MAS9 is a specific small molecule inhibitor targeting the C-type lectin-like receptor-2 (CLEC-2)-podoplanin interaction with IC50 of 4.5 uM, inhibits CLEC-2-mediated platelet aggregation.
MAS9 (20-30 uM) significantly inhibits platelet aggregation to both CLEC-2 agonists rhodocytin and hemin.
MAS9 displaysinhibition for CLEC-2-mediated aggregation over other platelet receptors, GPVI, thromboxane prostanoid (TP) receptor, and proteinase activated receptors (PAR1 and PAR4).
MAS9 also displays selective inhibition of CLEC-2-mediated tyrosine kinase signalling. CLEC-2 and GPVI share similar proximal signalling events, including the phosphorylation and activation of the kinase Syk.
MAS9 has no inhibitory effect either on 0.3 μg·ml−1 CRP-XL or 0.1 U·ml−1 thrombin-mediated platelet aggregation, also shows no inhibitory effect on lower concentrations of thrombin or U46619-mediated aggregation.
MAS9 inhibits CLEC-2-dependent platelet adhesion but inhibits platelet spreading to all substrates.
MAS9 (10-30 uM) inhibits platelet adhesion to human dermal lymphatic endothelial cells.