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  3. 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.

For research use only. We do not sell to patients.

SPU-106

SPU-106 Chemical Structure

CAS No. : 713080-84-3

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Description

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[1].

IC50 & Target[1]

PAK4

21.36 μM (IC50)

In Vitro

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.

Cell Cytotoxicity Assay[1]

Cell Line: human gastric cancer SGC7901 and MKN-1 cells
Concentration: 0-80 μM
Incubation Time: 24 h
Result: Did not reduce cell viability in either SGC7901 or MKN-1 cells at concentrations up to 80 μM.

Cell Cycle Analysis[1]

Cell Line: human gastric cancer SGC7901 cells
Concentration: 20-40 μM
Incubation Time: 72 h
Result: Did not cause significant changes in the cell cycle distribution of SGC7901 cells at concentrations up to 40 μM.

Cell Invasion Assay[1]

Cell Line: human gastric cancer SGC7901 cells
Concentration: 20-40 μM
Incubation Time: 18 h
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.

Western Blot Analysis[1]

Cell Line: human gastric cancer SGC7901 and BCG823 cells; SGC7901 cells transiently transfected with Flag-PAK4
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)
Incubation Time: 24 h (SGC7901 and BCG823 cells); 0-24 h (time-dependent assays)
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.
Molecular Weight

403.45

Formula

C22H17N3O3S

CAS No.
SMILES

O=C1C=C(N=C(N1C2=CC=CC=C2)SCC(NC3=CC4=C(C=CC=C4)C=C3)=O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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SPU-106
Cat. No.:
HY-183941
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