A 286982 |
Catalog No.GC15192
One-Click Copy Product Info
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A 286982 is a potent, nonpeptide inhibitors of leukocyte function-associated antigen-1/ intracellular adhesion molecule-1 (LFA-1/ICAM-1) interaction, with IC50 values of 44 and 35nM in LFA-1/ICAM-1 binding assay and LFA-1-mediated cellular adhesion assay, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 280749-17-9
Sample solution is provided at 25 µL, 10mM.
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A 286982 is a potent, nonpeptide inhibitors of leukocyte function-associated antigen-1/ intracellular adhesion molecule-1 (LFA-1/ICAM-1) interaction, with IC50 values of 44 and 35nM in LFA-1/ICAM-1 binding assay and LFA-1-mediated cellular adhesion assay, respectively[1]. The interaction of LFA-1 with ICAM-1 is critical for adhesion and recruitment of immune cells to antigen-presenting cells and for cell killing by NK cells[2].
In vitro, treatment with A-286982 at 22–176nM for 49h dose-dependently reduced Interferon-Stimulated Gene 15 (ISG15)-induced IFN-γ secretion in NK-92 cells[2]. Treatment with 88nM A 286982 for 24-48h inhibited C-C motif chemokine ligand 18 (CCL18) secretion in macrophages and blocked ISG15-induced activation of the Proto-oncogene tyrosine-protein kinase Src (SRC) signaling pathway[3]. Treatment with 100nM A 286982 for 12-24h significantly reduced the expression of the cytotoxic marker GZMB and the activation marker CD69 in CD8⁺T cells isolated from peripheral blood mononuclear cells (PBMCs) co-cultured with A549 cells[4].
References:
[1] Liu G, Link JT, Pei Z, 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):4025-4040.
[2] Swaim CD, Scott AF, Canadeo LA, Huibregtse JM. Extracellular ISG15 Signals Cytokine Secretion through the LFA-1 Integrin Receptor. Mol Cell. 2017;68(3):581-590.e5.
[3] Chen RH, Xiao ZW, Yan XQ, et al. Tumor Cell-Secreted ISG15 Promotes Tumor Cell Migration and Immune Suppression by Inducing the Macrophage M2-Like Phenotype. Front Immunol. 2020;11:594775.
[4] Wang CL, Ho AS, Chang CC, et al. Radiotherapy enhances CXCR3highCD8+ T cell activation through inducing IFNγ-mediated CXCL10 and ICAM-1 expression in lung cancer cells. Cancer Immunol Immunother. 2023;72(6):1865-1880.
| Cell experiment [1]: | |
Cell lines | NK-92 |
Preparation Method | MHM24 and TS1/22 antibodies, a small molecule inhibitor of LFA-1 (A-286982), or an antibody against the transferrin receptor (G1/221/12) was pre-incubated with NK-92 cells for 1h prior to the addition of IL-12 and ISG15 for 48h, followed by an IFN-g ELISA of the cell culture supernatants. |
Reaction Conditions | 22, 44, 88 and 176nM; 49h |
Applications | Increasing amounts of either of the MHM24, TS1/22 antibodies or A-286982 reduced the ability of ISG15 to stimulate IFN-g secretion from NK-92 cells, while a control antibody against the transferrin receptor did not. |
References: | |
| Cas No. | 280749-17-9 | SDF | |
| Chemical Name | (E)-1-(4-acetylpiperazin-1-yl)-3-[3-nitro-4-(2-propan-2-ylphenyl)sulfanylphenyl]prop-2-en-1-one | ||
| Canonical SMILES | CC(C)C1=CC=CC=C1SC2=C(C=C(C=C2)C=CC(=O)N3CCN(CC3)C(=O)C)[N+](=O)[O-] | ||
| Formula | C24H27N3O4S | M.Wt | 453.55 |
| Solubility | 30mg/mL in DMSO, or in DMF | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2048 mL | 11.0241 mL | 22.0483 mL |
| 5 mM | 441 μL | 2.2048 mL | 4.4097 mL |
| 10 mM | 220.5 μL | 1.1024 mL | 2.2048 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)