| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C20H22ClN7O |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
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Compound Overview
CZh226 is a selective inhibitor of PAK4, with an IC50 of 0.0111 μM and a Ki of 0.009 μM. It functionally suppresses PAK4 activity, lowering phosphorylation of downstream signaling molecules, and inhibits the migration and invasion of tumor cells. The compound is applicable to lung cancer-related research[1]. It has the molecular formula C20H22ClN7O (MW 411.89).
Physical & Chemical Properties
| CAS Number | 2196199-00-3 |
|---|---|
| Molecular Formula | C20H22ClN7O |
| Molecular Weight | 411.89 g/mol |
| SMILES | N(C=1C2=C(N=C(C(=O)N3C[C@@H](C)NCC3)N1)C=CC(Cl)=C2)C=4C=C(NN4)C5CC5 |
| Target | LIMK1, PAK4, MMP2 |
| Signaling Pathway | Cell Cycle/DNA Damage; Cytoskeleton; Metabolic Enzyme/Protease |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
CZh226 (0.1-5.0 μM; 0-72 h) lowers the viability of human lung adenocarcinoma A549 cells whereas effects on PAK4-independent HEK-293 and NCI-H460 cells are weak[1]. In the human lung adenocarcinoma cell line A549, CZh226 (0.5-10 μM; 24-48 h) dose-dependently inhibits migration and invasion[1]. In A549 cells, CZh226 (0-10 μM; 24 h) dose-dependently inhibits the PAK4-dependent downstream signaling pathway[1].
Western Blot Analysis[1]
| Cell Line | A549 human lung adenocarcinoma cells |
|---|---|
| Concentration | 0 μM, 0.5 μM, 1 μM, 2 μM, 5 μM, 10 μM |
| Incubation Time | 24 h |
| 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. |
In Vivo
In male Sprague-Dawley rats, a single intravenous dose of CZh226 (2 mg/kg) gives moderate pharmacokinetic properties: half-life 1.46 h, AUC0-∞ 472 ng·h/mL[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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