1. Immunology/Inflammation
  2. Kallikrein
  3. 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.

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DKFZ-633

DKFZ-633 Chemical Structure

CAS No. : 2244425-14-5

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Description

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[1].

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.
Molecular Weight

440.50

Formula

C26H24N4O3

CAS No.
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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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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DKFZ-633
Cat. No.:
HY-124610
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