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NanoBRET™ TE Intracellular Kinase Assay ServicesPromega

Quantifying kinase inhibitor occupancy, selectivity, and affinity within the cellular environment, where engagement would naturally occur, is crucial to more accurately predict its engagement potencies against human kinases. In addition to equilibrium evaluation, it's also desirable to obtain kinetic parameters such as Residence Time enabling better compound optimization.

Quantitative and wide-spectrum kinase profiling services using the NanoBRET™ Target Engagement Intracellular Kinase Assay System (Promega) enable you to assess your compound's engagement for a selected intracellular target under physiological conditions. The platform also enables determination of compound Residence Time on the target while keeping the cells intact. Please submit your compound(s) of interest, and Carna will rapidly deliver cellular IC50 values and Residence Time analyses!

Investigate compound functions in intact cells expressing full-length kinases
One type of tracer covers a wide-range of kinase investigations

Please consult us for a targets not currently listed on our website or a request for custom assays.

Services

● IC50 Determinations & Residence Time Analysis

IC50Determinations
(Half-log dilutions, in 8 conc. points)
↓
Residence Time Analysis
(performed in duplicate based upon the IC50 evaluation result)

● Panel Services

CDK Panel Assay Service

Kinome-Wide Profiling Service (192 Kinase Panel)

<Guide for Service Customers>
Improved selectivity under cellular environment
Target occupancy with 1μM Crizotinib
(Right)using intracellular kinases in HEK293
(Left)using recombinant kinases assayed biochemically
at Km ATP on Carna's MSA
Biochemical Assay [ATP=Km] NanoBRET Assay

NanoBRET™ System

This proximity-based assay detects molecular interactions in live cells by measuring energy transfer from a bioluminescent protein donor (NanoLuc® luciferase) to a fluorescent probe (NanoBRET™ tracer). The NanoBRET™ TE Assay measures the apparent affinity of test compounds by competitive displacement of the NanoBRET™ tracer, reversibly bound to a NanoLuc® luciferase-kinase fusion protein expressed in live cells.

A cell-permeable fluorescent NanoBRET™ tracer, a BRET acceptor, is added to HEK293 cells expressing a full length kinase/NanoLuc® fusion protein. Engagement of the tracer to the target protein generates a BRET signal
Binding of the test compound to the target protein results in a loss of BRET signal between the target protein and the tracer inside intact cells

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