Product Data Sheet

DKFZ-251

Catalog No. A64989

main product photo
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.
Chemical Information
Catalog NumA64989
M. Wt416.48
FormulaC24H24N4O3
Purity>98%
Storageat -20 °C 3 years (powder form); at -20 °C 6 months (Solution base)
CAS No.2222059-70-1
Synonyms
SMILESO=C(OCC(=O)NC=1C(=NN(C=2C=CC=CC2)C1C)C)CC=3C=4C=CC=CC4NC3C
Biological Activity
DescriptionDKFZ-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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