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

CZh226 是一种选择性 PAK4 抑制剂，IC50 为 0.0111 μM，Ki 为 0.009 μM。CZh226 可在功能上抑制 PAK4 活性，降低下游信号分子的磷酸化水平。CZh226 可抑制肿瘤细胞的迁移与侵袭。CZh226 可用于肺癌相关研究。

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CZh226

CZh226 Chemical Structure

CAS No. : 2196199-00-3

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Other Forms of CZh226:

CZh226 相关抗体

Top Publications Citing Use of Products

查看 PAK 亚型特异性产品:

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PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

查看 LIM Kinase (LIMK) 亚型特异性产品:

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LIMK1 LIMK2

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

CZh226 (0.1-5.0 μM; 0-72 h) 可降低人肺腺癌细胞 A549 的活力，而对非 PAK4 依赖的 HEK-293 细胞和 NCI-H460 细胞的作用较弱[1]。
CZh226 (0.5-10 μM; 24-48 h) 可呈剂量依赖性地抑制人肺腺癌细胞 A549 的迁移与侵袭[1]。
CZh226 (0-10 μM; 24 h) 以剂量依赖方式抑制 A549 细胞中 PAK4 依赖性下游信号通路[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CZh226 相关抗体:

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.
药代动力学
(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
体内研究
(In Vivo)

CZh226 (2 mg/kg；静脉注射；单次给药) 在雄性 Sprague-Dawley 大鼠后，表现出中等药代动力学特性，其半衰期为 1.46 h，AUC0-∞ 为 472 ng·h/mL[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

411.89

Formula

C20H22ClN7O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CZh226 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

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

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