Promega Corporation

Life Technologies Corporation

Thomas Machleidt

Keith V Wood

Thomas A Kirkland

Mary P Hall

Lance P Encell

Brock Binkowski

Matthew B Robers

Melanie Dart

Monika G Wood

Joel R Walker

Andrew S Dixon

Marie Schwinn

Poncho Meisenheimer

Nidhi Nath

Said A Goueli

James Unch

Anton Shakhmin

Hicham Zegzouti

Subhanjan Mondal

Dileep K Pulukkunat

Wenhui Zhou

Ce Shi

Rachel Friedman Ohana

Carolyn Woodroofe Hitko

Matt Robers

Kris Zimmerman

Hui Wang

Braeden L Butler

Kurt William Vogel

Roderick G Flemming

Thomas P Smith

Steven Riddle

Robert Horton

Gregory Michaud

Kevin Vedvik

Kristin Huwiler

Brock F Binkowski

Thomas Kirland

Braeden Butler

Described are substituted imidazo[1,2-a]pyrazine compounds, which are coelenterazine analogues, kits comprising the analogues, and methods of using the compounds for the detection of luminescence in luciferase-based assays. Also described are methods from making the compounds, such as a method using aminopyrazine acetophosphonates as synthesis intermediates.

Substituted imidazo[1,2-α]pyrazines as luciferase substrates

Provided herein are compositions and methods for the assembly of a bioluminescent complex from two or more non-luminescent (e.g., substantially non-luminescent) peptide and/or polypeptide units. In particular, bioluminescent activity is conferred upon a non-luminescent polypeptide via structural complementation with another, complementary non-luminescent peptide.

Activation of bioluminescence by structural complementation

Provided herein are systems and methods for characterizing target/ligand engagement. In particular, luciferase-labeled polypeptide targets are used to detect or quantify target/ligand engagement (e.g., within a cell or cell lysate).

Luciferase-based thermal shift assays

Described are processes for preparing substituted imidazo[1,2-a]pyrazine compounds of formula (I): by reacting a compound of formula (xi): with carbonyldiimidazole to form the compound of formula (I).

Process for preparing substituted imidazo[1,2-&#x3b1;]pyrazines

Provided herein are compositions and methods for detection and analysis of intracellular binding of a bioactive agent to a cellular target. In particular, bioactive agents tethered to fluorophores, cellular targets fused to bioluminescent reporters, and methods of detecting and analyzing the interaction of bioactive agents with cellular targets therewith.

Recognition of cellular target binding by a bioactive agent using intracellular bioluminescence resonance energy transfer

Compounds that may inhibit-derived luciferases are disclosed as well as compositions and kits comprising the compounds and methods of using the compounds.

Nanoluc suicide substrates

Provided herein are compositions and methods for stabilizing coelenterazine and analogs or derivatives thereof, and for improving the solubility and reconstitution efficiency of coelenterazine and analogs and derivatives thereof.

Compositions and methods for stabilizing coelenterazine and analogs and derivatives thereof

Activation of bioluminescene by structural complementation

Provided herein are substantially non-luminescent peptide/polypeptide tags that are inserted internally within a protein of interest or between N-terminal and C-terminal peptides/polypeptides. Interaction of the internally-inserted tag with a complement polypeptide/peptide that is also substantially non-luminescent results in the formation a bioluminescent reporter complex.

Internal protein tags

Described are substituted imidazo[1,2-a]pyrazine compounds, which are coelenterazine analogues, kits comprising the compounds, and methods of using the compounds for the detection of luminescence in luciferase-based assays. Also described are methods of making the compounds, such as a method using aminopyrazine acetophosphonates as synthesis intermediates. The substituted imidazo[1,2-a]pyrazine compounds include compounds of formula (I): 

Substituted imidazo[1,2-a]pyrazines as luciferase substrates

Compounds that may inhibit-derived luciferases are disclosed as well as compositions and kits comprising the compounds, and methods of using the compounds.

Functionalized NANOLUC inhibitors

Described are coelenterazine analogues, methods for making the analogues, kits comprising the analogues, and methods of using the compounds for the detection of luminescence in luciferase-based assays.

Coelenterazine analogues

Growing community of inventors

Madison, WI, United States of America

Thomas Machleidt