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NanoBRET™ Target Engagement BET BRD Assays

32463142-L1-NanoBRET-Chalk-Talk

Directly Measure BET BRD-Test Compound Affinity and Residence Time

  • Compound and tracer compete directly for the binding site
  • Assays rely on full-length proteins that are similar to the native forms
  • Express target proteins at low levels

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Catalog number selected: N2131

$ 3,570.00
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NanoBRET™ Target Engagement BET BRD Assays
Assay/1,000 assays
$ 3,570.00
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32463142-NanoBretBETBRD-OverviewImage2

NanoBRET™ Technology for Target Engagement

The NanoBRET™ Target Engagement (TE) Assay measures compound binding at select target proteins in intact cells, in real time. The NanoBRET™ TE Assay uses four key components: An expressed cellular target protein that is fused to the bright NanoLuc® luciferase; a cell-permeable fluorescent tracer that specifically binds to the target protein; a substrate for NanoLuc® luciferase; and a cell-impermeable inhibitor for NanoLuc® luciferase. 

The assay uses bioluminescence resonance energy transfer (BRET), achieved by transferring the luminescent energy from NanoLuc® luciferase to the fluorescent tracer that is bound to the target protein-NanoLuc® fusion. This energy transfer makes it possible to directly measure compound binding affinity as well as compound-target residence time.

Compounds that are applied to the cells and specifically engage the intracellular target protein-NanoLuc® fusion will result in a decrease in BRET. To ensure accurate assessment of intracellular target engagement, a NanoLuc® inhibitor is used to mitigate any extracellular NanoLuc® signal that may arise from cells compromised during handling, while not adversely affecting NanoLuc® luciferase expressed within healthy living cells

Analyze Binding Affinity and Permeability

The NanoBRET™ TE Assay analyzes the apparent binding affinity and permeability of test compounds by competitive displacement of a NanoBRET™ Tracer reversibly bound to a NanoLuc® fusion protein in cells.

Binding of test compound results in loss of NanoBRET signal
Compound engagement is measured in a competitive format using a cell-permeable NanoBRET™ tracer. Binding of the test compound results in a loss of NanoBRET™ signal between the target protein and the tracer in intact cells.

The optimal NanoBRET™ Tracer affinity is determined for each target protein.

13990MA-W-2
For analysis of target engagement by a test compound, cells are treated with a fixed concentration of NanoBRET™ Tracer that is near the EC50 value of the NanoBRET™ Tracer dose response curve.
13991MA-W-2
To determine test compound affinity, cells are titrated with varying concentrations of the test compound in the presence of a fixed concentration (EC50–EC80) of tracer.

The optimal NanoBRET™ Tracer affinity is determined for the bromodomain (BRD)-NanoLuc® luciferase fusion protein.

13694MA-W
Apparent intracellular NanoBRET™ tracer affinity in HEK293 cells transiently expressing NanoLuc®-BRD4 full-length fusion protein.

Directly Measure Residence Time

The NanoBRET™ TE Assay directly measures the durability of compound-target engagement after binding in real time and provides information on full-length protein targets.

13716MA-W
Compound residence time is determined from the rate of NanoBRET™ signal between the tracer and the NanoLuc® fusion protein.

13725MA-W
The NanoBRET™ TE Intracellular Assay analyzes compound residence time at a bromodomain (BRD)-NanoLuc® luciferase fusion protein.

Evaluate Key Drug Target Class

The NanoBRET™ Target Engagement Assay can be used to evaluate binding of compounds to BRDs, a key drug target class.

13695MA-W
NanoBRET™ Tracer competition in transiently transfected HEK293 cells expressing NanoLuc®-BRD4 full-length fusion proteins.

DNA Bundle Components

13738MA-W
13739MA-W
12737MA-W
13740MA-W
13741MA-W
13742MA-W
13743MA-W
12900MA-W

Specifications

You are viewing: N2131 Change Configuration

What's in the box?

