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Cat. No.: HY-124610

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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

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

DKFZ-633 Chemical Structure

CAS No.: 2244425-14-5

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Sample (0.1mg)

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(In Japan)

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

All Kallikrein Isoforms :

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.

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay^[1]

Cell Line:

FaDu head and neck squamous cell carcinoma cells
Concentration:

100, 300, 500 nM
Incubation Time:

48 h (daily treatment)
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

CAS No. 2244425-14-5
Molecular Weight 440.50
Formula C₂₆H₂₄N₄O₃
SMILES

O=C(OCC(=O)NC=1C(=NN(C=2C=CC=CC2)C1C)C)CC=3C=4C=C(C#C)C=CC4NC3C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. De Vita E, et al. Depsipeptides Featuring a Neutral P1 Are Potent Inhibitors of Kallikrein-Related Peptidase 6 with On-Target Cellular Activity. J Med Chem. 2018;61(19):8859-8874. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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