NanoBRET® Target Engagement HDAC Assays

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Directly Measure HDAC-Test Compound Affinity and Residence Time in Live Cells

  • 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: N2080

$ 765.00
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NanoBRET® Target Engagement HDAC Assays
Assay/100 assays
$ 765.00
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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
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
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 histone deacetylase (HDAC)-NanoLuc® luciferase fusion protein.

NanoLuc- HDAC6 FL fusion protein

14006MA-W
Apparent intracellular NanoBRET® tracer affinity in HEK293 cells transiently expressing NanoLuc®-HDAC6 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.

13724MA-W
The NanoBRET® TE Intracellular HDAC Assay analyzes compound residence time at a histone deacetylase (HDAC)-NanoLuc® fusion protein.

Evaluate Key Drug Target Class

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

14007MA-W
The NanoBRET® TE Assay analyzes compound binding to a histone deacetylase (HDAC)-NanoLuc® fusion protein.

DNA Bundle Components

13726MA-W
HDAC2 NanoLuc FL Fusion Vector
HDAC3 NanoLuc FL Fusion Vector
NanoLuc HDAC6 FL Fusion Vector
NanoLuc HDAC6 CD2 Fusion Vector
HDAC10 NanoLuc Fusion Vector

Specifications

You are viewing: N2080 Change Configuration

What's in the box?

Item Part # Size Concentration Available Separately

Transfection Carrier DNA

E488A 1 × 20μg 1μg/μl View Product

NanoBRET® Nano-Glo® Substrate

N157A 1 × 50μl View Product

Tracer Dilution Buffer

N219A 1 × 5ml View Product

NanoLuc®-HDAC6 FL Fusion Vector

N223A 1 × 20μg

NanoBRET® Intracellular TE HDAC Tracer

N233A 1 × 110μl

Extracellular NanoLuc® Inhibitor

N235A 1 × 17μl View Product

Certificate of Analysis

Search by lot number

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:
(i) use NanoBRET®-branded energy acceptors (e.g., BRET-optimized HaloTag® ligands) for all determinations of energy transfer activity by this product; or
(ii) 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 this product (Nano-Glo® ORF Vector) for energy transfer (such as bioluminescence resonance energy transfer), researcher must:
(2a) use NanoBRET®-branded luminescent assay reagents (LARs; e.g., NanoBRET® Nano-Glo® Substrate) or Intracellular TE Nano-Glo® Substrate/Inhibitor for all determinations of luminescent activity; and
(2b) use NanoBRET®-branded energy acceptors (e.g., NanoBRET® tracers, NanoBRET® dyes, BRET-optimized HaloTag® ligands) for all determinations of energy transfer activity; or
(2c) contact Promega to obtain a license for use of the product for energy transfer assays using energy acceptors not manufactured by Promega. No license is needed if the energy transfer acceptor is a genetically encoded autofluorescent protein.

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, Japanese Pat. No. 5889910 and other patents and patents pending.

U.S. Pat. Nos. 9,056,885 and 10,139,400, European Pat. No. 2782916 and other patents pending.

Patent Pending.

U.S. Pat. Nos. 8,557,970, 8,669,103, 9,777,311, 9,840,730, 9,951,373, 10,233,485, 10,633,690, 10,774,364, 10,844,422, 11,365,436, 11,661,623, 11,667,950; European Pat. Nos. 2456864, 2635595, 2990478, 3181687, 3409764; Japanese Pat. Nos. 6038649, 6155424, 6227615, 6374420, 6539689; and other patents and patents pending.

U.S. Pat. Nos. 10,067,149 and 10,024,862, European Pat. No. 2932267, Japanese Pat. Nos. 6751294 and 7092691 and other patents and patents pending.

Specifications

You are viewing: N2081 Change Configuration

What's in the box?

Item Part # Size Available Separately

Transfection Carrier DNA

E488B 1 × 100μg View Product

NanoBRET® Nano-Glo® Substrate

N157C 1 × 330μl View Product

Tracer Dilution Buffer

N219A 1 × 5ml View Product

NanoLuc®-HDAC6 FL Fusion Vector

N223A 1 × 20μg

NanoBRET® Intracellular TE HDAC Tracer

N233B 1 × 1.1ml

Extracellular NanoLuc® Inhibitor

N235B 1 × 110μl View Product

Certificate of Analysis

Search by lot number

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:
(i) use NanoBRET®-branded energy acceptors (e.g., BRET-optimized HaloTag® ligands) for all determinations of energy transfer activity by this product; or
(ii) 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 this product (Nano-Glo® ORF Vector) for energy transfer (such as bioluminescence resonance energy transfer), researcher must:
(2a) use NanoBRET®-branded luminescent assay reagents (LARs; e.g., NanoBRET® Nano-Glo® Substrate) or Intracellular TE Nano-Glo® Substrate/Inhibitor for all determinations of luminescent activity; and
(2b) use NanoBRET®-branded energy acceptors (e.g., NanoBRET® tracers, NanoBRET® dyes, BRET-optimized HaloTag® ligands) for all determinations of energy transfer activity; or
(2c) contact Promega to obtain a license for use of the product for energy transfer assays using energy acceptors not manufactured by Promega. No license is needed if the energy transfer acceptor is a genetically encoded autofluorescent protein.

