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A 286982
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
A 286982图片
CAS NO:280749-17-9
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
A 286982 是一种有效的变构 LFA-1/ICAM-1 相互作用抑制剂，在 LFA-1/ICAM-1 结合和 LFA-1 介导的细胞粘附试验中，IC50 分别为 44 nM 和 35 nM。
Cas No.280749-17-9
化学名(E)-1-(4-acetylpiperazin-1-yl)-3-[3-nitro-4-(2-propan-2-ylphenyl)sulfanylphenyl]prop-2-en-1-one
Canonical SMILESCC(C)C1=CC=CC=C1SC2=C(C=C(C=C2)C=CC(=O)N3CCN(CC3)C(=O)C)[N+](=O)[O-]
分子式C24H27N3O4S
分子量453.55
溶解度30mg/mL in DMSO, or in DMF
储存条件Store at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

A 286982 is a selective inhibitor of LFA-1/ICAM-1 binding and LFA-1 with IC50 value of 44 nM and 35 nM, respectively [1].

Lymphocyte function-associated antigen-1 (LFA-1) is a member of leukocyte intergrins family and involves in T cells binding to antigen presenting cells. Intracellular adhension molecule-1 (ICAM-1) is a type of intercellular adhesion molecule and plays a pivotal role in cell-cell interactions. LFA-1/ICAM-1 interaction plays an important role in the pathogenesis of inflammatory disease [2].

A 286982 is a potent LFA-1/ICAM-1 inhibitor and has a different effect on the binding of compound 2B. When tested with LFA-1/ICAM-1 binding assay and LFA-1-mediated cellular adhesion assays, A-286982 treatment for 28h exhibited inhibition on LFA-1/ICAM-1interaction [1]. Using the LFA-1/ICAM-1 ELISA assay, it was shown that A 286982 exhibited inhibition on the binding of ICAM-1-Ig to LFA-1 by reducing both ligands affinity and binding capacity [3].

References:
[1]. Liu, G., 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. 43(21): p. 4025-40.
[2]. Katakai, T., K. Habiro, and T. Kinashi, Dendritic cells regulate high-speed interstitial T cell migration in the lymph node via LFA-1/ICAM-1. J Immunol, 2013. 191(3): p. 1188-99.
[3]. Keating, S.M., 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. 15(2): p. 290-303.