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。
| 生物活性 | PAK4-IN-2 is a highly potentPAK4inhibitor withIC50value of 2.7 nM. PAK4-IN-2 can arrest MV4-11 cells at G0/G1 phase and induce cellapoptosis. PAK4-IN-2 can be used for researchingcancer[1]. |
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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].
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. |
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| 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. |
