IP Library Granted Patent US 8,835,632
Granted Patent B2
US 8,835,632 · App. 12/743,128 · Granted Sep 16, 2014

Methods to increase the photostability of dyes

Inventors: Klaus Hahn (Chapel Hill, NC); Alexei Toutchkine (Arlington, MA)
Assignee: The University of North Carolina at Chapel Hill
G01N33/582C09B23/107C09B23/0058
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Quick Facts
Patent No.
US 8,835,632
App. No.
12/743,128
Granted
Sep 16, 2014
Kind
B2
Abstract

The presently disclosed subject matter provides dyes having an improved photostability, biosensors comprising such dyes, and methods of use thereof, including methods for detecting target molecules in a sample under test and for live-cell imaging. The dyes can include a binding member, including a biomolecule or fragments thereof, which can interact with target molecules of interest and can be specific to a given conformational state or covalent modification, e.g., phosphorylation, of the target molecule. The presently disclosed dyes can be used for detecting changes in the binding, conformational change, or posttranslational modification of the target molecule.

Claims (17)

1. A dye of Formula (II);

wherein:

m is an integer from 1 to 4;

X 2 is halogen;

R 1 , R 2 , R 3 , R 6 , and R 7 are each independently selected from the group consisting of H, alkyl, substituted alkyl, heteroalkyl, substituted heteroalkyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, aryl, substituted aryl, aralkyl, hydroxyl, alkoxyl, hydroxyalkyl, hydroxycycloalkyl, alkoxycycloalkyl, aminoalkyl, acyloxyl, alkylaminoalkyl, alkoxycarbonyl, alkyleneaminoalkyl, alkylenesulfate, —(CH 2 ) p —SO 3 , —(CH 2 ) p —N + (CH 3 ) 2 —(CH 2 ) p NCS, and —(CH 2 ) p —NH—CO—CH 2 —X 2 ; wherein X 2 is halogen;

R 5 is selected from the group consisting of alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, aryl, substituted aryl, aralkyl, hydroxyl, alkoxyl, hydroxyalkyl, hydroxycycloalkyl, alkoxycycloalkyl, aminoalkyl, acyloxyl, alkylaminoalkyl, alkoxycarbonyl, alkyleneaminoalkyl, alkylenesulfate, —(CH 2 ) p —SO 3 , —(CH 2 ) p —N + CH 3 ) 2 —(CH 2 ) p —NCS, and —(CH 2 ) p —NH—CO—CH 2 —X 2 ; wherein X 2 is halogen;

R 8 is selected from the group consisting of H, alkyl, substituted alkyl, hydroxyl, amino, nitro, alkoxyl, and hydroxyalkyl;

Y 1 is H;

Y 2 is selected from the group consisting of H, —NH 2 , —SO 3 − , —(CH 2 ) t OH, —(CH 2 ) t NH 3 + X 2 − ; CH 3 CONH—, X 2 CH 2 CONH—, HO(CH 2 ) 2 —S—CH 2 CONH—, SuOCOCH 2 OCH 2 CON(CH 3 )—, —CH 2 —NH—C(═O)—O—(CH 3 ) 3 , —(CH 2 ) t —NH 2 + —(CH 2 ) s —SO 3 − , —(CH 2 ) t —NH—C(═O)—(CH 2 ) s —X 2 , a succinimidyl ester, a hydroxysuccinimide, a maleimide, a haloacetyl, a pyridyl disulfide, a hydrazine, an ethyldiethylamino propylcarbodiimide,

 or a protecting group, including t-butoxycarbonyl and carbobenzoxy;

and

wherein each p, r, s and t is independently an integer from 1 to 8; and Su is succinimidyl ester;

and salts thereof.

2. The dye of claim 1 , wherein Y 1 is selected from the group consisting of: —(CH 2 ) 2 OH, —CH 2 —NH 3 + X 2 − ; —CH 2 —NH 2 + —(CH 2 ) 3 —SO 3 − ; —CH 2 —NH—C(═O)—CH 2 —X 2 ; —CH 2 —NH—C(═O)—O—(CH 3 ) 3 ;

wherein X 2 is halogen selected from the group consisting of Cl and I.

3. A dye selected from

and salts thereof.

Assignments (1)
CONFIRMATORY LICENSE Recorded Oct 2, 2019
From: UNIVERSITY OF NORTH CAROLINA, CHAPEL HILL
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 050608/0987 →
Continuity (2)
Provisional Application 60936527 · Jun 21, 2007
Related Publication 20110046000A1 · Feb 24, 2011