TMPRSS6 inhibitor 8 (TMPRSS6-IN-8) is a highly potent (IC50=8.1 nM), peptidomimetic inhibitor of TMPRSS6 (matriptase-2).
TMPRSS6-IN-8 inhibits two closely related TTSPs (matriptase and hepsin, IC50 52 nM and 16 nM, respectively), weakly inhibits thrombin and factor Xa and has no inhibitory activity toward furin.
TMPRSS6-IN-8 forms a reversible covalent bond with TMPRSS6.
Inhibiting TMPRSS6 proteolytic activity prevents cleavage of hemojuvelin (HJV) in HeLa cells (IC50=267 nM).
TMPRSS6 inhibition increases hepcidin encoding gene (HAMP) expression in HepG2 cells and human primary hepatocytes.