Item Part # SizeAvailable Separately

Transfection Carrier DNA

E488B 1 × 100μg View Product

NanoBRET™ Nano-Glo® Substrate

N157C 1 × 330μl

NanoLuc®-BRD4 FL Fusion Vector

N169A 1 × 20μg

Tracer Dilution Buffer

N219A 1 × 5ml View Product

NanoBRET™ Intracellular TE BET BRD Tracer

N234B 1 × 1.1ml

Extracellular NanoLuc® Inhibitor

N235B 1 × 110μl

SDS

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Certificate of Analysis

See all certificates for N2131 Search
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Use Restrictions

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

Storage Conditions

AA

See Protocol for storage recommendations.

Patents and Disclaimers

BY USE OF THIS PRODUCT, RESEARCHER AGREES TO BE BOUND BY THE TERMS OF THIS LIMITED USE LABEL LICENSE. If researcher is not willing to accept the terms of this label license, and the product is unused, Promega will accept return of the unused product and provide researcher with a full refund.

Researcher may use this product for research use only; no commercial use is allowed. Commercial use means any and all uses of this product by a party in exchange for consideration, including, but not limited to (1) use in further product manufacture; (2) use in provision of services, information or data; and (3) resale of the product, whether or not such product is resold for use in research. Researcher shall have no right to modify or otherwise create variations of the product. No other use or transfer of this product is authorized without the prior express written consent of Promega.

For uses of Nano-Glo®-branded reagents intended for energy transfer (such as bioluminescence resonance energy transfer) to acceptors other than a genetically encoded autofluorescent protein, researchers must:
(a) use NanoBRET™-branded energy acceptors (e.g., BRET-optimized HaloTag® ligands) for all determinations of energy transfer activity by this product; or
(b) contact Promega to obtain a license for use of the product for energy transfer assays to energy acceptors not manufactured by Promega.

With respect to any uses outside this label license, including any diagnostic, therapeutic, prophylactic or commercial uses, please contact Promega for supply and licensing information. PROMEGA MAKES NO REPRESENTATIONS OR WARRANTIES OF ANY KIND, EITHER EXPRESSED OR IMPLIED, INCLUDING FOR MERCHANTABILITY OR FITNESS FOR A PARTICULAR PURPOSE, WITH REGARD TO THE PRODUCT. The terms of this label license shall be governed under the laws of the State of Wisconsin, USA.

BY USE OF THIS PRODUCT, RESEARCHER AGREES TO BE BOUND BY THE TERMS OF THIS LIMITED USE LABEL LICENSE. If researcher is not willing to accept the terms of this label license, and the product is unused, Promega will accept return of the unused product and provide researcher with a full refund.

Researcher may use this product for research use only; no transfer or commercial use of this product is allowed. Commercial use means any and all uses of this product by a party in exchange for consideration, including, but not limited to (1) use in further product manufacture; (2) use in provision of services, information or data; and (3) resale of the product, whether or not such product is resold for use in research. Researcher shall have no right to modify or otherwise create variations of the nucleotide sequence of the luciferase gene. No other use of this product is authorized without the prior express written consent of Promega.

In addition, researcher must:
(1a) use Nano-Glo®-branded luminescent assay reagents (LARs) for all determinations of luminescence activity of this product; or
(1b) contact Promega to obtain a license for use of the product with LARs not manufactured by Promega.

For uses of Nano-Glo®-branded LARs intended for energy transfer (such as bioluminescence resonance energy transfer) to acceptors other than a genetically encoded autofluorescent protein, researcher must:
(2a) use NanoBRET™-branded energy acceptors (e.g., BRET-optimized HaloTag® ligands) for all determinations of energy transfer activity by this product; or
(2b) contact Promega to obtain a license for use of the product for energy transfer assays to energy acceptors not manufactured by Promega.

With respect to any uses outside this label license, including any diagnostic, therapeutic, prophylactic or commercial uses, please contact Promega for supply and licensing information. PROMEGA MAKES NO REPRESENTATIONS OR WARRANTIES OF ANY KIND, EITHER EXPRESSED OR IMPLIED, INCLUDING FOR MERCHANTABILITY OR FITNESS FOR A PARTICULAR PURPOSE, WITH REGARD TO THE PRODUCT. The terms of this label license shall be governed under the laws of the State of Wisconsin, USA.

