DKFZ-251 is an inhibitor of the kininogenase-related peptidase KLK6, demonstrating an IC50 of 0.47 μM. It also shows inhibitory activity against KLK5 and KLK7 with IC50 values of 1.1 nM and 73 nM, respectively. This compound functions by transiently acylating the catalytic serine of KLK6, resulting in a stable acyl-enzyme complex that effectively inhibits enzymatic activity. DKFZ-251 serves as a phenotypic modulator, impacting cell proliferation and regulating epithelial-mesenchymal transition (EMT), making it a valuable tool in studies related to head and neck cancer.
DKFZ-251 is an inhibitor of the kininogenase-related peptidase KLK6, demonstrating an IC50 of 0.47 μM. It also shows inhibitory activity against KLK5 and KLK7 with IC50 values of 1.1 nM and 73 nM, respectively. This compound functions by transiently acylating the catalytic serine of KLK6, resulting in a stable acyl-enzyme complex that effectively inhibits enzymatic activity. DKFZ-251 serves as a phenotypic modulator, impacting cell proliferation and regulating epithelial-mesenchymal transition (EMT), making it a valuable tool in studies related to head and neck cancer.
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