Integrin Agonist

Pyrintegrin is an β1-integrin agonist and a 2,4-disubstituted pyrimidine that promotes embryonic stem cells survival. Pyrintegrin enhances cell-extracellular matrix (ECM) adhesion-mediated integrin signaling. Pyrintegrin can be used as a podocyte-protective agent and has robustly adipogenic.

Leukadherin-1, a specific agonist of the leukocyte surface integrin CD11b/CD18, increases CD11b/CD18-dependent cell adhesion to fibrinogen with an EC₅₀ of 4 μM. Leukadherin-1 enhances leukocyte adhesion to ligands (such as ICAM-1) and vascular endothelium and thus reduces leukocyte transendothelial migration and influx to the injury sites. Leukadherin-1 suppresses innate inflammatory signaling.

Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC₅₀ of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC₅₀ of 12.9 nM.

α5β1 integrin agonist-1 is an α5β1 integrin agonist, with an EC₅₀ of 1.5 nM. α5β1 integrin agonist-1 inhabits α4β1 integrin (IC₅₀ = 2.99 μM) in Jurkat/VCAM-1 adhesion assayα5β1 integrin agonist-1 induces concentration-dependent apoptosis and activates the caspase 3/7 pathway in α5β1 integrin-expressing K562 cancer cells. α5β1 integrin agonist-1 can be used for the study of cancer.

FZ1 peptide is a cyclic heptapeptide and also an integrin αvβ3 agonist. FZ1 peptide activates the FAK/PI3K-AKT/ERK pathway and upregulates VEGFC to promote angiogenesis. FZ1 peptide exhibits antibacterial activity in extracts of HA-c-FZ1 hydrogel; it inhibits LPS-induced proinflammatory cytokine secretion in RAW264.7 macrophages; it reduces H₂O₂-induced ROS levels; it increases the healing rate of scratch wounds. FZ1 peptide can be used in studies related to diabetic skin wounds.

LT25 (compound 17) is a agonist of α5β1 integrin with EC₅₀ value of 9.9 nM.

α5β1 integrin agonist-2 (Compound 2) is a selective α5β1 integrin agonist (EC₅₀ = 45.98 nM). α5β1 integrin agonist-2 induces integrin activation. α5β1 integrin agonist-2 is applicable to the research of leukemia.

αMβ2 integrin agonist-1 (Compound 8) is a highly selective αMβ2 integrin agonist with anti-inflammatory activity (EC₅₀=1.4 nM). αMβ2 integrin agonist-1 activates integrin-mediated cell adhesion and JNK/ERK signaling. αMβ2 integrin agonist-1 induces tumor-associated macrophage repolarization and enhances antitumor T-cell immune responses. αMβ2 integrin agonist-1 is promising for research of cancers and chronic inflammatory diseases (e.g., pancreatic cancer, rheumatoid arthritis).

Leukadherin-1 (Standard) is the analytical standard of Leukadherin-1. This product is intended for research and analytical applications. Leukadherin-1, a specific agonist of the leukocyte surface integrin CD11b/CD18, increases CD11b/CD18-dependent cell adhesion to fibrinogen with an EC50 of 4 μM. Leukadherin-1 enhances leukocyte adhesion to ligands (such as ICAM-1) and vascular endothelium and thus reduces leukocyte transendothelial migration and influx to the injury sites. Leukadherin-1 suppresses innate inflammatory signaling.