PAK4-IN-2

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PAK4-IN-2 

PAK4-IN-2 是一种高效的 PAK4 抑制剂，IC50 为 2.7 nM。PAK4-IN-2 能将 MV4-11 细胞周期阻滞在 G0/G1 期，诱导细胞凋亡 (apoptosis)。PAK4-IN-2 可用于癌症研究。

PAK4-IN-2

PAK4-IN-2 Chemical Structure

CAS No. : 2488706-33-6

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生物活性

PAK4-IN-2 is a highly potent PAK4 inhibitor with IC50 value of 2.7 nM. PAK4-IN-2 can arrest MV4-11 cells at G0/G1 phase and induce cell apoptosis. PAK4-IN-2 can be used for researching cancer[1].

IC50 & Target

PAK3

2.7 nM (IC50)

体外研究
(In Vitro)

PAK4-IN-2 (compound 5n) (0-10 μM; 72 hours) exhibits cell growth inhibition potency in hematoma tumor MV4-11 and solid tumor cell line MDA-MB-231, shows less sensitivity in normal human renal epithelial cell 239 T cell[1].
PAK4-IN-2 (5-50 nM; 48 hours) causes a majority of cells in G0/G1 phase with decreasing S-phase populations[1].
PAK4-IN-2 (10-250 nM; 48 hours) induces apoptosis in a dose-dependent manner[1].
PAK4-IN-2 (50-800 nM; 24 hours) markedly reduces the expression levels of p-PAK4(Ser474) in concentration dependently[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: MV4-11, MDA-MB-231 and 293T[1]
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Exhibited significant cell growth inhibition potency in hematoma tumor MV4-11 (IC50 = 7.8 ± 2.8 nM), and moderate potent anti-proliferative effect in solid tumor cell line MDA-MB-231 (IC50 = 825 ± 106 nM), less sensitivity in normal human renal epithelial cell 239 T cell (IC50 > 10000 nM).

Cell Cycle Analysis

Cell Line: MV4-11[1]
Concentration: 5, 10 and 50 nM
Incubation Time: 48 hours
Result: Caused a majority of cells in G0/G1 phase with decreasing S-phase populations.

Apoptosis Analysis

Cell Line: MV4-11[1]
Concentration: 10, 50 and 250 nM
Incubation Time: 48 hours
Result: Induced apoptosis in a dose-dependent manner.

Western Blot Analysis

Cell Line: MV4-11[1]
Concentration: 50, 200 and 800 nM
Incubation Time: 24 hours
Result: Markedly reduced the expression levels of p-PAK4(Ser474) in concentration dependently.

分子量

356.85

Formula

C18H21ClN6
CAS 号

2488706-33-6
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.
参考文献

  • [1]. Wang C, Xia J, Lei Y, et al. Synthesis and biological evaluation of 7H-pyrrolo [2,3-d] pyrimidine derivatives as potential p21-activated kinase 4 (PAK4) inhibitors. Bioorg Med Chem. 2022;60:116700.

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