Integrin

SR121566A is a non-peptide integrin antagonist targeting Glycoprotein IIb/IIIa (GP IIb-IIIa). This compound effectively inhibits human platelet aggregation induced by ADP, arachidonic acid, and collagen, with IC50 values of 46±7.5 nM, 56±6 nM, and 42±3 nM, respectively. SR121566A is valuable for research applications focused on thrombus formation and cardiovascular diseases.

SM6.1-azide is a ligand specifically targeting the αvβ6 integrin, featuring an azide group. This reactive moiety enables click chemistry with small molecules, peptides, or siRNA that possess DBCO or alkyne functionalities, facilitating efficient pulmonary-targeted delivery. This compound is valuable for research applications focused on integrin interactions and targeted therapeutics in respiratory conditions.

Tri-SM6.1 is a tridentate small-molecule ligand that specifically targets integrin αvβ6. This compound effectively binds to integrin αvβ6 on epithelial cells, facilitating the delivery of conjugated α-ENaC RNA interference agents. Its biological activity and targeting capability make it a valuable tool for research applications focused on epithelial cell signaling and RNAi-mediated gene regulation.

KAFDITYVRLKF is a selective integrin αvβ3 binder that exhibits competitive inhibitory activity. This compound is known to induce the production of matrix metalloproteinase-9 (MMP-9) and has been shown to block monocyte migration while promoting melanoma cell migration. Additionally, KAFDITYVRLKF demonstrates neuroprotective effects and enhances both motor and cognitive functions. Its applications are particularly relevant in research focused on melanoma and Parkinson's disease.

SU015 is an antagonist of the integrins αvβ3 and αvβ5, demonstrating comparable affinity for both targets with enhanced potency and specificity. This compound effectively inhibits αvβ3-mediated cell adhesion to fibrinogen and osteopontin, as well as αvβ5-mediated cell adhesion to vitronectin. Additionally, SU015 exhibits significant inhibitory effects on FGF2-induced angiogenesis in the chick embryo chorioallantoic membrane (CAM) model. Its properties allow for potential applications in tumor metastasis studies, and it features a linker arm suitable for radioisotope conjugation, serving as a target-specific radioreagent when labeled with isotopes such as 90Y or 177Lu.

3P-RGD2 is a dimeric cyclic RGD (Arg-Gly-Asp) peptide that selectively binds to integrin αvβ3. When radiolabeled with 99mTc, it functions as a specific radiotracer, facilitating single-photon emission computed tomography (SPECT) imaging of integrin αvβ3 expression. This compound is useful in researching angiogenesis, cancer diagnostics, and targeted therapy applications.