CU-3
CU-3 is a DGKα inhibitor with an IC50 of 0.6 μM. CU-3 competitively reduces DGKα’s affinity for ATP via binding to the enzyme’s catalytic region. CU-3 induces apoptosis in cancer cells. CU-3 promotes T-cell activation and enhances IL-2 production. CU-3 can be used for the research of hepatocellular carcinoma and cervical cancer.
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- CAS No.: 2983265-35-4
- Formule: C16H12N2O4S3
- Masse moléculaire:392.47
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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IL-2 |
Caspase 3 |
Caspase-7 |
CU-3 potently and selectively inhibits purified pig DGK α activity with an IC50 of 0.6 μM by targeting the catalytic domain and competitively interfering with ATP binding[1].
CU-3 (2 μM; 24 h) inhibits intracellular DGK α activity in COS-7 cells, reducing phosphatidic acid production induced by overexpressed constitutively active DGK α[1].
CU-3 (5 μM; 24 h) induces apoptosis in HepG2 and HeLa cancer cells, as measured by increased caspase-3/7 activity, without causing nonspecific toxicity to noncancerous COS-7 cells[1].
CU-3 (5 μM; 5 min) enhances Con A-induced IL-2 mRNA expression in Jurkat T cells by inhibiting DGK α, promoting T-cell activation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 human hepatocellular carcinoma cells, HeLa human cervical cancer cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Increased caspase-3/7 activity by ~50% in HepG2 cells.
Increased caspase-3/7 activity by ~24% in HeLa cells.
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Cell Line:Jurkat human T cells
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Concentration:5 μM
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Incubation Time:5 min
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Result:Enhanced Con A-induced IL-2 mRNA production by ~50% in Jurkat T cells.
Exhibited an effect comparable to that of DGK α siRNA knockdown.
Did not further increase IL-2 production when combined with DGK α siRNA.
Chemical Information
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CAS No. 2983265-35-4
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Masse moléculaire 392.47
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Formule C16H12N2O4S3
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SMILES
O=C1N(C(S/C1=C\C=C\C2=CC=CO2)=S)NS(=O)(C3=CC=CC=C3)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CU-3 Related Classifications
HY-121638 Related Classifications
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