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.
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- 화학식: C35H41N9O8
- 분자량:715.76
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
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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분자량 715.76
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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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.
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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.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)