2. Cell Cycle/DNA Damage Cytoskeleton Metabolic Enzyme/Protease
  3. PAK LIM Kinase (LIMK) MMP
  4. 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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CZh226

CZh226 Chemical Structure

CAS No. : 2196199-00-3

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CZh226 Related Antibodies

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Description

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[1].

IC50 & Target[1]

LIMK1

 

PAK4

 

MMP2

 

In Vitro

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.

CZh226 Related Antibodies

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.
Parmacokinetics
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
In Vivo

CZh226 (2 mg/kg; intravenous administration; single dose) exhibits moderate pharmacokinetic properties in male Sprague-Dawley rats, with a half-life of 1.46 h and an AUC0-∞ of 472 ng·h/mL[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

411.89

Formula

C20H22ClN7O
CAS No.
SMILES

N(C=1C2=C(N=C(C(=O)N3C[C@@H](C)NCC3)N1)C=CC(Cl)=C2)C=4C=C(NN4)C5CC5
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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CZh226 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CZh2262196199-00-3CZh 226CZh-226PAKLIM Kinase (LIMK)MMPp21 activated kinasesLIMKsMatrix metalloproteinasesFLT3A549 human lung adenocarcinoma cellsPAK5PAK4PAK1LIMK1NCI-H460cofilinlung cancerHEK-293Inhibitorinhibitorinhibit

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