SPU-106
SPU-106 is a p21 activated kinase 4 (PAK4) inhibitor with a target IC50 of 21.36 μM. SPU-106 selectively binds to the C-terminal kinase domain of PAK4 to inhibit its kinase activity. SPU-106 inhibits the PAK4/LIMK1/cofilin and PAK4/SCG10 signaling pathways. SPU-106 inhibits invasion of gastric cancer cells and lacks cytotoxicity against cancer cells. SPU-106 can be used for the research of gastric cancer.
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- CAS No.: 713080-84-3
- Formule: C22H17N3O3S
- Masse moléculaire:403.45
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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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PAK4 21.36 μM (IC50) |
SPU-106 (0-80 μM; 24 h) does not exhibit cytotoxicity against human gastric cancer SGC7901 and MKN-1 cells at concentrations up to 80 μM after 24 h of incubation[1].
SPU-106 (20-40 μM; 72 h) does not alter cell cycle dynamics in human gastric cancer SGC7901 cells at concentrations up to 40 μM after 72 h of incubation[1].
SPU-106 (20-40 μM; 18 h) dose-dependently inhibits the invasive potential of human gastric cancer SGC7901 cells, with significant inhibition observed at 20 μM and further inhibition at 40 μM after 18 h of incubation[1].
SPU-106 (0-80 μM; 0-24 h) dose-dependently inhibits the PAK4/LIMK1/cofilin and PAK4/SCG10 signaling pathways in human gastric cancer SGC7901 and BCG823 cells by reducing phosphorylation of PAK4 and its downstream targets, while leaving upstream c-Met activity unaffected[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human gastric cancer SGC7901 and MKN-1 cells
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Concentration:0-80 μM
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Incubation Time:24 h
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Result:Did not reduce cell viability in either SGC7901 or MKN-1 cells at concentrations up to 80 μM.
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Cell Line:human gastric cancer SGC7901 cells
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Concentration:20-40 μM
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Incubation Time:72 h
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Result:Did not cause significant changes in the cell cycle distribution of SGC7901 cells at concentrations up to 40 μM.
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Cell Line:human gastric cancer SGC7901 cells
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Concentration:20-40 μM
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Incubation Time:18 h
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Result:Reduced the invasion rate of SGC7901 cells to less than half of the control group at 20 μM.
Further reduced invasion of SGC7901 cells at 40 μM, demonstrating a dose-dependent inhibitory effect.
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Cell Line:human gastric cancer SGC7901 and BCG823 cells; SGC7901 cells transiently transfected with Flag-PAK4
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Concentration:20-80 μM (24 h incubation in SGC7901 cells); 5-20 μM (signaling pathway analysis); 20 μM (time-dependent assays); 0-40 μM (dose-dependent SCG10 phosphorylation assays)
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Incubation Time:24 h (SGC7901 and BCG823 cells); 0-24 h (time-dependent assays)
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Result:Dose-dependently reduced phosphorylated PAK4, phosphorylated LIMK1, and phosphorylated cofilin levels in SGC7901 cells, without affecting total PAK4, total LIMK1, total cofilin, or c-Met levels.
Time-dependently and dose-dependently inhibited phosphorylation of SCG10 in SGC7901 cells transfected with Flag-PAK4.
Dose-dependently reduced phosphorylated PAK4 and phosphorylated SCG10 levels in both SGC7901 and BCG823 cells, with no effect on c-Met phosphorylation.
Chemical Information
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CAS No. 713080-84-3
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Masse moléculaire 403.45
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Formule C22H17N3O3S
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SMILES
O=C1C=C(N=C(N1C2=CC=CC=C2)SCC(NC3=CC4=C(C=CC=C4)C=C3)=O)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)
SPU-106 Related Classifications
HY-183941 Related Classifications
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