Leukadherin-1

Leukadherin-1 (LA1) is a small molecule agonist that enhances CD11b/CD18-dependent cell adhesion to its ligand ICAM-1(an agonist for the complement receptor 3 (CD11b/CD18)).

Leukadherin-1 Chemical Structure

Leukadherin-1 Chemical Structure

CAS: 344897-95-6

Selleck's Leukadherin-1 has been cited by 5 publications

Purity & Quality Control

Batch: S830601 DMSO] 5 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.86%
99.86

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Biological Activity

Description Leukadherin-1 (LA1) is a small molecule agonist that enhances CD11b/CD18-dependent cell adhesion to its ligand ICAM-1(an agonist for the complement receptor 3 (CD11b/CD18)).
Targets
CD11b/CD18 [3]
In vitro
In vitro Leukadherin-1 pretreatment reduces secretion of interferon (IFN)-γ, tumour necrosis factor (TNF) and macrophage inflammatory protein (MIP)-1β by monokine-stimulated NK cells. It also reduces secretion of IL-1β, IL-6 and TNF by Toll-like receptor (TLR)-2 and TLR-7/8-stimulated monocytes. Leukadherin-1 modulates NK cell cytokine secretion and does not modulate Syk activation in NK cells[1]. LA1 increases CD11b/CD18-dependent cell adhesion to fibrinogen with 50% effective concentration (EC50, the effective concentration for a 50% increase in adhesion) values of 4 μM[3].
Cell Research Cell lines NK cells
Concentrations 7.5 μM
Incubation Time 30-45 min
Method

NK cell stimuli (where used) were added as follows: (1) Syk inhibitor (1 μM), (2) Leukadherin-1 or dimethylsulphoxide (DMSO) (vector control) (7.5 μM). Shown to induce ∼82% of maximum response with negligible off-target effect, (3) anti-CD210 or isotype control (5 µg/ml), (4) 30-45 min after Leukadherin‐1 NK cells were stimulated with combinations of IL-12 (10 ng/ml), IL-15 (30 ng/ml) or IL-18 (10 ng/ml): either IL-12 + IL-15 or IL-12 + IL-18. Monocytes were stimulated using pam3csk4 (TLR-2 agonist, 300 ng/ml) or R848 (TLR-7/8 agonist, 2 µg/ml). Supernatants were stored at −80ºC for < 1 month before quantification. To exclude non-specific Leukadherin-1-mediated cytotoxicity, cell viability is assessed at 24 h using the CellTitre-Glo reagent.

In Vivo
In vivo Leukadherin-1 has potent anti-inflammatory effects in a range of animal models, including an autoimmune nephritis model, without obvious short-term side effects[1]. Leukadherin-1 (LA1) increases leukocyte adhesion, preventing their transmigration and tissue recruitment in vivo. LA1 treatment reduces interstitial leukocyte infiltration in the allograft, reduces neointimal hyperplasia and glomerular damage, and prolongs graft survival from 48.5% (CsA only) to 100% (CsA and LA1) on day 60 in a mouse model of fully MHC-mismatched orthotopic kidney transplantation[2].
Animal Research Animal Models Male C57BL/6J (H-2b) and Balb/cJ (H-2d) mice
Dosages 1 mg/kg or 2.5 mg/kg
Administration i.v or i.p

Chemical Information & Solubility

Molecular Weight 421.49 Formula

C22H15NO4S2

CAS No. 344897-95-6 SDF Download Leukadherin-1 SDF
Smiles C1=CC=C(C=C1)CN2C(=O)C(=CC3=CC=C(O3)C4=CC=C(C=C4)C(=O)O)SC2=S
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 5 mg/mL ( (11.86 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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