labchip ez reader series - · pdf filelabchip | ez reader series benchtop readers for...

4
LabChip | EZ Reader Series Benchtop Readers for Enzymatic Assays and Selectivity Profiling The LabChip EZ Reader Series is Caliper’s next generation microfluidic instrumentation for drug screening. Using cutting edge microfluidic technology, the LabChip EZ Readers enable you to perform a broad range of enzymatic assays on a single integratable platform. The precision of microfluidics allows researchers to detect both strong and weak inhibitors with high accuracy, and routinely identify drug candidates that alternative technologies miss.

Upload: hoangduong

Post on 06-Feb-2018

220 views

Category:

Documents


1 download

TRANSCRIPT

Page 1: LabChip EZ Reader Series - · PDF fileLabChip | EZ Reader Series Benchtop Readers for Enzymatic Assays and Selectivity Profiling The LabChip EZ Reader Series is Caliper’s next generation

LabChip | EZ Reader SeriesBenchtop Readers for Enzymatic Assaysand Selectivity ProfilingThe LabChip EZ Reader Series is Caliper’s next generation microfluidic

instrumentation for drug screening. Using cutting edge microfluidic

technology, the LabChip EZ Readers enable you to perform a broad range of

enzymatic assays on a single integratable platform.

The precision of microfluidics allows researchers to detect both strong and

weak inhibitors with high accuracy, and routinely identify drug candidates

that alternative technologies miss.

Corporate Headquarters68 Elm StreetHopkinton, MA 01748-1668

Tel: 1.508.435.9500 / 1.877.LabChipFax: 1.508-435-3439Email: [email protected]

©2007 Caliper Life Sciences. All rights reserved.Caliper, LabChip, EZ Reader are tradenames and/or trademarks of Caliper Life Sciences, Inc.

EZ-BR-01 Aug07

472 mm(18.60 in)

649 mm(25.57 in)

464 mm(18.28 in)

Front View Side View

Note:Adequate space of 200 mm (8 in) must be provided in front of instrument for plate loading. Right hand side of the instrument must provide sufficient clearance to allow for reagent access.

LabChip EZ Reader Specifications Height 464 mm (18.28 in)

Width 472 mm (18.60 in)

Depth 649 mm (25.57 in)

Weight 45.5 kg (100 lbs)

Power 100/110/230 VAC 50-60 Hz

2.4/2.0/2.0 AMPS

PC Controller 115/230 VAC 50-60 Hz

5.0/2.5 AMPS

Monitor 100/240 VAC

1.5 AMPS

Part Numbers 123224 LabChip EZ Reader and Controller

122919 LabChip EZ Reader II and Controller

760407 LabChip EZ Reader and LabChip EZ Reader II 4 Sipper Chip

760404 LabChip EZ Reader II 12 Sipper Chip

760373 ProfilerPro Kinase Panel Kit - plate 1

760374 ProfilerPro Kinase Panel Kit - plate 2

760367 Separation Buffer (400 mL)

760394 ProfilerPro Four Sipper Chip with 3X 400 mL Separation Buffer

Page 2: LabChip EZ Reader Series - · PDF fileLabChip | EZ Reader Series Benchtop Readers for Enzymatic Assays and Selectivity Profiling The LabChip EZ Reader Series is Caliper’s next generation

Utilizing Caliper’s widely adopted mobility shift microfluidic assay technology, the LabChip EZ Reader II is a bench top instrument that analyzes enzyme activity by ‘sipping’ reactions from 96 or 384 well microtitre plates into a Caliper LabChip.

The data signature is generated by the shift in mobility of non-phosphorylated peptide substrates and phosphorylated products by electrophoresis in the chip and detected via LED induced fluorescence (Figure 1). The height of the fluorescent signal reveals the extent of the reaction (Figure 2).

Data is analyzed using LabChip EZ Reader software, which calculates the relative heights of the substrate and product peaks, and reports the product/(product+substrate) peak ratio (P/(P+S)).

LabChip EZ Reader supports 4-sipper chips and is designed for compound profiling using ProfilerPro kit plates.

LabChip EZ Reader II supports both 4 and 12-sipper chips making this the ideal instrument for secondary screening and MOA.

Real-Time Kinetic AnalysisThe flexibility of the LabChip EZ Reader Series al-lows its use throughout the drug discovery process including assay development, primary screening, selectivity screening, generation of Structure-Ac-tivity Relationships (SARs) and Mechanism of Ac-tion (MOA). Most important therapeutic enzymatic ‘targets’ such as kinases, proteases, phosphatases, histone deacetylases (HDAC), phosphodiesterases (PDE), and acyl-transferases can be developed using the LabChip EZ Readers.

