coupling extracellular signals to cytoskeletal reorganization. Upon CDC42 binding via its CRIB domain, CDC42BPG autophosphorylates and phosphorylates key substrates including myosin light chain (MLC2) and the myosin phosphatase targeting subunit MYPT1, thereby regulating actomyosin contractility. These activities position CDC42BPG within pathways governing cell polarity, migration, and invasion. Dysregulation of CDC42BPG has been implicated in cancer metastasis, with altered expression observed in colorectal, breast, and lung cancers. Its role in tumor cell invasiveness and cytoskeletal remodeling makes CDC42BPG an emerging drug target, particularly in oncology programs seeking to disrupt pro-metastatic signaling without broadly inhibiting ROCK isoforms.
Why PhosphoSens for CDC42BPG?
CDC42BPG presents several assay challenges: its relatively low catalytic activity compared to MRCK-alpha, sensitivity to detergent conditions, and the need for physiological ATP concentrations to accurately capture inhibitor potency against competitive scaffolds. Endpoint assays such as ADP-Glo and HTRF require ATP depletion or antibody-based detection, introducing artifacts when assaying slow or covalent inhibitors and obscuring the kinetic mechanism. Radiometric formats add throughput and safety constraints. PhosphoSens continuous fluorescence technology monitors real-time phosphorylation of CSox-based peptide substrates across the full progress curve, enabling precise Km(ATP) determination at physiological ATP, mechanistic classification of inhibitors, and direct measurement of covalent kinact/KI parameters — all in a homogeneous, antibody-free format ideal for CDC42BPG inhibitor profiling and selectivity studies across the DMPK family.
Key Pathways:
CDC42-MRCK cytoskeletal signaling
Actomyosin contractility
Cell polarity and migration
RhoGTPase signaling
Talk to a Scientist
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How pricing works:
Select a kit or substrate below, then request a quote. Bundle discounts apply automatically.
Select a kit or substrate below, then request a quote. Bundle discounts apply automatically.
Real-Time CDC42BPG Activity Assays
Continuous, real-time fluorescent assays optimized for quantitative CDC42BPG activity measurements, IC50 determination, and mechanistic studies.
Assay Format: Continuous kinetic fluorescence (real-time)
PhosphoSens-Kinetic assays directly quantify enzyme activity by continuously monitoring substrate phosphorylation or dephosphorylation in real time, generating a full progress curve in every well.
Learn more about PhosphoSens-Kinetic →Need pricing or availability? Select a kit or substrate to request a quote below.
Kits
PhosphoSens-Kinetic Kinase Activity Kit - AQT0324
Ready-to-use assay kits containing substrate and all essential reagents.
Kit Contents
- Optimized PhosphoSens® substrate (AQT0324)
- ATP, DTT, EGTA, Reaction Buffer & Dilution Buffer
Automatically save 10% when bundling 10ug recombinant enzyme with your 1,000 assay kit. View enzymes
Price: $425
Substrate
PhosphoSens Kinase Substrate AQT0324
Bulk PhosphoSens® substrate for assay development and high-throughput workflows.
Specifications
Automatically save 10% when bundling Reagent Packs with your substrate. View Reagent Packs
Price: $2795
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Request a QuoteTRF CDC42BPG Screening Assays
Robust endpoint TRF assays optimized for high-throughput screening and quantitative CDC42BPG activity measurement in plate-based workflows.
Assay Format: Time-resolved fluorescence (TRF, endpoint)
PhosphoSens-Red assays use europium-based time-resolved fluorescence detection to enable robust, plate-based quantification of enzyme activity, making them well suited for high-throughput screening workflows.
Learn more about PhosphoSens-Red →Need pricing or availability? Select a kit or substrate to request a quote below.
Kits
PhosphoSens-Red Kinase Activity Kit - AQT0837
Ready-to-use TRF assay kits containing substrate and essential reagents.
