A286982|CAS 280749-17-9|DC Chemicals

Cas No.:	280749-17-9
Chemical Name:	A 286982
Synonyms:	A 286982;A-286982;(E)-1-(4-acetylpiperazin-1-yl)-3-[3-nitro-4-(2-propan-2-ylphenyl)sulfanylphenyl]prop-2-en-1-one;(2E)-1-(4-Acetyl-1-piperazinyl)-3-[4-[[2-(1-methylethyl)phenyl]thio]-3-nitrophenyl]-2-propen-1-one
SMILES:	CC(N1CCN(C(/C=C/C2C=CC(SC3=CC=CC=C3C(C)C)=C([N+]([O-])=O)C=2)=O)CC1)=O
Formula:	C₂₄H₂₇N₃O₄S
M.Wt:	453.553884744644
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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].
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

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