DKFZ-633
DKFZ-633 is a potent KLK6 inhibitor and KLK6-specific probe with an IC50 of 250 nM against human KLK6. DKFZ-633 covalently labels active KLK6 in a specific manner, and successfully pulls down and captures endogenous active KLK6 from cell-conditioned media. DKFZ-633 serves as a critical tool for investigating the function of KLK6 and its regulatory mechanisms in head and neck cancer.
For research use only. We do not sell to patients.
- CAS No.: 2244425-14-5
- Formula: C26H24N4O3
- Molecular Weight:440.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
DKFZ-633 (compound 44) (0.25 μM; 30 min) inhibits recombinant triple-mutant human KLK6, with an IC50 of 0.25 μM after 30 min of pre-incubation at room temperature[1].
DKFZ-633 (12-25 μM; 1 h; room temperature) pulls down active endogenous human KLK6 from FaDu cell-conditioned medium in a dose-dependent manner[1].
DKFZ-633 (50 μM; 1 h; room temperature) pulls down active endogenous human KLK6 from the conditioned media of various human cancer cell lines, including two cell-dependent glycoforms[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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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. 2244425-14-5
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Molecular Weight 440.50
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Formula C26H24N4O3
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SMILES
O=C(OCC(=O)NC=1C(=NN(C=2C=CC=CC2)C1C)C)CC=3C=4C=C(C#C)C=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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)