DKFZ-938
DKFZ-938 is a kallikrein-related peptidase 6 (KLK6) inhibitor, with an IC50 of 0.09 μM against human KLK6. DKFZ-938 binds to the catalytic serine residue in the active-site pocket of KLK6 and mimics the natural KLK6 substrate to inhibit the enzymatic activity of KLK6. DKFZ-938 can be conjugated to the non-canonical amino acid propargyllysine via copper-catalyzed azide-alkyne cycloaddition click chemistry. DKFZ-938 is used in research related to colorectal cancer and pancreatic cancer.
For research use only. We do not sell to patients.
- Formula: C35H41N9O8
- Molecular Weight:715.76
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
KLK6 0.09 μM (IC50) |
In Vitro
DKFZ-938 (0-3000 nM; 30 min) exhibits potent covalent inhibitory activity against purified KLK6 in a cell-free biochemical assay, with an IC50 of 0.09 μM and a kinact/Ki of 1030 M-1s-1 [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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Molecular Weight 715.76
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Formula C35H41N9O8
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SMILES
O=C(COC1=CC=C(N2C(C)=C(NC(COC(CC3=C(C)NC4=C3C=C(C#N)C=C4)=O)=O)C(C)=N2)C=C1)NCCOCCOCCOCCN=[N+]=[N-]
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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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EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
The EdU incorporation assay measures DNA synthesis by adding the thymidine analog 5-ethynyl-2′-deoxyuridine to cells or tissues, where it is incorporated into newly synthesized DNA during S phase. Incorporated EdU is detected by copper-catalyzed azide-alkyne cycloaddition, in which a fluorescent azide covalently reacts with the ethynyl group on EdU, allowing S-phase cells to be detected by fluorescence microscopy, flow cytometry, or high-content imaging. EdU detection does not require DNA denaturation or anti-BrdU antibody access, which preserves sample structure and improves compatibility with immunostaining and multiparameter cytometry compared with BrdU-based detection. EdU can be cytotoxic in a cell-type- and exposure-dependent manner, so pulse duration, concentration, and continuous-labeling designs should be validated for each cell type.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DKFZ-938 Related Classifications
HY-189205 Related Classifications
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