A 286982
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.
Physical Appearance | Yellow solid |
Storage | Store at RT |
M.Wt | 453.55 |
Cas No. | 280749-17-9 |
Formula | C24H27N3O4S |
Solubility | ≥51.2 mg/mL in DMSO; ≥25.55 mg/mL in EtOH; insoluble in H2O |
Chemical Name | (E)-1-(4-acetylpiperazin-1-yl)-3-[3-nitro-4-(2-propan-2-ylphenyl)sulfanylphenyl]prop-2-en-1-one |
SDF | Download SDF |
Canonical SMILES | CC(C)C1=CC=CC=C1SC2=C(C=C(C=C2)C=CC(=O)N3CCN(CC3)C(=O)C)[N+](=O)[O-] |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
- View current batch:
Chemical structure
