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Selectivity Screening of Library Compounds for Effect on Panels of Kinases

  • 24 kinase and substrate pairs organized in three 8-tube strips
  • Simple reaction assembly and automation-friendly protocol
  • Streamlines profiling of hits and leads for potency against families of related kinases

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Overview
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Profile Lead Compounds in Hours, Not Days

The Kinase Selectivity Profiling Systems are ideal for profiling lead-compound kinase inhibitors against a broad panel of kinases to better understand inhibitor activity and obviate any off-target effects. Each system includes kinase and substrate pairs organized in an easy-to-use 8-tube strip format optimized for fast and simple kinase profiling reactions.

The General Panel Kinase Selectivity Profiling System contains 24 kinases arranged in three 8-well strips, the corresponding substrates and cofactors, and kinase reaction buffer.

Optimized for Use With ADP-Glo™ Kinase Assay

The Kinase Selectivity Profiling Systems rely on the luminescent ADP-Glo™ Kinase Assay technology to characterize kinase selectivity. The luminescence generated by the ADP-Glo™ Kinase Assay is proportional to ADP concentration and correlates with kinase activity.

Each Kinase Selectivity Profiling System is available with or without ADP-Glo™ Assay reagents.

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Simple, Automation-Friendly Assay, No Time-Consuming Optimization

Simply dilute the stock solutions provided, and you’re ready to go.  Two quick, one-step dilutions provide working stocks of kinases and substrate/cofactor solutions. 

Concentrated kinases and substrates/cofactor stocks are first diluted and then combined with test compound in a 384-well plate. After a 1-hour incubation, the ADP-Glo™ Assay is performed to measure kinase activity.

Kinase profiling method overview 12059ma-w

Assays can be performed manually, or automated on a liquid-handler.

Single-Dose Profiling

Each Kinase Selectivity Profiling System provides enough material to profile up to 20 compounds at a single dose or create a dose response for two compounds against eight kinases at once. 
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Example single-dose inhibitor profiles of eight compounds created using the Kinase Selectivity Profiling System—TK-3. Kinase assays were assembled in the presence of the indicated compounds (1μM final concentration). Kinase activity was quantified using the ADP-Glo™ Kinase Assay. The percent activity of each kinase in the presence of each compound is shown.

Specifications

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分析証明書

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使用制限

For Research Use Only. Not for Use in Diagnostic Procedures.

保存条件

AA

See Protocol for detailed storage recommendations.

選択製品の構成品内容

Item Part # Size

Kinase Selectivity Profiling System: General Panel

V6928 1 × 24 × 50 reactions

ADP-Glo™ Kinase Assay

V6930 3 × 400 assays

分析証明書

Search by lot number

使用制限

For Research Use Only. Not for Use in Diagnostic Procedures.

保存条件

See Protocol for detailed storage recommendations.

Resources

No related resources available