DKFZ-251 is a kininogenase-related peptidase KLK6 inhibitor ( IC 50 =0.47 μM), and also exhibits certain inhibitory activity against KLK5 and KLK7 ( IC 50 values are 1.1 nM and 73 nM, respectively). DKFZ-251 transiently acylates the catalytic serine of KLK6 to form a long-lived acyl-enzyme complex that inhibits enzyme function. DKFZ-251 is a phenotypic modulator that alters cell proliferation capacity and regulates epithelial-mesenchymal transition (EMT). DKFZ-251 can be used in research related to head and neck cancer .
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