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Art. -Nr.: HY-124714

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DKFZ-251

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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.

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Reinheit: 95.93%
CAS. Nr.: 2222059-70-1
Formel: C₂₄H₂₄N₄O₃
Molecular Weight:416.48

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

DKFZ-251 Chemical Structure

CAS. Nr.: 2222059-70-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

KLK5

1.1 nM (IC₅₀)

Alle Kallikrein Isoform-spezifische Produkte anzeigen :

In Vitro

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.

Cell Proliferation 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. Nr. 2222059-70-1
Appearance Solid
Molecular Weight 416.48
Formel C₂₄H₂₄N₄O₃
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

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DKFZ-251

Alle Kallikrein Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

DKFZ-251 Related Classifications

HY-124714 Related Classifications