CZh226
CZh226 is a selective PAK4 inhibitor with an IC50 of 0.0111 μM and a Ki of 0.009 μM. CZh226 functionally inhibits PAK4 activity and reduces the phosphorylation level of downstream signaling molecules. CZh226 inhibits the migration and invasion of tumor cells. CZh226 is applicable to lung cancer-related research.
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- No. CAS: 2196199-00-3
- Fòrmula: C20H22ClN7O
- Peso molecular:411.89
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Actividad biológica
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LIMK1 |
PAK4 |
MMP2 |
CZh226 (0.1-5.0 μM; 0-72 h) reduces the viability of human lung adenocarcinoma A549 cells, while exerts weak effects on PAK4-independent HEK-293 and NCI-H460 cells[1].
CZh226 (0.5-10 μM; 24-48 h) inhibits the migration and invasion of human lung adenocarcinoma cell line A549 in a dose-dependent manner[1].
CZh226 (0-10 μM; 24 h) inhibits the PAK4-dependent downstream signaling pathway in A549 cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 human lung adenocarcinoma cells
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Concentration:0 μM, 0.5 μM, 1 μM, 2 μM, 5 μM, 10 μM
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Incubation Time:24 h
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Result:Dose-dependently inhibited phosphorylation of PAK4 (Ser474), LIMK1 (Thr508), and cofilin (Ser3).
Reduced phosphorylation of GEF-H1 (Ser810) in a dose-dependent manner.
Reduced expression of MMP-2.
Unchanged the levels of PAK4, LIMK1, and cofilin.
| Species | Dose | Route | C0 | CL | Vss | T1/2 | AUC0-t | AUC0-∞ |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 2 mg/kg | i.v. | 736 ng/mL | 70.7 mL/min/kg | 6.43 L/kg | 1.46 h | 465 ng·h/mL | 472 ng·h/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2196199-00-3
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Peso molecular 411.89
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Fòrmula C20H22ClN7O
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SMILES
N(C=1C2=C(N=C(C(=O)N3C[C@@H](C)NCC3)N1)C=CC(Cl)=C2)C=4C=C(NN4)C5CC5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CZh226 Related Classifications
HY-111103 Related Classifications
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