ZMF-10 是一种高效的PAK1抑制剂，对 PAK1、PAK2 和 PAK3 的IC50分别为 174 nM、1.038 μM 和 1.372 μM。ZMF-10 可抑制 PAK1 活性，影响 MDA-MB-231 细胞中 PAK1 调控的细胞凋亡 (apoptosis)、内质网应激和迁移。ZMF-10 可用于抗癌研究。
| 生物活性 | ZMF-10 is a highly potentPAK1inhibitor, withIC50s of 174 nM, 1.038 μM and 1.372 μM forPAK1,PAK2andPAK3, respectively. ZMF-10 can inhibitPAK1activity to affect PAK1-regulatedapoptosis, ER-Stress and migration in MDA-MB-231 cells. ZMF-10 can be used for researching anticancer[1]. |
| IC50& Target[1] | PAK1 174 nM (IC50) | PAK2 1.038 μM (IC50) | PAK3 1.372 μM (IC50) |
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体外研究
(In Vitro) | ZMF-10 (0-10 μM; 48 hours) exhibits potent antiproliferative activity in a dose-dependent manner[1].
ZMF-10 (20 μM; 24 hours) suppresses the phosphorylation of PAK1 at Ser199 and Thr212[1].
ZMF-10 (10-40 μM; 24 hours) downregulates the expression of ERK, and suppresses the phosphorylation of c-Raf, MEK and ERK; up-regulates the expression of Bax and downregulates the expression of Bcl-2; induces apoptosis in a dose-dependent manner with the increase of early and late apoptotic cell population[1].
ZMF-10 (10-40 μM; 24 hours) inhibits the PI3K-AKT-mTOR signaling with the decreasing phosphorylation of AKT and mTOR; inhibits JNK1/2 and cells migration in MDA-MB-231 cells[1].
Cell Proliferation Assay | Cell Line: | MDA-MB-231[1] | | Concentration: | 0-10 μM | | Incubation Time: | 48 hours | | Result: | Exhibited potent antiproliferative activity in a dose-dependent manner with an IC50value of 3.48 μM. |
Immunofluorescence | Cell Line: | MDA-MB-231[1] | | Concentration: | 20 μM | | Incubation Time: | 24 hours | | Result: | Suppressed the phosphorylation of PAK1 at Ser199 and Thr212. |
Western Blot Analysis | Cell Line: | MDA-MB-231[1] | | Concentration: | 10, 20 and 40 μM | | Incubation Time: | 24 hours | | Result: | Downregulated the expression of ERK, and suppressed the phosphorylation of c-Raf, MEK and ERK; up-regulated the expression of Bax and downregulated the expression of Bcl-2. |
Apoptosis Analysis | Cell Line: | MDA-MB-231[1] | | Concentration: | 10, 20 and 40 μM | | Incubation Time: | 24 hours | | Result: | Induced apoptosis in a dose-dependent manner with the increase of early and late apoptotic cell population. |
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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. |
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