U.S. Pat. No. 8,809,529, European Pat. No. 2635582 and other patents and patents pending.

U.S. Pat. No. 9,056,885 and other patents pending.

Patent Pending.

U.S. Pat. Nos. 8,557,970 and 8,669,103 and other patents and patents pending.

Licensed under EP1295121 and EP1088233.

Specifications

You are viewing: N2180 Change Configuration

What's in the box?

Item Part # Size

NanoBRET™ TE Intracellular BET BRD Assay

N2131 1 × 1,000 assays

NanoBRET™ TE BET BRD DNA Bundle

N2150 1 × 1 each

SDS

Choose language:

Certificate of Analysis

See all certificates for N2180 Search
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Use Restrictions

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

Storage Conditions

See Protocol for storage recommendations.

Patents and Disclaimers

BY USE OF THIS PRODUCT, RESEARCHER AGREES TO BE BOUND BY THE TERMS OF THIS LIMITED USE LABEL LICENSE. If researcher is not willing to accept the terms of this label license, and the product is unused, Promega will accept return of the unused product and provide researcher with a full refund.

Researcher may use this product for research use only; no commercial use is allowed. Commercial use means any and all uses of this product by a party in exchange for consideration, including, but not limited to (1) use in further product manufacture; (2) use in provision of services, information or data; and (3) resale of the product, whether or not such product is resold for use in research. Researcher shall have no right to modify or otherwise create variations of the product. No other use or transfer of this product is authorized without the prior express written consent of Promega.

For uses of Nano-Glo®-branded reagents intended for energy transfer (such as bioluminescence resonance energy transfer) to acceptors other than a genetically encoded autofluorescent protein, researchers must:
(a) use NanoBRET™-branded energy acceptors (e.g., BRET-optimized HaloTag® ligands) for all determinations of energy transfer activity by this product; or
(b) contact Promega to obtain a license for use of the product for energy transfer assays to energy acceptors not manufactured by Promega.

With respect to any uses outside this label license, including any diagnostic, therapeutic, prophylactic or commercial uses, please contact Promega for supply and licensing information. PROMEGA MAKES NO REPRESENTATIONS OR WARRANTIES OF ANY KIND, EITHER EXPRESSED OR IMPLIED, INCLUDING FOR MERCHANTABILITY OR FITNESS FOR A PARTICULAR PURPOSE, WITH REGARD TO THE PRODUCT. The terms of this label license shall be governed under the laws of the State of Wisconsin, USA.

BY USE OF THIS PRODUCT, RESEARCHER AGREES TO BE BOUND BY THE TERMS OF THIS LIMITED USE LABEL LICENSE. If researcher is not willing to accept the terms of this label license, and the product is unused, Promega will accept return of the unused product and provide researcher with a full refund.

Researcher may use this product for research use only; no transfer or commercial use of this product is allowed. Commercial use means any and all uses of this product by a party in exchange for consideration, including, but not limited to (1) use in further product manufacture; (2) use in provision of services, information or data; and (3) resale of the product, whether or not such product is resold for use in research. Researcher shall have no right to modify or otherwise create variations of the nucleotide sequence of the luciferase gene. No other use of this product is authorized without the prior express written consent of Promega.

In addition, researcher must:
(1a) use Nano-Glo®-branded luminescent assay reagents (LARs) for all determinations of luminescence activity of this product; or
(1b) contact Promega to obtain a license for use of the product with LARs not manufactured by Promega.

For uses of Nano-Glo®-branded LARs intended for energy transfer (such as bioluminescence resonance energy transfer) to acceptors other than a genetically encoded autofluorescent protein, researcher must:
(2a) use NanoBRET™-branded energy acceptors (e.g., BRET-optimized HaloTag® ligands) for all determinations of energy transfer activity by this product; or
(2b) contact Promega to obtain a license for use of the product for energy transfer assays to energy acceptors not manufactured by Promega.