• Real-Time Kinetic Data

• Mechanism of Action Studies

• Kinase Profiling

• Reproducable High Quality Data

• No Radioactivity

• No Antibodies

Mobility Shift Assay Technology- The Caliper Advantage...

LabChip EZ Reader SeriesLabChip EZ Reader Series

Figure 1. Shift in mobility of non-phosphorylated peptide substrate and phosphorylated product when separated in the chip by electro-phoresis and detected via LED induced fluorescence used for HDAC assay development.

Figure 2. Height of the signal reveals the extent of the reaction.

A Truer Understanding of Enzyme BehaviorOnce compounds are identified, Mechanism of Action (MOA) studies are necessary to characterize and compare the potential drug candidates. The ability to follow reaction rates in real time greatly facilitates the determination of inhibition mechanisms and the calculation of disassociation constants.

Characterization of enzyme activity through accurate determination of substrate Km and inhibitor Ki requires the ability to measure the rates of product formed as a result of an enzymatic reaction. Many of the methodologies used for identifying active compounds that modulate activity are limited to endpoint assays resulting in apparent kinetic measurements.

Using LabChip EZ Reader II, researchers may monitor enzyme reactions over time, resulting in more detailed data using less reagents.

Advantages of Microfluidic Technology with Real-Time Kinetic Analysis • Assay development and optimization is simplified and accelerated by the ability to follow reactions in real time.

• Initial rates are used to calculate actual Km and Ki values using real-time kinetics.

• Enzyme reaction linearity is precisely measured.

• Measurement of both product and substrate concentration improves data quality by providing:

- Ratiometric data analysis

- Lower false positive and negative artifacts

- Detection of low potency inhibitors

LabChip EZ Reader Series Supports ProfilerPro Kinase Profiling KitsProfile up to 12 compounds against 48 kinases in one day... in your lab!Simple, Easy & Robust... ProfilerPro kits consist of

a matched pairs of 384 well kinase assay and substrate

plates. The assay plates each contain 24 different kinases,

pre-dispensed and frozen. The substrate plates contain

the appropriate fluorescent labeled peptides and ATP. The

final ATP concentration in each reaction is at the ATP Km.

The kit also contains all reagents required and complete

protocols.

Determination of ATP-Competitive Inhibition

Irreversibility of ERBB4 Inhibition

Determination of ATP-Competitive Inhibition

Irreversibility of ERBB4 Inhibition

Page 3: LabChip EZ Reader Series - · PDF fileLabChip | EZ Reader Series Benchtop Readers for Enzymatic Assays and Selectivity Profiling The LabChip EZ Reader Series is Caliper’s next generation

Utilizing Caliper’s widely adopted mobility shift microfluidic assay technology, the LabChip EZ Reader II is a bench top instrument that analyzes enzyme activity by ‘sipping’ reactions from 96 or 384 well microtitre plates into a Caliper LabChip.

The data signature is generated by the shift in mobility of non-phosphorylated peptide substrates and phosphorylated products by electrophoresis in the chip and detected via LED induced fluorescence (Figure 1). The height of the fluorescent signal reveals the extent of the reaction (Figure 2).

Data is analyzed using LabChip EZ Reader software, which calculates the relative heights of the substrate and product peaks, and reports the product/(product+substrate) peak ratio (P/(P+S)).

LabChip EZ Reader supports 4-sipper chips and is designed for compound profiling using ProfilerPro kit plates.

LabChip EZ Reader II supports both 4 and 12-sipper chips making this the ideal instrument for secondary screening and MOA.

Real-Time Kinetic AnalysisThe flexibility of the LabChip EZ Reader Series al-lows its use throughout the drug discovery process including assay development, primary screening, selectivity screening, generation of Structure-Ac-tivity Relationships (SARs) and Mechanism of Ac-tion (MOA). Most important therapeutic enzymatic ‘targets’ such as kinases, proteases, phosphatases, histone deacetylases (HDAC), phosphodiesterases (PDE), and acyl-transferases can be developed using the LabChip EZ Readers.

• Real-Time Kinetic Data

• Mechanism of Action Studies

• Kinase Profiling

• Reproducable High Quality Data

• No Radioactivity

• No Antibodies

Mobility Shift Assay Technology- The Caliper Advantage...

