A 286982

Names

[ Name ]:
A 286982

[Synonym ]:
unii-5i8wfs075a

Biological Activity

[Description]:

A-286982 is a potent and allosteric LFA-1/ICAM-1 interaction inhibitor with IC50s of 44 nM and 35 nM in an LFA-1/ICAM-1 binding and LFA-1-mediated cellular adhesion assay, respectively[1][2].

[Related Catalog]:

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Cytoskeleton >> Integrin

[Target]

IC50: 44 nM (LFA-1/ICAM-1 interaction in an LFA-1/ICAM-1 binding assay) and 35 nM (LFA-1/ICAM-1 interaction in LFA-1-mediated cellular adhesion assay)[1]

[In Vitro]

A-286982 binds to the I domain allosteric site (IDAS). The allosteric ICAM inhibition such as this would be expected to exhibit the unsurmountable competition we have observed for A-286982 as a result of the passage of this allostery through the A-286982 binding site in its transmission from the β subunit I-like domain to the α subunit ICAM binding site[2].

[References]

[1]. G Liu, et al. Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 1. Identification of an additional binding pocket based on an anilino diaryl sulfide lead. J Med Chem. 2000 Oct 19;43(21):4025-40.

[2]. Susan M Keating, et al. Competition between intercellular adhesion molecule-1 and a small-molecule antagonist for a common binding site on the alphal subunit of lymphocyte function-associated antigen-1. Protein Sci. 2006 Feb;15(2):290-303.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₄H₂₇N₃O₄S

[ Molecular Weight ]:
453.55400

[ Exact Mass ]:
453.17200

[ PSA ]:
111.74000

[ LogP ]:
4.97230

[ Storage condition ]:
-20°C

MSDS

Click to get detail MSDS

Safety Information

[ RIDADR ]:
NONH for all modes of transport