With respect to any uses outside this label license, including any diagnostic, therapeutic, prophylactic or commercial uses, please contact Promega for supply and licensing information. PROMEGA MAKES NO REPRESENTATIONS OR WARRANTIES OF ANY KIND, EITHER EXPRESSED OR IMPLIED, INCLUDING FOR MERCHANTABILITY OR FITNESS FOR A PARTICULAR PURPOSE, WITH REGARD TO THE PRODUCT. The terms of this label license shall be governed under the laws of the State of Wisconsin, USA.

U.S. Pat. No. 8,809,529, European Pat. No. 2635582 and other patents and patents pending.

U.S. Pat. No. 9,056,885 and other patents pending.

Patent Pending.

U.S. Pat. Nos. 8,557,970 and 8,669,103 and other patents and patents pending.

Licensed under EP1295121 and EP1088233.

Specifications

You are viewing: N2130 Change Configuration

What's in the box?

Item Part # SizeConcentrationAvailable Separately

Transfection Carrier DNA

E488A 1 × 20μg1μg/μl View Product

NanoBRET™ Nano-Glo® Substrate

N157A 1 × 50μl

NanoLuc®-BRD4 FL Fusion Vector

N169A 1 × 20μg

Tracer Dilution Buffer

N219A 1 × 5ml View Product

NanoBRET™ Intracellular TE BET BRD Tracer

N234A 1 × 110μl

Extracellular NanoLuc® Inhibitor

N235A 1 × 17μl

SDS

Choose language:

Certificate of Analysis

See all certificates for N2130 Search
View more results
No results
Loading…

Use Restrictions

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

Storage Conditions

AA

See Protocol for storage recommendations.

Patents and Disclaimers

BY USE OF THIS PRODUCT, RESEARCHER AGREES TO BE BOUND BY THE TERMS OF THIS LIMITED USE LABEL LICENSE. If researcher is not willing to accept the terms of this label license, and the product is unused, Promega will accept return of the unused product and provide researcher with a full refund.

Researcher may use this product for research use only; no commercial use is allowed. Commercial use means any and all uses of this product by a party in exchange for consideration, including, but not limited to (1) use in further product manufacture; (2) use in provision of services, information or data; and (3) resale of the product, whether or not such product is resold for use in research. Researcher shall have no right to modify or otherwise create variations of the product. No other use or transfer of this product is authorized without the prior express written consent of Promega.

For uses of Nano-Glo®-branded reagents intended for energy transfer (such as bioluminescence resonance energy transfer) to acceptors other than a genetically encoded autofluorescent protein, researchers must:
(a) use NanoBRET™-branded energy acceptors (e.g., BRET-optimized HaloTag® ligands) for all determinations of energy transfer activity by this product; or
(b) contact Promega to obtain a license for use of the product for energy transfer assays to energy acceptors not manufactured by Promega.

With respect to any uses outside this label license, including any diagnostic, therapeutic, prophylactic or commercial uses, please contact Promega for supply and licensing information. PROMEGA MAKES NO REPRESENTATIONS OR WARRANTIES OF ANY KIND, EITHER EXPRESSED OR IMPLIED, INCLUDING FOR MERCHANTABILITY OR FITNESS FOR A PARTICULAR PURPOSE, WITH REGARD TO THE PRODUCT. The terms of this label license shall be governed under the laws of the State of Wisconsin, USA.

BY USE OF THIS PRODUCT, RESEARCHER AGREES TO BE BOUND BY THE TERMS OF THIS LIMITED USE LABEL LICENSE. If researcher is not willing to accept the terms of this label license, and the product is unused, Promega will accept return of the unused product and provide researcher with a full refund.

Researcher may use this product for research use only; no transfer or commercial use of this product is allowed. Commercial use means any and all uses of this product by a party in exchange for consideration, including, but not limited to (1) use in further product manufacture; (2) use in provision of services, information or data; and (3) resale of the product, whether or not such product is resold for use in research. Researcher shall have no right to modify or otherwise create variations of the nucleotide sequence of the luciferase gene. No other use of this product is authorized without the prior express written consent of Promega.