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, Japanese Pat. No. 5889910 and other patents and patents pending.

U.S. Pat. Nos. 9,056,885 and 10,139,400, European Pat. No. 2782916 and other patents pending.

Patent Pending.

U.S. Pat. Nos. 8,557,970, 8,669,103, 9,777,311, 9,840,730, 9,951,373, 10,233,485, 10,633,690, 10,774,364, 10,844,422, 11,365,436, 11,661,623, 11,667,950; European Pat. Nos. 2456864, 2635595, 2990478, 3181687, 3409764; Japanese Pat. Nos. 6038649, 6155424, 6227615, 6374420, 6539689; and other patents and patents pending.

U.S. Pat. Nos. 10,067,149 and 10,024,862, European Pat. No. 2932267, Japanese Pat. Nos. 6751294 and 7092691 and other patents and patents pending.

Specifications

You are viewing: N2170 Change Configuration

What's in the box?

Item Part # Size

NanoBRET® TE Intracellular HDAC Assay

N2081 1 × 1,000 assays

NanoBRET® TE HDAC DNA Bundle

N2120 1 × 1 each

Certificate of Analysis

Search by lot number

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 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 this product (Nano-Glo® ORF Vector) for energy transfer (such as bioluminescence resonance energy transfer), researcher must:
(2a) use NanoBRET®-branded luminescent assay reagents (LARs; e.g., NanoBRET® Nano-Glo® Substrate) or Intracellular TE Nano-Glo® Substrate/Inhibitor for all determinations of luminescent activity; and
(2b) use NanoBRET®-branded energy acceptors (e.g., NanoBRET® tracers, NanoBRET® dyes, BRET-optimized HaloTag® ligands) for all determinations of energy transfer activity; or
(2c) contact Promega to obtain a license for use of the product for energy transfer assays using energy acceptors not manufactured by Promega. No license is needed if the energy transfer acceptor is a genetically encoded autofluorescent protein.

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, Japanese Pat. No. 5889910 and other patents and patents pending.

U.S. Pat. Nos. 9,056,885 and 10,139,400, European Pat. No. 2782916 and other patents pending.

Patent Pending.

U.S. Pat. Nos. 8,557,970, 8,669,103, 9,777,311, 9,840,730, 9,951,373, 10,233,485, 10,633,690, 10,774,364, 10,844,422, 11,365,436, 11,661,623, 11,667,950; European Pat. Nos. 2456864, 2635595, 2990478, 3181687, 3409764; Japanese Pat. Nos. 6038649, 6155424, 6227615, 6374420, 6539689; and other patents and patents pending.

U.S. Pat. Nos. 10,067,149 and 10,024,862, European Pat. No. 2932267, Japanese Pat. Nos. 6751294 and 7092691 and other patents and patents pending.

Specifications

You are viewing: N2090 Change Configuration

What's in the box?

Item Part # Size Available Separately

NanoBRET® Nano-Glo® Substrate

N157D 1 × 3.3ml View Product

Tracer Dilution Buffer

N219B 1 × 50ml View Product

NanoBRET® Intracellular TE HDAC Tracer

N233B 10 × 1.1ml

Extracellular NanoLuc® Inhibitor

N235C 1 × 1.1ml View Product

Certificate of Analysis

Search by lot number

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:
(i) use NanoBRET®-branded energy acceptors (e.g., BRET-optimized HaloTag® ligands) for all determinations of energy transfer activity by this product; or
(ii) 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, Japanese Pat. No. 5889910 and other patents and patents pending.

U.S. Pat. Nos. 9,056,885 and 10,139,400, European Pat. No. 2782916 and other patents pending.

Patent Pending.

U.S. Pat. Nos. 10,067,149 and 10,024,862, European Pat. No. 2932267, Japanese Pat. Nos. 6751294 and 7092691 and other patents and patents pending.

U.S. Pat. Nos. 8,557,970, 8,669,103, 9,777,311, 9,840,730, 9,951,373, 10,233,485, 10,633,690, 10,774,364, 10,844,422, 11,365,436, 11,661,623, 11,667,950; European Pat. Nos. 2456864, 2635595, 2990478, 3181687, 3409764; Japanese Pat. Nos. 6038649, 6155424, 6227615, 6374420, 6539689; and other patents and patents pending.

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