Kit Contents
- Optimized PhosphoSens® substrate (AQT0837)
- ATP, DTT, EGTA, Reaction Buffer & Dilution Buffer
- Europium Detection Solution
Automatically save 10% when bundling 10ug recombinant enzyme with your 1,000 assay kit. View enzymes
Price: $455
Substrate
PhosphoSens Kinase Substrate AQT0837
Bulk substrate for PhosphoSens-Red TRF assays and high-throughput workflows.
Specifications
Automatically save 10% when bundling Reagent Packs with your substrate. View Reagent Packs
Price: $2795
Ready to request pricing for CDC42BPG?
Select a kit, substrate, or enzyme above. Our team will confirm pricing, availability, and any applicable bundle discounts.
Request a QuoteActive Recombinant Enzymes for CDC42BPG
Wild-type and mutant forms of CDC42BPG for assay development, kinase profiling, and mechanistic studies. Enzymes are supplied active and optimized for PhosphoSens® substrates.
CDC42BPG (DMPK2), Active
Human • Baculovirus-Insect Cells
Technical Specifications
- Catalog: AQT-D17-11G
- Species: Human
- Expression System: Baculovirus-Insect Cells
- Storage Buffer: Supplied as sterile 50 mM Tris-HCl, pH 7.5, 50-300mM NaCl, 10mM glutathione, 0.1mM EDTA, 0.25-1.0mM DTT, 0-0.1mM PMSF, 10-25% glycerol
- Molecular Weight: ~78 kDa
- Purity/Activity: For specific information on a given lot, see related technical data sheet.
- Storage Conditions: Store product at -70°C. For optimal storage, aliquot target into smaller quantities after centrifugation and store at recommended temperature. For most favorable performance, avoid repeated handling and multiple freeze/thaw cycles.
Available Sizes:
Price: $$348.00
Request a QuoteFrequently Asked Questions: CDC42BPG Assays
What peptide substrate does AssayQuant use for CDC42BPG kinase assays?
AssayQuant designs CSox-based fluorescent peptide substrates derived from validated CDC42BPG phosphorylation sites, such as sequences derived from MLC2 or MYPT1. The chelation-enhanced fluorescence signal increases upon phosphorylation, enabling real-time monitoring without secondary reagents or antibodies.
Can the PhosphoSens assay detect covalent inhibitors of CDC42BPG?
Yes. Because PhosphoSens generates continuous progress curves, time-dependent loss of enzyme activity characteristic of covalent inhibition is directly observable. This allows accurate determination of kinact and KI parameters for covalent or irreversible CDC42BPG inhibitors, which endpoint formats cannot reliably capture.
How does the PhosphoSens CDC42BPG assay perform at physiological ATP concentrations?
The assay is fully compatible with physiological ATP concentrations (1-5 mM), which is critical for correctly ranking ATP-competitive inhibitors by their true cellular potency. Unlike ADP-Glo or coupled enzyme assays that require low-ATP conditions, PhosphoSens does not consume or detect ATP directly, eliminating this source of inhibitor potency artifact.
Data & Resources
Explore data and documents to support your kinase and phosphatase experiments. Download sample data, protocols and other resources to see how our assays perform and to help you get started in your own lab. All validation data generated using PhosphoSens® assays under recommended conditions.
Sample Report: AQT0734 - EGFR Assay Validation Report
Each validation report provides experimental conditions and data showing:
- Enzyme titration and linearity
- Sensor peptide substrate titration and Km determination
- ATP titration and Km determination
- DMSO titration and assay tolerance
- Inhibitor titration and IC50 determination
Protocol
Inhibitor IC50 Protocol
See how the PhosphoSens-Kinetic Assay can be used to find the IC50 of a kinase inhibitor.
Download Protocol →Webinar
Webinar: Continuous Assay Validation
Discover how continuous assay formats power deep understanding of kinase function. See how PhosphoSens® assays guide inhibitor profiling, selectivity assessment, and mechanistic characterization.
Watch the Webinar →Service
KinSight™ CDC42BPG Profiling
Need broader selectivity data? KinSight profiling runs your compounds across our full kinase panel under identical PhosphoSens conditions.
Learn about KinSight →Stay Informed
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