In addition, researcher must:
(1a) use Nano-Glo®-branded luminescent assay reagents (LARs) for all determinations of luminescence activity of this product; or
(1b) contact Promega to obtain a license for use of the product with LARs not manufactured by Promega.

For uses of Nano-Glo®-branded LARs intended for energy transfer (such as bioluminescence resonance energy transfer) to acceptors other than a genetically encoded autofluorescent protein, researcher must:
(2a) use NanoBRET™-branded energy acceptors (e.g., BRET-optimized HaloTag® ligands) for all determinations of energy transfer activity by this product; or
(2b) contact Promega to obtain a license for use of the product for energy transfer assays to energy acceptors not manufactured by Promega.

With respect to any uses outside this label license, including any diagnostic, therapeutic, prophylactic or commercial uses, please contact Promega for supply and licensing information. PROMEGA MAKES NO REPRESENTATIONS OR WARRANTIES OF ANY KIND, EITHER EXPRESSED OR IMPLIED, INCLUDING FOR MERCHANTABILITY OR FITNESS FOR A PARTICULAR PURPOSE, WITH REGARD TO THE PRODUCT. The terms of this label license shall be governed under the laws of the State of Wisconsin, USA.

U.S. Pat. No. 8,809,529, European Pat. No. 2635582 and other patents and patents pending.

Patent Pending.

U.S. Pat. No. 9,056,885 and other patents pending.

U.S. Pat. Nos. 8,557,970 and 8,669,103 and other patents and patents pending.

Licensed under EP1295121 and EP1088233.

Specifications

You are viewing: N2140 Change Configuration

What's in the box?

Item Part # SizeAvailable Separately

NanoBRET™ Nano-Glo® Substrate

N157D 1 × 3.3ml

Tracer Dilution Buffer

N219B 1 × 50ml View Product

NanoBRET™ Intracellular TE BET BRD Tracer

N234B 10 × 1.1ml

Extracellular NanoLuc® Inhibitor

N235C 1 × 1.1ml

SDS

Choose language:

Certificate of Analysis

See all certificates for N2140 Search
View more results
No results
Loading…

Use Restrictions

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

Storage Conditions

AA

See Protocol for storage recommendations.

Patents and Disclaimers

BY USE OF THIS PRODUCT, RESEARCHER AGREES TO BE BOUND BY THE TERMS OF THIS LIMITED USE LABEL LICENSE. If researcher is not willing to accept the terms of this label license, and the product is unused, Promega will accept return of the unused product and provide researcher with a full refund.

Researcher may use this product for research use only; no commercial use is allowed. Commercial use means any and all uses of this product by a party in exchange for consideration, including, but not limited to (1) use in further product manufacture; (2) use in provision of services, information or data; and (3) resale of the product, whether or not such product is resold for use in research. Researcher shall have no right to modify or otherwise create variations of the product. No other use or transfer of this product is authorized without the prior express written consent of Promega.

For uses of Nano-Glo®-branded reagents intended for energy transfer (such as bioluminescence resonance energy transfer) to acceptors other than a genetically encoded autofluorescent protein, researchers must:
(a) use NanoBRET™-branded energy acceptors (e.g., BRET-optimized HaloTag® ligands) for all determinations of energy transfer activity by this product; or
(b) contact Promega to obtain a license for use of the product for energy transfer assays to energy acceptors not manufactured by Promega.

With respect to any uses outside this label license, including any diagnostic, therapeutic, prophylactic or commercial uses, please contact Promega for supply and licensing information. PROMEGA MAKES NO REPRESENTATIONS OR WARRANTIES OF ANY KIND, EITHER EXPRESSED OR IMPLIED, INCLUDING FOR MERCHANTABILITY OR FITNESS FOR A PARTICULAR PURPOSE, WITH REGARD TO THE PRODUCT. The terms of this label license shall be governed under the laws of the State of Wisconsin, USA.

U.S. Pat. No. 8,809,529, European Pat. No. 2635582 and other patents and patents pending.

U.S. Pat. No. 9,056,885 and other patents pending.

Patent Pending.

Licensed under EP1295121 and EP1088233.

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