DKFZ-251
DKFZ-251 is a kininogenase-related peptidase KLK6 inhibitor (IC50=0.47 μM), and also exhibits certain inhibitory activity against KLK5 and KLK7 (IC50 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.
For research use only. We do not sell to patients.
- CAS No.: 2222059-70-1
- Formula: C24H24N4O3
- Molecular Weight:416.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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KLK5 1.1 nM (IC50) |
DKFZ-251 (compound 11) (200 μM; 1 h) forms a long-lived acyl-enzyme complex with recombinant triple-mutant KLK6, with a half-life of 6.43 h[1].
DKFZ-251 (100-500 nM; 48 h) induces a dose-dependent increase in BrdU incorporation and causes phenotypic changes in FaDu cells, which is consistent with the targeted inhibition of endogenous KLK6[1].
DKFZ-251 (2.5-10 μM; 30 min) specifically inhibits the labeling of recombinant KLK6 by the activity-based probe DKFZ-633[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:FaDu head and neck squamous cell carcinoma cells
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Concentration:100, 300, 500 nM
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Incubation Time:48 h (daily treatment)
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Result:Increased BrdU-positive FaDu cells in a dose-dependent manner: ~45% (100 nM), ~50% (300 nM), ~60% (500 nM), compared to ~45% in vehicle control.
Induced a dose-dependent phenotypic change in FaDu cells, mimicking the effect of KLK6 shRNA silencing.
Chemical Information
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CAS No. 2222059-70-1
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Molecular Weight 416.48
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Formula C24H24N4O3
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SMILES
O=C(OCC(=O)NC=1C(=NN(C=2C=CC=CC2)C1C)C)CC=3C=4C=CC=CC4NC3C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DKFZ-251 Related Classifications
HY-124714 Related Classifications
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