LabChip EZ Reader SeriesLabChip EZ Reader Series

Figure 1. Shift in mobility of non-phosphorylated peptide substrate and phosphorylated product when separated in the chip by electro-phoresis and detected via LED induced fluorescence used for HDAC assay development.

Figure 2. Height of the signal reveals the extent of the reaction.

A Truer Understanding of Enzyme BehaviorOnce compounds are identified, Mechanism of Action (MOA) studies are necessary to characterize and compare the potential drug candidates. The ability to follow reaction rates in real time greatly facilitates the determination of inhibition mechanisms and the calculation of disassociation constants.

Characterization of enzyme activity through accurate determination of substrate Km and inhibitor Ki requires the ability to measure the rates of product formed as a result of an enzymatic reaction. Many of the methodologies used for identifying active compounds that modulate activity are limited to endpoint assays resulting in apparent kinetic measurements.

Using LabChip EZ Reader II, researchers may monitor enzyme reactions over time, resulting in more detailed data using less reagents.

Advantages of Microfluidic Technology with Real-Time Kinetic Analysis • Assay development and optimization is simplified and accelerated by the ability to follow reactions in real time.

• Initial rates are used to calculate actual Km and Ki values using real-time kinetics.

• Enzyme reaction linearity is precisely measured.

• Measurement of both product and substrate concentration improves data quality by providing:

- Ratiometric data analysis

- Lower false positive and negative artifacts

- Detection of low potency inhibitors

LabChip EZ Reader Series Supports ProfilerPro Kinase Profiling KitsProfile up to 12 compounds against 48 kinases in one day... in your lab!Simple, Easy & Robust... ProfilerPro kits consist of

a matched pairs of 384 well kinase assay and substrate

plates. The assay plates each contain 24 different kinases,

pre-dispensed and frozen. The substrate plates contain

the appropriate fluorescent labeled peptides and ATP. The

final ATP concentration in each reaction is at the ATP Km.

The kit also contains all reagents required and complete

protocols.

Determination of ATP-Competitive Inhibition

Irreversibility of ERBB4 Inhibition

Determination of ATP-Competitive Inhibition

Irreversibility of ERBB4 Inhibition

Page 4: LabChip EZ Reader Series - · PDF fileLabChip | EZ Reader Series Benchtop Readers for Enzymatic Assays and Selectivity Profiling The LabChip EZ Reader Series is Caliper’s next generation

LabChip | EZ Reader SeriesBenchtop Readers for Enzymatic Assaysand Selectivity ProfilingThe LabChip EZ Reader Series is Caliper’s next generation microfluidic

instrumentation for drug screening. Using cutting edge microfluidic

technology, the LabChip EZ Readers enable you to perform a broad range of

enzymatic assays on a single integratable platform.

The precision of microfluidics allows researchers to detect both strong and

weak inhibitors with high accuracy, and routinely identify drug candidates

that alternative technologies miss.

Corporate Headquarters68 Elm StreetHopkinton, MA 01748-1668

Tel: 1.508.435.9500 / 1.877.LabChipFax: 1.508-435-3439Email: [email protected]

©2007 Caliper Life Sciences. All rights reserved.Caliper, LabChip, EZ Reader are tradenames and/or trademarks of Caliper Life Sciences, Inc.

EZ-BR-01 Aug07

472 mm(18.60 in)

649 mm(25.57 in)

464 mm(18.28 in)

Front View Side View

Note:Adequate space of 200 mm (8 in) must be provided in front of instrument for plate loading. Right hand side of the instrument must provide sufficient clearance to allow for reagent access.

LabChip EZ Reader Specifications Height 464 mm (18.28 in)

Width 472 mm (18.60 in)

Depth 649 mm (25.57 in)

Weight 45.5 kg (100 lbs)

Power 100/110/230 VAC 50-60 Hz

2.4/2.0/2.0 AMPS

PC Controller 115/230 VAC 50-60 Hz

5.0/2.5 AMPS

Monitor 100/240 VAC

1.5 AMPS

Part Numbers 123224 LabChip EZ Reader and Controller

122919 LabChip EZ Reader II and Controller

760407 LabChip EZ Reader and LabChip EZ Reader II 4 Sipper Chip

760404 LabChip EZ Reader II 12 Sipper Chip

760373 ProfilerPro Kinase Panel Kit - plate 1

760374 ProfilerPro Kinase Panel Kit - plate 2

760367 Separation Buffer (400 mL)

760394 ProfilerPro Four Sipper Chip with 3X 400 mL Separation Buffer